☆ 4.2 Review

Role of protein phosphorylation in cell signaling, disease, and the intervention therapy

MEDCOMM (2022)

相关参考文献

注意：仅列出部分参考文献，下载原文获取全部文献信息。

Review Pharmacology & Pharmacy

Current developments in extracellular-regulated protein kinase (ERK1/2) inhibitors

Yuzhen Niu et al.

Summary: In this review, the importance of the ERK1/2 signaling pathway in the treatment of various diseases and the current research on ERK1/2 inhibitors are summarized. The main approaches used to discover ERK inhibitors, including the advantages of computer-aided drug design, are also discussed.

DRUG DISCOVERY TODAY (2022)

添加到收藏夹

Article Pharmacology & Pharmacy

Asciminib: First Approval

Emma D. Deeks

Summary: Asciminib is a drug developed by Novartis for the treatment of Ph+ CML. It targets BCR-ABL1 tyrosine kinase and is effective against resistant mutations. It has received accelerated and full approvals, and further research is being conducted on its potential in CML treatment.

DRUGS (2022)

添加到收藏夹

Article Pharmacology & Pharmacy

Inhibition MNK-eIF4E-β-catenin preferentially sensitizes gastric cancer to chemotherapy

Xiaolin Yang et al.

Summary: Aberrant activation of eIF4E contributes to gastric cancer growth and resistance. Tomivosertib, a dual MNK1/2 inhibitor, enhances the sensitivity of gastric cancer to chemotherapy by suppressing MNK-eIF4E-beta-catenin. This study provides preclinical evidence for clinical trials using tomivosertib in combination with chemotherapy for gastric cancer.

FUNDAMENTAL & CLINICAL PHARMACOLOGY (2022)

添加到收藏夹

Article Biochemistry & Molecular Biology

VRK2 activates TNFa/NF-KB signaling by phosphorylating IKKss in pancreatic cancer

Jionghuang Chen et al.

Summary: NF-KB signaling is active in pancreatic cancer and plays a crucial role in its progression. This study demonstrates that VRK2 regulates TNFa/NF-KB signaling by interacting with IKKss and activating the pathway. VRK2 overexpression promotes the growth of pancreatic cancer cells and organoids. Inhibition of IKKss abolishes the promotive effect of VRK2. These findings suggest that VRK2 may serve as a potential therapeutic target for pancreatic cancer.

INTERNATIONAL JOURNAL OF BIOLOGICAL SCIENCES (2022)

添加到收藏夹

Review Biochemistry & Molecular Biology

Functional Roles of JNK and p38 MAPK Signaling in Nasopharyngeal Carcinoma

Lesley Jia Wei Pua et al.

Summary: JNK and p38 MAPK signaling pathways play important roles in nasopharyngeal carcinoma (NPC), promoting tumor processes such as cell proliferation, apoptosis, inflammation, metastasis, and angiogenesis. Although the underlying mechanisms are not fully understood, further research on JNK and p38 MAPK could provide important insights for diagnosis, prognosis, and treatment decision-making in NPC patients.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

添加到收藏夹

Article Biochemistry & Molecular Biology

Rigosertib and Cholangiocarcinoma: A Cell Cycle Affair

Alessio Malacrida et al.

Summary: This study investigated the mechanism of action of Rigosertib on cholangiocarcinoma cells EGI-1 using Western blotting technique. The results showed an increase in EMI1 and Cyclin B protein levels and a significant reduction in CDK1 phosphorylation after Rigosertib treatment. The expression of PLK1 increased after 24 hours of treatment and decreased after 48 hours. Additionally, p53 levels increased and its activity was found to be necessary for the effects of Rigosertib on cell viability in EGI-1 cells.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

添加到收藏夹

Article Biochemistry & Molecular Biology

The plastoglobule-localized protein AtABC1K6 is a Mn2+-dependent kinase necessary for timely transition to reproductive growth

Roberto Espinoza-Corral et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2022)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of Cysteine-targeting Covalent Protein Kinase Inhibitors

Xiaoyun Lu et al.

Summary: Small molecule covalent kinase inhibitors (CKIs) have advantages for sustained target inhibition and high selectivity, with major medicinal chemistry strategies involving the addition of a warhead to a reversible lead/inhibitor scaffold to generate CKIs, while also facing challenges in drug discovery in this area.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Chemistry, Medicinal

TDP-43 Modulation by Tau-Tubulin Kinase 1 Inhibitors: A New Avenue for Future Amyotrophic Lateral Sclerosis Therapy

Vanesa Nozal et al.

Summary: Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease characterized by the aggregation of protein TDP-43. In this study, TTBK1 inhibitors were identified as a promising therapeutic strategy for ALS. The novel pyrrolopyrimidine derivatives demonstrated their ability to reduce TDP-43 phosphorylation and preserve motor neurons in mouse models, suggesting their potential for future ALS therapy.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Multidisciplinary Sciences

Structural insights into inhibitor regulation of the DNA repair protein DNA-PKcs

Shikang Liang et al.

Summary: DNA-PKcs plays a crucial role in DNA repair and its inhibitors show potential for cancer treatment. In this study, cryo-EM structures of human DNA-PKcs in complex with inhibitors were obtained, providing insights into the mechanisms and specificities of the inhibitors.

NATURE (2022)

添加到收藏夹

Review Pharmacology & Pharmacy

Properties of FDA-approved small molecule protein kinase inhibitors: A 2022 update

Robert Roskoski

Summary: Due to the dysregulation of protein kinase activity, this enzyme family has become one of the most important drug targets in the 21st century. There are 68 FDA-approved therapeutic agents that target protein kinases, with six new drugs approved in 2021. These drugs are mainly used in the treatment of neoplasms and inflammatory diseases, with 58 drugs prescribed for tumor treatment. In addition, 18 drugs are used for the treatment of multiple diseases. This review summarizes the physicochemical properties of all FDA-approved small molecule protein kinase inhibitors.

PHARMACOLOGICAL RESEARCH (2022)

添加到收藏夹

Article Oncology

Bruton Tyrosine Kinase Inhibitors in B-Cell Malignancies: Their Use and Differential Features

Matt Shirley

Summary: The development of Bruton tyrosine kinase (BTK) inhibitors has dramatically improved the management of B-cell malignancies, with more advanced second and third-generation agents providing better tolerability and treatment options. These inhibitors have shown strong activity in various B-cell malignancies and are generally well-tolerated, with manageable adverse events through dosage adjustment. This review article summarizes the evidence supporting the role of BTK inhibitors in the management of B-cell malignancies, highlighting their differences and benefits.

TARGETED ONCOLOGY (2022)

添加到收藏夹

Review Biochemistry & Molecular Biology

Tumor-intrinsic and immune modulatory roles of receptor-interacting protein kinases

A. Justin Rucker et al.

Summary: Receptor-interacting protein kinase 1 (RIPK1) and RIPK3 play crucial roles in regulating cell death and inflammation, and tumors have found ways to exploit them for their own benefit. RIPK-driven cell death can enhance antitumor immunity, but it can also induce inflammation and aid tumor progression.

TRENDS IN BIOCHEMICAL SCIENCES (2022)

添加到收藏夹

Review Oncology

25 Years of Adjuvant Therapy in Melanoma: A Perspective on Current Approvals and Insights into Future Directions

Thach-Giao Truong et al.

CURRENT ONCOLOGY REPORTS (2022)

添加到收藏夹

Editorial Material Oncology

Precision Targeting of Mutant PI3Ka in Cancer by Selective Degradation

Bart Vanhaesebroeck et al.

Summary: PIK3CA is a frequently activated kinase gene in solid tumors. This study shows that the PI3Kα inhibitors taselisib and inavolisib can induce degradation of mutant p110α protein in breast cancer cells that are positive for HER2 RTK, thereby limiting feedback-mediated drug resistance and potentially widening the therapeutic range of PI3Kα inhibition.

CANCER DISCOVERY (2022)

添加到收藏夹

Article Multidisciplinary Sciences

The efficacy of PI3Kγ and EGFR inhibitors on the suppression of the characteristics of cancer stem cells

Yanning Xu et al.

Summary: This study established a model of cancer stem cells (CSCs) derived from mouse induced pluripotent stem cells (miPSCs) and found that the activation of PI3K-Akt and EGFR signaling pathways played significant roles in the process. The inhibitors targeting these pathways showed significant anti-tumor effects in vitro and in vivo, with PI3K-gamma inhibitor Eganelisib demonstrating better therapeutic efficacy and fewer side effects.

SCIENTIFIC REPORTS (2022)

添加到收藏夹

Article Respiratory System

RAGE mediates airway inflammation via the HDAC1 pathway in a toluene diisocyanate-induced murine asthma model

Xianru Peng et al.

Summary: In this study, it was found that RAGE regulates the expression of HDAC1 through the PI3K/AKT pathway, and inhibition of HDAC prevents TDI-induced airway inflammation.

BMC PULMONARY MEDICINE (2022)

添加到收藏夹

Review Cell Biology

Structural Aspects of LIMK Regulation and Pharmacology

Deep Chatterjee et al.

Summary: This review focuses on the regulation of actin cytoskeleton dynamics by LIMKs and their potential therapeutic applications in diseases such as neurological disorders and cancer. It provides a comprehensive understanding of the LIMK conformational space, its catalytic mechanism, and the regulation of its activity, shedding light on substrate recognition. The implications of these structural features on drug discovery are also discussed, along with potential future directions for targeting LIMKs beyond kinase inhibition.

CELLS (2022)

添加到收藏夹

Article Medicine, Research & Experimental

Functional impact and targetability of PI3KCA, GNAS, and PTEN mutations in a spindle cell rhabdomyosarcoma with MYOD1 L122R mutation

Florence Choo et al.

Summary: This study established and characterized a new patient-derived ssRMS cell line harboring MYOD1 L122R mutation and alterations in PTEN, PIK3CA, and GNAS. It was found that PIK3CA(I459_T462del) is a constitutively active kinase, and both PI3K/AKT/mTOR and RAS/MAPK pathways are activated in this cell line. Additionally, dual PI3K/mTOR and AKT inhibitors showed dose-dependent reductions in cell growth. These findings suggest that molecularly targeted therapies may be effective in PI3K/AKT/mTOR activated ssRMS.

COLD SPRING HARBOR MOLECULAR CASE STUDIES (2022)

添加到收藏夹

Review Hematology

Long-term safety review of tyrosine kinase inhibitors in chronic myeloid leukemia- What to look for when treatment-free remission is not an option

Jeffrey H. Lipton et al.

Summary: The development of BCR::ABL1-targeting tyrosine kinase inhibitors has improved the prognosis of patients with chronic myeloid leukemia. Differences in safety profiles between TKIs allow for personalized treatment plans based on various factors. This review summarizes the safety profiles of currently approved TKIs and their impact on treatment selection, as well as strategies to manage adverse events and comorbidities.

BLOOD REVIEWS (2022)

添加到收藏夹

Review Oncology

Emerging strategies for TNBC with early clinical data: new chemoimmunotherapy strategies

Peter E. Hall et al.

Summary: The review highlights the complexity of chemoimmunotherapy strategies for triple-negative breast cancer, emphasizing the importance of considering the type and sequence of chemotherapy agents to optimize the response to immune checkpoint inhibitors. The emerging therapeutic class of antibody-drug conjugates in combination with immune checkpoint inhibitors shows promise for the treatment of triple-negative breast cancer.

BREAST CANCER RESEARCH AND TREATMENT (2022)

添加到收藏夹

Article Environmental Sciences

Exploration of binding mechanism of triclosan towards cancer markers using molecular docking and molecular dynamics

Prashant Bhardwaj et al.

Summary: The goal of this study is to investigate the protein binding patterns of TCS and proteins from various cancer signaling pathways. Through molecular docking and molecular dynamics simulation, it was found that AIF and JNK proteins may play a key role in TCS-mediated reactions.

CHEMOSPHERE (2022)

添加到收藏夹

Article Cardiac & Cardiovascular Systems

Evidence-Based Medical Therapy in Patients With Heart Failure With Reduced Ejection Fraction and Chronic Kidney Disease

Iris E. Beldhuis et al.

Summary: Chronic kidney disease is a common comorbidity in patients with heart failure and is associated with increased severity and poor cardiovascular outcomes. Limited information is available on the efficacy and safety of heart failure therapies in patients with severe CKD, particularly in stage 5 CKD. However, some drug classes have shown evidence of safety and efficacy in patients with stage 4 CKD. Additionally, the decline in eGFR observed with the initiation of certain heart failure drug classes does not necessarily indicate a worsening condition and should not lead to discontinuation of life-saving therapies.

CIRCULATION (2022)

添加到收藏夹

Review Oncology

Development of asciminib, a novel allosteric inhibitor of BCR-ABL1

Delphine Rea et al.

Summary: This article discusses the mechanism and clinical challenges of chronic myeloid leukemia, as well as the development and potential application of a new drug called Asciminib.

CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY (2022)

添加到收藏夹

Article Pharmacology & Pharmacy

RETRA induces necroptosis in cervical cancer cells through RIPK1, RIPK3, MLKL and increased ROS production

Suchitra Mohanty et al.

Summary: The study found that RETRA selectively induces necroptosis in cervical cancer cells without cytotoxic effects on normal cells. The induction of cell death by RETRA is associated with mitochondrial hyperpolarization and increased ROS production, emphasizing its importance in the treatment of cervical cancer.

EUROPEAN JOURNAL OF PHARMACOLOGY (2022)

添加到收藏夹

Article Biochemistry & Molecular Biology

Crosstalk between p38 MAPK and GR Signaling

Lisa Zeyen et al.

Summary: The p38 MAPK pathway is important for cellular stress response. It regulates downstream effectors to control inflammation and cellular processes. Dysregulation of this pathway is associated with inflammatory diseases and cancer. Glucocorticoids (GCs) secretion is a classical endocrine response to stress and is regulated by the glucocorticoid receptor (GR). The crosstalk between p38 and GR plays a role in gene expression regulation and has potential clinical applications.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2022)

添加到收藏夹

Article Oncology

Identification of the JNK-Active Triple-Negative Breast Cancer Cluster Associated With an Immunosuppressive Tumor Microenvironment

Takashi Semba et al.

Summary: The study identified that high phosphorylated JNK level in TNBC is associated with increased Treg infiltration. Inhibition of JNK signaling led to reduced tumor growth and Treg infiltration, and increased CD8(+) T cell infiltration, possibly through suppression of CCL2 secretion. This suggests that targeting the JNK/C-JUN/CCL2 axis may offer new therapeutic strategies for combating the aggressiveness of TNBC.

JNCI-JOURNAL OF THE NATIONAL CANCER INSTITUTE (2022)

添加到收藏夹

Article Genetics & Heredity

ASK1 is a novel molecular target for preventing aminoglycoside-induced hair cell death

Jacqueline M. Ogier et al.

Summary: Aminoglycoside antibiotics can cause toxic effects on the sensory hair cells in the inner ear, leading to permanent hearing loss and vestibular impairment. This study investigates the potential of ASK1 inhibition as a novel strategy to prevent aminoglycoside ototoxicity, providing significant pre-clinical evidence.

JOURNAL OF MOLECULAR MEDICINE-JMM (2022)

添加到收藏夹

Review Oncology

Treatment strategies and outcomes for patients with EGFR-mutant non-small cell lung cancer resistant to EGFR tyrosine kinase inhibitors: Focus on novel therapies

Melissa Johnson et al.

Summary: Tyrosine kinase inhibitors (TKIs) are the standard treatment for patients with EGFR-mutant non-small cell lung cancer (NSCLC). Despite the initial effectiveness of TKIs, almost all patients eventually develop resistance. Current research focuses on developing novel therapies to overcome resistance mechanisms.

LUNG CANCER (2022)

添加到收藏夹

Article Oncology

In vitro anticancer effects of alpelisib against PIK3CA-mutated canine hemangiosarcoma cell lines

Marika Maeda et al.

Summary: Hemangiosarcoma (HSA) is a malignant neoplasm with poor prognosis, especially in canines, and can serve as a valuable model for intractable human diseases. The high frequency of PIK3CA mutations in canine HSA affects the EGFR signaling pathway, and the molecular targeted drug alpelisib shows significant antitumor effects against these mutations.

ONCOLOGY REPORTS (2022)

添加到收藏夹

Article Endocrinology & Metabolism

Targeted therapies in the medical management of craniopharyngioma

Pedro Iglesias

Summary: Craniopharyngioma is a benign intracranial tumor that shows aggressive behavior and high recurrence rate. Recent studies have identified genetic alterations in different histological types of craniopharyngioma, indicating the potential use of targeted drugs as a therapeutic option.

PITUITARY (2022)

添加到收藏夹

Article Multidisciplinary Sciences

Combining explainable machine learning, demographic and multi-omic data to inform precision medicine strategies for inflammatory bowel disease

Laura-Jayne Gardiner et al.

Summary: This study proposes an explainable machine learning approach that integrates bioinformatics and domain insights to predict inter-patient variation in drug response for inflammatory bowel diseases (IBDs). The researchers identified important predictive features, including genomic, transcriptomic, demographic, medicinal, and pharmacological data. The study showed that patient characteristics and genetic polymorphisms are associated with variations in drug effectiveness for anti-inflammatory treatment.

PLOS ONE (2022)

添加到收藏夹

Article Oncology

RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy

Kyung W. Song et al.

Summary: The PI3K inhibitors GDC-0077 and taselisib have a unique mechanism of action by degrading mutant p110a protein, leading to more potent inhibition of mutant PI3K pathway signaling and cell viability, and better maintenance of prolonged pathway suppression.

CANCER DISCOVERY (2022)

添加到收藏夹

Article Chemistry, Medicinal

2-Aminoquinazolines as LRRK2 Inhibitors for Treating Parkinson’s Disease

Ram W. Sabnis

ACS Medicinal Chemistry Letters (2022)

添加到收藏夹

Article Multidisciplinary Sciences

Preventing erosion of X-chromosome inactivation in human embryonic stem cells

Marissa Cloutier et al.

Summary: Cloutier et al. discovered that inhibitors of GSK3 proteins in the culture medium can reduce X-chromosome inactivation in human embryonic stem cells, leading to equal expression of X-linked genes between females and males. These findings are significant for the faithful culture of hESCs.

NATURE COMMUNICATIONS (2022)

添加到收藏夹

Article Pharmacology & Pharmacy

A Novel N-Arylpyridone Compound Alleviates the Inflammatory and Fibrotic Reaction of Silicosis by Inhibiting the ASK1-p38 Pathway and Regulating Macrophage Polarization

Mingming Fan et al.

Summary: AKEX0011, a novel N-arylpyridone compound, has been found to have protective effects against silicosis. It ameliorates lung damage and respiratory dysfunction caused by silica, reduces the secretion of inflammatory and fibrotic factors, inhibits cell apoptosis and signaling pathways, and regulates macrophage polarization.

FRONTIERS IN PHARMACOLOGY (2022)

添加到收藏夹

Review Endocrinology & Metabolism

Peptide Receptor Radionuclide Therapy in Thyroid Cancer

Sriram Gubbi et al.

Summary: The currently available treatment options for RAI-refractory thyroid cancers are limited. Peptide receptor radionuclide therapy (PRRT) has the potential to be an effective and safe treatment for patients with SSTR-positive RAI-refractory DTCs and MTCs. However, further research is needed in this field.

FRONTIERS IN ENDOCRINOLOGY (2022)

添加到收藏夹

Article Oncology

Harnessing radiotherapy-induced NK-cell activity by combining DNA damage-response inhibition and immune checkpoint blockade

Emmanuel C. Patin et al.

Summary: This study identifies a role for NK cells in the antitumor immune response to radiotherapy that can be enhanced by small-molecule DNA damage-response inhibitors and immune checkpoint blockade, with promising translational potential in clinical samples.

JOURNAL FOR IMMUNOTHERAPY OF CANCER (2022)

添加到收藏夹

Article Oncology

CK1 Is a Druggable Regulator of Microtubule Dynamics and Microtubule-Associated Processes

Aileen Roth et al.

Summary: Protein kinases of the Casein Kinase 1 family are essential for the regulation of various cellular processes, including microtubule dynamics. They directly modulate microtubule dynamics by phosphorylating tubulin isoforms and microtubule-associated proteins, which can affect microtubule stability and genomic stability. Therefore, targeting Casein Kinase 1 functions may be a potential therapeutic strategy for cancer treatment.

CANCERS (2022)

添加到收藏夹

Article Cell Biology

MicroRNA-145 Impairs Classical Non-Homologous End-Joining in Response to Ionizing Radiation-Induced DNA Double-Strand Breaks via Targeting DNA-PKcs

Muddenahalli Srinivasa Sudhanva et al.

Summary: This study demonstrates that miR-145 suppresses DNA-PKcs expression, affecting DNA double-strand break repair and rendering cells sensitive to ionizing radiation. Additionally, miR-145 inhibition is associated with increased Akt1 phosphorylation and upregulation of DNA-PKcs in cancer cells.

CELLS (2022)

添加到收藏夹

Article Cell Biology

Extracellular Matrix Stiffness and TGFβ2 Regulate YAP/TAZ Activity in Human Trabecular Meshwork Cells

Haiyan Li et al.

Summary: Progression of primary open-angle glaucoma is associated with increased trabecular meshwork (HTM) stiffness and elevated TGF beta 2 levels. YAP/TAZ, important factors in mechanotransduction, play a role in glaucomatous HTM cell dysfunction. Increased ECM stiffness elevates nuclear localization of YAP/TAZ, potentially through modulating focal adhesions and cytoskeletal rearrangement. TGF beta 2 also increases nuclear YAP/TAZ in HTM cells, which can be prevented by inhibiting ERK and ROCK signaling pathways. Inactivation of YAP/TAZ with verteporfin partially blocks TGF beta 2-induced hydrogel contraction and stiffening. This study provides evidence for the pathological role of aberrant YAP/TAZ signaling in glaucomatous HTM cell dysfunction and suggests potential strategies for preventing progressive ocular hypertension in glaucoma.

FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY (2022)

添加到收藏夹

Article Veterinary Sciences

Pharmacokinetic Exposures Associated With Oral Administration of Sorafenib in Dogs With Spontaneous Tumors

Jacob R. Cawley et al.

Summary: This study evaluated the pharmacokinetics of sorafenib in tumor-bearing dogs and found that a twice-daily oral dose of 3 mg/kg was well-tolerated without any adverse events.

FRONTIERS IN VETERINARY SCIENCE (2022)

添加到收藏夹

Article Biochemistry & Molecular Biology

Targeting CDK4/6 for Anticancer Therapy

Jiating Qi et al.

Summary: This article summarizes the targeted therapies for cyclin-dependent kinase 4/6 (CDK4/6), including CRISPR, siRNA, and drug inhibition. It highlights the mechanisms of small molecular inhibitors and drug resistance, and describes strategies to combat resistance.

BIOMEDICINES (2022)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of novel 7,8-dihydropteridine-6(5H)-one-based DNA-PK inhibitors as potential anticancer agents via scaffold hopping strategy

Zongbao Ding et al.

Summary: DK1 is a novel DNA-PK inhibitor with great potential for further study. It has favorable drug-like properties and in vivo pharmacokinetics as an oral drug candidate. When used in combination with doxorubicin, DK1 shows synergistic antiproliferative activity against various cancer cell lines.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Review Immunology

Targeting PARP1 to Enhance Anticancer Checkpoint Immunotherapy Response: Rationale and Clinical Implications

Carlos Wagner S. Wanderley et al.

Summary: The use of immune checkpoint inhibitors (ICIs) in cancer treatment has revolutionized the field, but prolonged use of ICIs has resulted in a specific response to certain types of cancer. To overcome resistance and improve outcomes, researchers have explored novel strategies involving the combination of ICIs with other therapies. One promising class of agents is poly ADP-ribose polymerase inhibitors (PARPi), which have the potential to enhance the antitumor immune response through various mechanisms.

FRONTIERS IN IMMUNOLOGY (2022)

添加到收藏夹

Article Gastroenterology & Hepatology

Phosphoproteomics identifies pathways underlying the role of receptor-interaction protein kinase 3 in alcohol-associated liver disease and uncovers apoptosis signal-regulating kinase 1 as a target

Vaibhav Singh et al.

Summary: This study investigates the impact of chronic ethanol feeding on the hepatic phosphoproteome, focusing on the death receptor signaling pathways. It is found that chronic ethanol dysregulates these pathways and decreases the inhibitory phosphorylation of ASK1, a critical protein involved in programmed cell death. Furthermore, the study suggests the involvement of noncanonical functions of RIP3 in alcohol-associated liver disease.

HEPATOLOGY COMMUNICATIONS (2022)

添加到收藏夹

Article Ophthalmology

The Therapeutic Roles of Recombinant Hsp90α on Cornea Epithelial Injury

Mingli Wang et al.

Summary: The study reveals that Hsp90α is upregulated and secreted after corneal injury, promoting the healing process. Recombinant Hsp90α can accelerate wound healing of injured corneal epithelium and may be a promising drug candidate for corneal injury treatment.

INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE (2022)

添加到收藏夹

Article Oncology

Phase I Study of Alvocidib Followed by 7+3 (Cytarabine plus Daunorubicin) in Newly Diagnosed Acute Myeloid Leukemia

Joshua F. Zeidner et al.

Summary: Alvocidib, when combined with 7+3 induction therapy, shows promising clinical activity in newly diagnosed acute myeloid leukemia patients, indicating the potential for further investigation of Alvocidib combinations in this population.

CLINICAL CANCER RESEARCH (2021)

添加到收藏夹

Article Immunology

Rigosertib inhibits MEK1-ERK pathway and alleviates lipopolysaccharide-induced sepsis

Yin Wang et al.

Summary: Rigosertib showed potential effects on sepsis in WT mice, but not in MEK1(DD) mice with constitutive activation of MEK1 signaling.

IMMUNITY INFLAMMATION AND DISEASE (2021)

添加到收藏夹

Review Biochemistry & Molecular Biology

Evaluating the current status of protein kinase C (PKC)-protein kinase D (PKD) signalling axis as a novel therapeutic target in ovarian cancer

Komal Tyagi et al.

Summary: Ovarian cancer, particularly high grade serous ovarian cancer, remains a lethal gynaecological malignancy with high relapse rates despite advancements in targeted therapies and immunotherapies. The signaling cascade initiated by protein kinase C (PKC) and protein kinase D (PKD) regulates various cellular processes involved in tumorigenesis, making it a potential novel target in the treatment of this deadly pathology. Studies have also highlighted the significance of recent clinical trials and development of small molecule inhibitors targeting the PKC/PKD signaling axis in ovarian cancer.

BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER (2021)

添加到收藏夹

Review Dermatology

Janus kinase inhibitors for atopic dermatitis: a promising treatment modality

A. M. Cartron et al.

Summary: Atopic dermatitis is a chronic inflammatory skin disease that can significantly impact sleep quality and quality of life. Recent studies suggest that inhibition of the JAK signaling pathway may offer a promising therapeutic approach to reduce inflammation in AD.

CLINICAL AND EXPERIMENTAL DERMATOLOGY (2021)

添加到收藏夹

Article Oncology

LXH254, a Potent and Selective ARAF-Sparing Inhibitor of BRAF and CRAF for the Treatment of MAPK-Driven Tumors

Kelli-Ann Monaco et al.

Summary: LXH254, a novel RAF inhibitor, demonstrates potent inhibition of BRAF and CRAF while sparing ARAF. Loss of ARAF, but not BRAF or CRAF, sensitizes RAS-mutant cells to LXH254, which requires both kinase function and dimerization. In cells expressing only ARAF, LXH254 leads to paradoxical activation of MAPK signaling similar to dabrafenib.

CLINICAL CANCER RESEARCH (2021)

添加到收藏夹

Article Urology & Nephrology

Effects of the Soluble Guanylate Cyclase Stimulator Praliciguat in Diabetic Kidney Disease A Randomized Placebo-Controlled Clinical Trial

John P. Hanrahan et al.

Summary: In this study, treatment with praliciguat for 12 weeks did not significantly reduce albuminuria compared with placebo in the primary efficacy analysis. However, observed changes in urine albumin-creatinine ratio, blood pressure, and metabolic parameters may encourage further investigation of praliciguat in the treatment of diabetic kidney disease.

CLINICAL JOURNAL OF THE AMERICAN SOCIETY OF NEPHROLOGY (2021)

添加到收藏夹

Review Pharmacology & Pharmacy

Clinical Pharmacokinetics and Pharmacodynamics of Selumetinib

Olivia Campagne et al.

Summary: Selumetinib is approved for the treatment of neurofibromatosis in children and has shown promising results in various cancers. Its pharmacokinetic properties have been well characterized, with rapid absorption and minimal accumulation, supporting further evaluation in combination with other treatments.

CLINICAL PHARMACOKINETICS (2021)

添加到收藏夹

Article Cell Biology

Evidence of off-target effects of bosutinib that promote retinoic acid-induced differentiation of non-APL AML cells

Noor Kazim et al.

Summary: In this study, the effects of SFK inhibitor Bosutinib and engineered loss of Lyn on RA-induced leukemic cell differentiation were investigated. Both Bosutinib and Lyn loss promoted RA-induced differentiation, G0 arrest, and respiratory burst of HL-60 cells without affecting the expression and phosphorylation of signaling molecules driving differentiation. This suggests a novel Lyn-independent effect of Bosutinib that enhances differentiation therapy.

CELL CYCLE (2021)

添加到收藏夹

Article Biology

Repurposing of gastric cancer drugs against COVID-19

Charu Sonkar et al.

Summary: The global pandemic of COVID-19 caused by SARS-CoV-2 poses a challenge for health management in gastric cancer patients. FDA-approved drugs for gastric cancer have high binding energies against SARS-CoV-2, potentially playing a key role in treatment for COVID-19 patients with gastric cancer as comorbidity. Kinases may serve as key therapeutic targets in the treatment of COVID-19.

COMPUTERS IN BIOLOGY AND MEDICINE (2021)

添加到收藏夹

Article Pharmacology & Pharmacy

Derazantinib: an investigational drug for the treatment of cholangiocarcinoma

Stephan Braun et al.

Summary: This review evaluates the clinical role of derazantinib, an investigational FGFR inhibitor, in patients with iCCA harboring actionable FGFR2 genetic aberrations. Derazantinib has shown clinically meaningful efficacy with durable objective responses, supporting its therapeutic potential in previously treated iCCA patients. The safety profile of derazantinib was manageable and compared favorably to other FGFR inhibitors, indicating the need for increased molecular profiling of cholangiocarcinoma patients.

EXPERT OPINION ON INVESTIGATIONAL DRUGS (2021)

添加到收藏夹

Article Oncology

Selective Oral MEK1/2 Inhibitor Pimasertib in Metastatic Melanoma: Antitumor Activity in a Phase I, Dose-Escalation Trial

Celeste Lebbe et al.

Summary: Results from this phase I study suggest that Pimasertib demonstrates clinical activity in patients with locally advanced/metastatic melanoma, particularly in tumors with BRAF and NRAS mutations, through inhibition of pERK in peripheral blood mononuclear cells.

TARGETED ONCOLOGY (2021)

添加到收藏夹

Review Biochemistry & Molecular Biology

Structural Insights Support Targeting ASK1 Kinase for Therapeutic Interventions

Veronika Obsilova et al.

Summary: ASK1, a crucial cellular stress sensor, activates JNKs and p38 MAPKs which when excessively activated can lead to cell death, inflammation and fibrosis. Targeted inhibition of ASK1, the upstream activator of these kinases, is a promising therapeutic strategy for treating various severe conditions including neurological disorders, cardiovascular diseases, diabetes and cancer.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

The Sphingosine Kinase 2 Inhibitor ABC294640 Restores the Sensitivity of BRAFV600E Mutant Colon Cancer Cells to Vemurafenib by Reducing AKT-Mediated Expression of Nucleophosmin and Translationally-Controlled Tumour Protein

Petra Grbcic et al.

Summary: This study demonstrates that increased sphingosine kinase activity in resistant cells plays a role in vemurafenib resistance, and inhibiting this activity can enhance the anti-proliferative effect of PLX4032. Additionally, the combination of ABC294640 and PLX4032 shows enhanced inhibition of cell proliferation, migration, clonogenicity, and induction of apoptosis compared to single drug treatments.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

添加到收藏夹

Article Oncology

Enhanced antitumor immunity by a novel small molecule HPK1 inhibitor

Dan You et al.

Summary: This study identified a novel, potent, and selective HPK1 small molecule kinase inhibitor called Compound K (CompK), which significantly improved human T-cell immune responses in the tumor microenvironment and showed significant synergy with anti-PD-1 therapy. Animal model studies demonstrated improved immune responses and antitumor efficacy with CompK in combination with anti-PD-1, suggesting its potential as a novel pharmacological agent for cancer treatment.

JOURNAL FOR IMMUNOTHERAPY OF CANCER (2021)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of the c-Jun N-Terminal Kinase Inhibitor CC-90001

Mark A. Nagy et al.

Summary: A novel series of JNK inhibitors with increased JNK1 bias have been identified through synthesis and SAR studies, showing low nanomolar JNK inhibitory potency, overall kinome selectivity, and the ability to inhibit cellular phosphorylation of the direct JNK substrate c-Jun. Physiochemical optimization in this series led to compounds with excellent systemic exposure post oral dosing, leading to the selection of a clinical development candidate, CC-90001, currently in Phase II trials for patients with idiopathic pulmonary fibrosis.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Cell Biology

Inhibition of Aurora Kinase B activity disrupts development and differentiation of salivary glands

Abeer K. Shaalan et al.

Summary: Research on the role of AURKB during embryonic development reveals its crucial function in supporting organogenesis and differentiation, while inhibiting senescence-inducing signals.

CELL DEATH DISCOVERY (2021)

添加到收藏夹

Article Oncology

NTRK fusions in lung cancer: From biology to therapy

Guilherme Harada et al.

Summary: Fusions involving TRK protein tyrosine kinases are oncogenic drivers in various tumors, with first-generation TRK inhibitors showing clinically meaningful antitumor activity but on-target resistance needs to be monitored. These inhibitors should be considered as first-line therapeutic options for TRK fusion-positive lung cancers, and next-generation TRK inhibitors are being studied for addressing resistance mechanisms.

LUNG CANCER (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

IL4/IL4R signaling promotes the osteolysis in metastatic bone of CRC through regulating the proliferation of osteoclast precursors

Qian Jin et al.

Summary: This study reveals the crucial role of IL4/IL4R signaling in promoting the proliferation of osteoclast precursor cells in bone metastasis of colorectal cancer. Additionally, activation of the ERK pathway is closely associated with this process. Ravoxertinib could potentially serve as a new therapeutic target for bone metastasis of colorectal cancer.

MOLECULAR MEDICINE (2021)

添加到收藏夹

Article Cell Biology

AS602801 sensitizes glioma cells to temozolomide and vincristine by blocking gap junction communication between glioma cells and astrocytes

Shuai Zhang et al.

Summary: AS602801 downregulated CX43 expression by inhibiting JNK, reducing gap junction activity between glioma cells and astrocytes. AS602801 significantly enhanced TMZ/VCR-induced glioma cell apoptosis and restored its inhibitory effect on p-JNK, CX43, and CASP-3 expression. This study suggests that AS602801 may serve as a novel adjuvant chemotherapeutic agent in the treatment of glioma.

JOURNAL OF CELLULAR AND MOLECULAR MEDICINE (2021)

添加到收藏夹

Review Pharmacology & Pharmacy

Blockade of mutant RAS oncogenic signaling with a special emphasis on KRAS

Robert Roskoski

Summary: RAS proteins play crucial roles in physiological signal transduction processes related to cell growth, division, and survival. RAS mutations, especially KRAS mutations, are common in various cancers, with potential implications for targeted therapy. Covalent modification of the KRAS C12 led to the discovery of a new pocket, facilitating the development of second-line treatment for KRAS(G12C)-mutant non-small cell lung cancer. Efforts are also being made to develop inhibitors targeting MAP kinase and PI3-kinase pathways as indirect RAS antagonists.

PHARMACOLOGICAL RESEARCH (2021)

添加到收藏夹

Article Multidisciplinary Sciences

Discovery of small molecule guanylyl cyclase A receptor positive allosteric modulators

S. Jeson Sangaralingham et al.

Summary: The discovery and development of an oral, small molecule GC-A PAM holds great potential as a therapeutic for cardiovascular, renal, and metabolic diseases by enhancing ANP-mediated cGMP generation and inhibiting cardiomyocyte hypertrophy.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2021)

添加到收藏夹

Review Oncology

Research update on the anticancer effects of buparlisib

Jinshan Xing et al.

Summary: Buparlisib is a potent and selective PI3K inhibitor that inhibits four isomers of PI3K, playing a role in inhibiting cell proliferation, promoting apoptosis, and blocking angiogenesis through antagonizing the PI3K/AKT pathway. It has demonstrated clinical efficacy in solid tumors and hematological malignancies.

ONCOLOGY LETTERS (2021)

添加到收藏夹

Article Multidisciplinary Sciences

Inhibition of casein kinase 1 δ/ε improves cognitive performance in adult C57BL/6J mice

Heather Mahoney et al.

Summary: Time-of-day effects have been observed in cognitive behavioral tests, and disruption of the circadian system can impair hippocampus-dependent learning and memory. Modulation of circadian kinases, such as CK1 delta/epsilon, presents a novel approach for improving cognitive deficits. The inhibitor PF-670462 showed potential in enhancing cognitive performance in mice, suggesting the utility of CK1 delta/epsilon inhibition in improving time-of-day cognitive performance.

SCIENTIFIC REPORTS (2021)

添加到收藏夹

Review Neurosciences

Brain-Derived Neurotrophic Factor Signaling in Depression and Antidepressant Action

Eero Castren et al.

Summary: Neurotrophic factors, especially BDNF, are associated with depression and the action of antidepressant drugs, with impaired BDNF signaling linked to mood disorders. Increased BDNF expression and signaling have been linked to the mechanisms of antidepressant drugs, and BDNF regulates various types of neuronal plasticities in the brain, which are connected to antidepressant action. The hypothesis of a connection between neurotrophic factors and neuronal plasticity with mood disorders and antidepressant action has been further supported by recent evidence.

BIOLOGICAL PSYCHIATRY (2021)

添加到收藏夹

Article Oncology

Immune modulating activity of the CHK1 inhibitor prexasertib and anti-PD-L1 antibody LY3300054 in patients with high-grade serous ovarian cancer and other solid tumors

Khanh T. Do et al.

Summary: The combination of CHK1 inhibitor prexasertib and anti-PD-L1 antibody LY3300054 showed tolerability and preliminary activity in CCNE1-amplified HGSOC patients, with evidence of cytotoxic T-cell activation in patient blood samples.

CANCER IMMUNOLOGY IMMUNOTHERAPY (2021)

添加到收藏夹

Article Pharmacology & Pharmacy

Vericiguat: First Approval

Anthony Markham et al.

Summary: Vericiguat is a soluble guanylate cyclase stimulator developed for the treatment of chronic heart failure. It enhances the effects of nitric oxide by stimulating sGC and cGMP production independently of nitric oxide. Recently approved in the USA for reducing the risk in patients with heart failure and ejection fraction < 45%.

DRUGS (2021)

添加到收藏夹

Article Chemistry, Medicinal

Developing novel classes of protein kinase CK1δ inhibitors by fusing [1,2,4]triazole with different bicyclic heteroaromatic systems

Ilenia Grieco et al.

Summary: Protein kinase CK1 delta plays a crucial role in various neuroinflammatory and neurodegenerative diseases, making it a potential therapeutic target. The development of ATP competitive inhibitors for CK1 delta, such as [1,2,4]triazolo[1,5-c]pyrimidines and [1,2,4]triazolo[1,5-a][1,3,5] triazines, represents a promising approach for future treatments. By identifying key interactions and structures, researchers aim to develop new inhibitors capable of crossing the blood-brain barrier for more effective treatment options.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Immunology

VRK2 inhibition synergizes with PD-1 blockade to improve T cell responses

Michael Peled et al.

Summary: The study revealed that VRK2 plays a key role in PD-1 signaling, and combination therapy of VRK2 inhibitors with PD-1 blockade enhances T cell activation and improves tumor clearance.

IMMUNOLOGY LETTERS (2021)

添加到收藏夹

Review Oncology

Biological Significance and Targeting of the FGFR Axis in Cancer

Athina-Myrto Chioni et al.

Summary: FGFR signaling is essential for maintaining normal body homeostasis, facilitating growth and healing, but can be hijacked by cancer cells. Aberrant FGFR signaling in cancer, such as mutations, gene fusions, and amplifications, has led to the development of targeted therapies using FGFR inhibitors, tyrosine kinase inhibitors, ligand traps, and monoclonal antibodies. The complex nature of FGFR signaling and the heterogeneous tumor microenvironment may contribute to resistance to therapy with FGFR-directed agents.

CANCERS (2021)

添加到收藏夹

Review Oncology

Improving Outcomes of Tyrosine Kinase Inhibitors in Hepatocellular Carcinoma: New Data and Ongoing Trials

Lisha Mou et al.

Summary: Targeted therapies like TKIs are crucial for advanced HCC treatment, with combination therapies involving immune checkpoint inhibitors showing promise. Nanoparticle-based TKI delivery techniques are also expected to enhance treatment efficacy, making it more efficient.

FRONTIERS IN ONCOLOGY (2021)

添加到收藏夹

Article Oncology

ROCK2 Inhibition With Belumosudil (KD025) for the Treatment of Chronic Graft-Versus-Host Disease

Madan Jagasia et al.

Summary: The study demonstrated that treatment with belumosudil resulted in a high overall response rate and overall survival rate, along with quality-of-life improvements, corticosteroid dose reductions, and limited toxicity, suggesting that belumosudil may be an effective therapy for patients with treatment-refractory cGVHD.

JOURNAL OF CLINICAL ONCOLOGY (2021)

添加到收藏夹

Review Biochemistry & Molecular Biology

Recent Advances in Pain Management: Relevant Protein Kinases and Their Inhibitors

Francis Giraud et al.

Summary: This review emphasizes the role of protein kinases as potential biological targets in pain management, categorizing them into different groups in the human kinome and describing examples of small molecule inhibitors demonstrating analgesic effects. It highlights the fundamental role that protein kinase inhibitors could play in the development of new pain treatments.

MOLECULES (2021)

添加到收藏夹

Review Biotechnology & Applied Microbiology

Kinase drug discovery 20 years after imatinib: progress and future directions

Philip Cohen et al.

Summary: Advances in improving the potency and specificity of small-molecule protein kinase inhibitors over the past 20 years have had a significant impact on the treatment of cancers and non-cancerous conditions. Efforts are being made to address the challenge of drug resistance to kinase inhibitors, and future directions in kinase drug discovery are being discussed.

NATURE REVIEWS DRUG DISCOVERY (2021)

添加到收藏夹

Review Microbiology

Interplay Between CMGC Kinases Targeting SR Proteins and Viral Replication: Splicing and Beyond

Florentin Pastor et al.

Summary: Protein phosphorylation is crucial in regulating protein half-life, intracellular distribution, and activity, with CMGC kinases playing a key role in gene expression through splicing control. These kinases, belonging to different families, also influence viral replication, indicating potential translational opportunities.

FRONTIERS IN MICROBIOLOGY (2021)

添加到收藏夹

Review Oncology

JNK in Tumor Microenvironment: Present Findings and Challenges in Clinical Translation

Shing Yau Tam et al.

Summary: JNK, a stress-activated protein kinase, plays dual roles in cancer development by influencing cell proliferation, apoptosis, and immune responses. It also plays complex roles in the heterogeneous tumor microenvironment, impacting tumor development through various pathways.

CANCERS (2021)

添加到收藏夹

Article Chemistry, Medicinal

DNA Aptamers against Vaccinia-Related Kinase (VRK) 1 Block Proliferation in MCF7 Breast Cancer Cells

Rebeca Carrion-Marchante et al.

Summary: VRK1 is a serine/threonine kinase involved in DNA damage response and cell cycle progression. Through in vitro selection, high-affinity DNA aptamers targeting VRK1 have been identified and show potential as therapeutic agents for cancer treatment.

PHARMACEUTICALS (2021)

添加到收藏夹

Article Cell Biology

Upregulation of fibroblast growth factor 2 contributes to endometriosis through SPRYs/DUSP6/ERK signaling pathway

Xiaoyan Yu et al.

Summary: The study indicates that upregulation of FGF2 in endometriosis patients may promote the disease progression by affecting the regulation of the SPRYs/DUSP6/ERK signaling pathway.

ACTA HISTOCHEMICA (2021)

添加到收藏夹

Article Oncology

Phase 1 study of the ATR inhibitor berzosertib (formerly M6620, VX-970) combined with gemcitabine ± cisplatin in patients with advanced solid tumours

Mark R. Middleton et al.

Summary: The study demonstrated that berzosertib + gemcitabine is well tolerated in patients with advanced solid tumors and showed preliminary signs of efficacy. Berzosertib 210 mg/m(2) + gemcitabine 1000 mg/m(2) Q3W was established as the recommended Phase 2 dose.

BRITISH JOURNAL OF CANCER (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Human TBK1 deficiency leads to autoinflammation driven by TNF-induced cell death

Justin Taft et al.

Summary: The loss of TBK1 leads to decreased IFN-I induction but affects autoinflammation and TNF-induced cell death, and treatment with anti-TNF can improve the clinical condition of patients.

CELL (2021)

添加到收藏夹

Article Pharmacology & Pharmacy

Belumosudil: First Approval

Hannah A. Blair

Summary: Belumosudil, a ROCK inhibitor developed by Kadmon Pharmaceuticals, has received its first approval in the USA for the treatment of cGVHD. Regulatory reviews are underway in other countries, and clinical development for systemic sclerosis is ongoing in the USA.

DRUGS (2021)

添加到收藏夹

Review Pharmacology & Pharmacy

Lazertinib: First Approval

Sohita Dhillon

Summary: Lazertinib is a novel oral medication developed for the treatment of non-small cell lung cancer, targeting specific EGFR mutations. It received its first approval in 2021 for use in patients who have previously received EGFR-TKI therapy.

DRUGS (2021)

添加到收藏夹

Review Chemistry, Medicinal

An updated patent review of VEGFR-2 inhibitors (2017-present)

Thoraya A. Farghaly et al.

Summary: The VEGFR-2 signaling pathway plays a critical role in angiogenesis and has become an important target for treating angiogenesis-related diseases. Current treatment methods may face challenges such as poor response, development of resistance, and serious adverse effects, so combining different treatment methods and utilizing nanomedicine may enhance efficacy, reduce side effects, and lower costs.

EXPERT OPINION ON THERAPEUTIC PATENTS (2021)

添加到收藏夹

Review Biochemistry & Molecular Biology

New Structural Perspectives in G Protein-Coupled Receptor-Mediated Src Family Kinase Activation

Sandra Berndt et al.

Summary: SFKs are crucial regulators of cell proliferation, differentiation, and survival, with their expression strongly linked to cancer development and tumor progression. The regulation of SFKs through GPCR-mediated pathways is complex and may involve direct protein interactions or allosteric regulation by arrestins and G proteins. The potential direct interaction between GPCRs and SFKs could lead to a novel mechanism of SFK signaling and identification of new GPCR-SFK interactions.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

添加到收藏夹

Review Biochemistry & Molecular Biology

Role of JAK/STAT in Interstitial Lung Diseases; Molecular and Cellular Mechanisms

Paula Montero et al.

Summary: This review explores the activation of the JAK/STAT molecular pathway in ILDs and its impact on cellular fibrotic processes, highlighting the significant role of JAK/STAT in ILDs. It also discusses the potential therapeutic drugs targeting JAK/STAT and their application in vitro and in clinical trials.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

添加到收藏夹

Review Biochemistry & Molecular Biology

Bruton's Tyrosine Kinase Targeting in Multiple Myeloma

Max Von Suskil et al.

Summary: Multiple myeloma remains an incurable disease despite advancements in treatment, leading to aggressive relapses in patients. The cytosolic kinase BTK plays a crucial role in the survival of malignant clones and multiple myeloma stem cells, making it a promising therapeutic target. Inhibition of the BTK pathway may disrupt interactions between malignant clones and the bone marrow microenvironment in MM patients.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

A Computational Workflow for the Identification of Novel Fragments Acting as Inhibitors of the Activity of Protein Kinase CK1δ

Giovanni Bolcato et al.

Summary: Fragment-based drug discovery (FBDD) has become a consolidated approach in the drug discovery process, with successful applications seen in kinase inhibitors like Vemurafenib. CK1 δ, a protein kinase in the kinase family, has shown promise as a target in the treatment of neurodegenerative diseases such as Alzheimer's, Parkinson's, and ALS.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

添加到收藏夹

Review Biochemistry & Molecular Biology

The Roles of c-Jun N-Terminal Kinase (JNK) in Infectious Diseases

Jing Chen et al.

Summary: JNKs, as crucial MAPKs, play key roles in regulating cellular processes and may be important in infectious diseases. This review discusses the signaling properties of JNKs in apoptosis, autophagy, and inflammation, as well as their potential therapeutic roles in various infectious diseases.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

添加到收藏夹

Review Oncology

Mechanisms and management of 3rd-generation EGFR-TKI resistance in advanced non-small cell lung cancer (Review)

Jingyi He et al.

Summary: Targeted therapy with EGFR-TKIs is standard for advanced EGFR-mutated NSCLC, with osimertinib being a representative 3rd-generation TKI for T790M-positive patients. However, complex resistance mechanisms including altered signaling pathways and cellular transformations challenge treatment efficacy, highlighting the need for novel combination therapies in addressing acquired resistance.

INTERNATIONAL JOURNAL OF ONCOLOGY (2021)

添加到收藏夹

Review Allergy

JAK inhibitors in the treatment of atopic dermatitis

Raj Chovatiya et al.

Summary: Atopic dermatitis (AD) is a chronic inflammatory skin disorder with limited treatment options. Recent studies have shown that both topical and systemic Janus kinase (JAK) inhibitors hold promise in treating AD, with further research needed to fully understand their efficacy and safety.

JOURNAL OF ALLERGY AND CLINICAL IMMUNOLOGY (2021)

添加到收藏夹

Article Microbiology

Identification and Enzymatic Analysis of an Archaeal ATP-Dependent Serine Kinase from the Hyperthermophilic Archaeon Staphylothermus marinus

Yasunobu Mori et al.

Summary: This study reveals that the Serine kinases from the Desulfurococcales archaeal order utilize ATP as a phosphate donor, suggesting their role in serine assimilation. These enzymes show differences in properties compared to the Thermococcales enzymes, indicating a wider range of phosphate donors for phosphorylating free serine.

JOURNAL OF BACTERIOLOGY (2021)

添加到收藏夹

Editorial Material Cell Biology

Aurora A kinase activation: Different means to different ends

Nicolas Tavernier et al.

Summary: Aurora A is a key kinase involved in regulating mitotic processes. Recent studies have identified multiple mechanisms of Aurora A activation, each occurring at specific subcellular locations and regulated by signaling events.

JOURNAL OF CELL BIOLOGY (2021)

添加到收藏夹

Article Biochemical Research Methods

LC-MS/MS method for the quantification of the anti-cancer agent infigratinib: Application for estimation of metabolic stability in human liver microsomes

Gamal A. E. Mostafa et al.

Summary: Infigratinib (INF) is a novel small molecule inhibitor of human FGFRs, approved by the FDA for the treatment of cholangiocarcinoma. A validated LC-MS/MS method was developed to estimate the concentration of INF in the HLM matrix in this study.

JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES (2021)

添加到收藏夹

Article Chemistry, Medicinal

Inhibiting Eukaryotic Elongation Factor 2 Kinase: An Update on Pharmacological Small-Molecule Compounds in Cancer

Shiou Zhu et al.

Summary: Eukaryotic elongation factor 2 kinase (eEF2K) is a key negative regulator of protein synthesis in tumorigenesis, with potential for cancer therapy improvement through single-target inhibitors, repurposed drugs, dual-target inhibitors, drug combination strategies, and emerging technologies.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Targeting Rearranged during Transfection in Cancer: A Perspective on Small-Molecule Inhibitors and Their Clinical Development

Debasmita Saha et al.

Summary: Aberrant signaling of RET in cancers can be effectively treated through pharmacological manipulation, and there has been an increasing focus on developing specific therapies for RET in recent years. In 2020, the first kinase inhibitors specifically developed to target the RET oncoprotein were approved, marking a significant advancement in precision medicine for RET-driven malignancies.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Chemistry, Medicinal

Development of Cdc2-like Kinase 2 Inhibitors: Achievements and Future Directions

Zhen Qin et al.

Summary: Cdc2-like kinases (CLKs), including CLK2, are associated with various diseases and CLK2 has received attention as a regulator that phosphorylates proteins to modulate splicing processes. Numerous CLK2 inhibitors have been identified, with Lorecivivint being in phase 3 clinical trials, but highly selective inhibitors are rarely reported.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

添加到收藏夹

Article Virology

SARS-CoV-2 Disrupts Proximal Elements in the JAK-STAT Pathway

Da-Yuan Chen et al.

Summary: SARS-CoV-2 can infect multiple organs in the human body and evade host antiviral immunity by suppressing interferon signaling. Targeting viral mediators of immune evasion may help block virus replication.

JOURNAL OF VIROLOGY (2021)

添加到收藏夹

News Item Biotechnology & Applied Microbiology

TARGET WATCH eEF2K: an atypical kinase target for cancer

Louisa Temme et al.

NATURE REVIEWS DRUG DISCOVERY (2021)

添加到收藏夹

Review Gastroenterology & Hepatology

Stress-activated kinases as therapeutic targets in pancreatic cancer

Benno Traub et al.

Summary: Pancreatic cancer is a devastating disease with poor survival rates, prompting the need for new therapeutic approaches. Protein kinases play crucial roles in development and pathogenesis, making them potential targets for precision medicine in patients with deregulated kinase pathways.

WORLD JOURNAL OF GASTROENTEROLOGY (2021)

添加到收藏夹

Article Multidisciplinary Sciences

NGF-TrkA signaling dictates neural ingrowth and aberrant osteochondral differentiation after soft tissue trauma

Seungyong Lee et al.

Summary: Soft tissue trauma can induce NGF expression, leading to axonal invasion and abnormal osteochondral differentiation, which can be prevented by inhibition of NGF signaling.

NATURE COMMUNICATIONS (2021)

添加到收藏夹

Article Multidisciplinary Sciences

Adipose tissue-derived neurotrophic factor 3 regulates sympathetic innervation and thermogenesis in adipose tissue

Xin Cui et al.

Summary: Activation of brown fat thermogenesis increases energy expenditure and alleviates obesity, and NT-3 is a key fat-derived neurotrophic factor that regulates SNS innervation and energy metabolism in adipose tissue. Increasing NT-3 promotes beige adipocyte development and protects against diet-induced obesity, while TRKC haploinsufficiency leads to cold intolerance and susceptibility to obesity.

NATURE COMMUNICATIONS (2021)

添加到收藏夹

Article Oncology

Combined inhibition of AURKA and HSF1 suppresses proliferation and promotes apoptosis in hepatocellular carcinoma by activating endoplasmic reticulum stress

Zetian Shen et al.

Summary: This study evaluated the anti-tumor effect of co-inhibition of AURKA and HSF1 on hepatocellular carcinoma (HCC) cells, both in vitro and in vivo. The results showed that the combined inhibition led to increased cell apoptosis, potentially mediated by the endoplasmic reticulum stress (ERS) pathway. These findings suggest that AURKA and HSF1 may be promising targets for HCC treatment.

CELLULAR ONCOLOGY (2021)

添加到收藏夹

Article Respiratory System

Nemiralisib in Patients with an Acute Exacerbation of COPD: Placebo-Controlled, Dose-Ranging Study

William A. Fahy et al.

Summary: Inhaled nemiralisib did not improve lung function or reduce re-exacerbations in patients with acute exacerbations of COPD. However, the study demonstrated the feasibility of conducting large clinical trials in acutely exacerbating patients.

INTERNATIONAL JOURNAL OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (2021)

添加到收藏夹

Review Oncology

Akt Isoforms: A Family Affair in Breast Cancer

Alakananda Basu et al.

Summary: This article discusses the importance of breast cancer in women in the United States and the role of Akt isoforms in the development of breast cancer. While Akt isoforms share similar structures, they exhibit redundant, distinct, and opposite functions in breast cancer. Understanding the isoform-specific function of Akt is critical for effectively targeting the Akt signaling pathway in cancer therapy.

CANCERS (2021)

添加到收藏夹

Review Oncology

RET Inhibitors in Non-Small-Cell Lung Cancer

Priscilla Cascetta et al.

Summary: RET rearrangements in NSCLC act as a potential therapeutic target, with selective RET inhibitors showing higher efficacy rates and good tolerability, providing hope for patients with RET-positive NSCLC. Ongoing phase III clinical trials will definitively establish the efficacy of these inhibitors in RET-positive NSCLC patients.

CANCERS (2021)

添加到收藏夹

Review Oncology

New Angiogenic Regulators Produced by TAMs: Perspective for Targeting Tumor Angiogenesis

Irina Larionova et al.

Summary: This review discusses the impact and regulatory role of pro-angiogenic factors produced by macrophages on angiogenesis in the tumor microenvironment, as well as the limitations of current anti-angiogenic therapy. It highlights the complexity of angiogenesis regulation and potential future directions for targeting pro-angiogenic activity of tumor-associated macrophages.

CANCERS (2021)

添加到收藏夹

Review Chemistry, Multidisciplinary

CDK4/6 inhibitors: a brief overview and prospective research directions

Tenzin Adon et al.

Summary: The discovery of CDK4/6 inhibitors is considered a game-changer in cancer therapy, as their inhibition triggers cell cycle arrest and apoptosis. Targeting CDK4/6 has been proposed as a paradigm shift in anticancer approaches, and the development of effective inhibitors is becoming a promising cancer therapy.

RSC ADVANCES (2021)

添加到收藏夹

Article Oncology

FLT3 mutated acute myeloid leukemia: 2021 treatment algorithm

Naval Daver et al.

Summary: Approximately 30% of newly diagnosed AML patients have FLT3 gene mutations, with FLT3-ITDmut showing adverse prognostic impact. Guidelines recommend rapid molecular testing for FLT3(mut) and early use of targeted agents, but challenges remain in prolonged remission, limited options for refractory patients, and resistance mechanisms that call for multi-agent therapies.

BLOOD CANCER JOURNAL (2021)

添加到收藏夹

Article Oncology

Population pharmacokinetics of ATR inhibitor berzosertib in phase I studies for different cancer types

Nadia Terranova et al.

Summary: Berzosertib is a first-in-class inhibitor being developed in combination with chemotherapy for the treatment of advanced cancers. Population PK analysis showed that concentrations of berzosertib exceeded p-Chk1 IC50 at recommended phase II doses when combined with carboplatin, cisplatin, and gemcitabine, indicating its potential efficacy in these combinations without significant PK interactions.

CANCER CHEMOTHERAPY AND PHARMACOLOGY (2021)

添加到收藏夹

Review Oncology

Inhibitors targeting Bruton's tyrosine kinase in cancers: drug development advances

Tingyu Wen et al.

Summary: BTK inhibitor ibrutinib has revolutionized the management of B-cell malignancies by creating a chemotherapy-free era, with sales exceeding 230 billion dollars in just 6 years and becoming one of the top five best-selling medicines globally. Numerous clinical trials of BTK inhibitors were initiated in the past decade, with around 73 trials intensively announced or updated in the most recent 3 years.

LEUKEMIA (2021)

添加到收藏夹

Review Allergy

Clinical, Immunological, and Genetic Features in Patients with Activated PI3Kδ Syndrome (APDS): a Systematic Review

Mahnaz Jamee et al.

CLINICAL REVIEWS IN ALLERGY & IMMUNOLOGY (2020)

添加到收藏夹

Article Cell Biology

Brivanib, a multitargeted small-molecule tyrosine kinase inhibitor, suppresses laser-induced CNV in a mouse model of neovascular AMD

Lele Li et al.

JOURNAL OF CELLULAR PHYSIOLOGY (2020)

添加到收藏夹

Article Oncology

Population pharmacokinetics of vactosertib, a new TGF-β receptor type Ι inhibitor, in patients with advanced solid tumors

Su Young Jung et al.

CANCER CHEMOTHERAPY AND PHARMACOLOGY (2020)

添加到收藏夹

Article Oncology

A First-in-human Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor, in Patients With Relapsed/Refractory Hematologic Malignancies: Results From the European Study

Carmelo Carlo-Stella et al.

CLINICAL LYMPHOMA MYELOMA & LEUKEMIA (2020)

添加到收藏夹

Review Immunology

IRAK family in inflammatory autoimmune diseases

Lin-Chong Su et al.

AUTOIMMUNITY REVIEWS (2020)

添加到收藏夹

Review Pharmacology & Pharmacy

Protein kinase inhibitor-based cancer therapies: Considering the potential of nitric oxide (NO) to improve cancer treatment

Silvia Ghione et al.

BIOCHEMICAL PHARMACOLOGY (2020)

添加到收藏夹

Review Chemistry, Medicinal

Akt Pathway Inhibitors

Nne E. Uko et al.

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Review Chemistry, Medicinal

Tropomyosin receptor kinase inhibitors: an updated patent review for 2016-2019

Justin J. Bailey et al.

EXPERT OPINION ON THERAPEUTIC PATENTS (2020)

添加到收藏夹

Review Oncology

The role of bosutinib in the treatment of chronic myeloid leukemia

Carlo Gambacorti-Passerini et al.

FUTURE ONCOLOGY (2020)

添加到收藏夹

Review Pharmacology & Pharmacy

Discovery of ATR kinase inhibitor berzosertib (VX-970, M6620): Clinical candidate for cancer therapy

Lukas Gorecki et al.

PHARMACOLOGY & THERAPEUTICS (2020)

添加到收藏夹

Review Pharmacology & Pharmacy

Therapeutic potential of targeting mixed lineage kinases in cancer and inflammation

Kathleen A. Gallo et al.

PHARMACOLOGY & THERAPEUTICS (2020)

添加到收藏夹

Article Pharmacology & Pharmacy

Tirabrutinib: First Approval

Sohita Dhillon

DRUGS (2020)

添加到收藏夹

Article Ophthalmology

A pyruvate dehydrogenase kinase inhibitor prevents retinal cell death and improves energy metabolism in rat retinas after ischemia/reperfusion injury

Kota Sato et al.

EXPERIMENTAL EYE RESEARCH (2020)

添加到收藏夹

Article Critical Care Medicine

Safety and efficacy of nazartinib (EGF816) in adults with EGFR-mutant non-small-cell lung carcinoma: a multicentre, open-label, phase 1 study

Daniel S-W Tan et al.

LANCET RESPIRATORY MEDICINE (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Small-molecule agonists of the RET receptor tyrosine kinase activate biased trophic signals that are influenced by the presence of GFRa1 co-receptors

Sean Jmaeff et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2020)

添加到收藏夹

Article Multidisciplinary Sciences

Acute inhibition of the CNS-specific kinase TTBK1 significantly lowers tau phosphorylation at several disease relevant sites

Gregory M. Dillon et al.

PLOS ONE (2020)

添加到收藏夹

Article Cell & Tissue Engineering

Mesenchymal stem cells combined with liraglutide relieve acute lung injury through apoptotic signaling restrained by PKA/β-catenin

Xiaotong Yang et al.

STEM CELL RESEARCH & THERAPY (2020)

添加到收藏夹

Article Pharmacology & Pharmacy

Olinciguat, an Oral sGC Stimulator, Exhibits Diverse Pharmacology Across Preclinical Models of Cardiovascular, Metabolic, Renal, and Inflammatory Disease

Daniel P. Zimmer et al.

FRONTIERS IN PHARMACOLOGY (2020)

添加到收藏夹

Article Oncology

Pharmacologic Inhibitor of DNA-PK, M3814, Potentiates Radiotherapy and Regresses Human Tumors in Mouse Models

Frank T. Zenke et al.

MOLECULAR CANCER THERAPEUTICS (2020)

添加到收藏夹

Review Medicine, General & Internal

ROCK (RhoA/Rho Kinase) in Cardiovascular-Renal Pathophysiology: A Review of New Advancements

Teresa M. Seccia et al.

JOURNAL OF CLINICAL MEDICINE (2020)

添加到收藏夹

Article Medicine, Research & Experimental

Inhibition of Aurora Kinase B attenuates fibroblast activation and pulmonary fibrosis

Rajesh K. Kasam et al.

EMBO MOLECULAR MEDICINE (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Overexpression of microRNA-23a-5p induces myocardial infarction by promoting cardiomyocyte apoptosis through inhibited of PI3K/AKT signalling pathway

Jiechun Huang et al.

CELL BIOCHEMISTRY AND FUNCTION (2020)

添加到收藏夹

Article Pharmacology & Pharmacy

Copanlisib for the treatment of adults with relapsed follicular lymphoma

Massimo Magagnoli et al.

EXPERT REVIEW OF CLINICAL PHARMACOLOGY (2020)

添加到收藏夹

Review Biochemistry & Molecular Biology

Growth Inhibitory Signaling of the Raf/MEK/ERK Pathway

Pui-Kei Wu et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)

添加到收藏夹

Article Medicine, General & Internal

The Inhibition of Protein Kinase C β Contributes to the Pathogenesis of Preeclampsia by Activating Autophagy

Huanqiang Zhao et al.

EBIOMEDICINE (2020)

添加到收藏夹

Article Oncology

Pimasertib Versus Dacarbazine in Patients With UnresectableNRAS-Mutated Cutaneous Melanoma: Phase II, Randomized, Controlled Trial with Crossover

Celeste Lebbe et al.

CANCERS (2020)

添加到收藏夹

Article Oncology

Berzosertib plus gemcitabine versus gemcitabine alone in platinum-resistant high-grade serous ovarian cancer: a multicentre, open-label, randomised, phase 2 trial

Panagiotis A. Konstantinopoulos et al.

LANCET ONCOLOGY (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

GDC-0980 (apitolisib) treatment with gemcitabine and/or cisplatin synergistically reduces cholangiocarcinoma cell growth by suppressing the PI3K/Akt/mTOR pathway

Dong Kee Jang et al.

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Comparative Assessment of Protein Kinase Inhibitors in Public Databases and in PKIDB

Colin Bournez et al.

MOLECULES (2020)

添加到收藏夹

Article Parasitology

Use of kinase inhibitors against schistosomes to improve and broaden praziquantel efficacy

Sujeevi S. K. Nawaratna et al.

PARASITOLOGY (2020)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of SP-96, the first non-ATP-competitive Aurora Kinase B inhibitor, for reduced myelosuppression

Naga Rajiv Lakkaniga et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Oncology

Phase I Trial of the PARP Inhibitor Olaparib and AKT Inhibitor Capivasertib in Patients with BRCA1/2- and Non-BRCA1/2-Mutant Cancers

Timothy A. Yap et al.

CANCER DISCOVERY (2020)

添加到收藏夹

Review Oncology

Encorafenib, Binimetinib, and Cetuximab in BRAF V600E-Mutated Colorectal Cancer

Giandomenico Roviello et al.

TRANSLATIONAL ONCOLOGY (2020)

添加到收藏夹

Article Oncology

Phase I/Ib Study of Tenalisib (RP6530), a Dual PI3K δ/γ Inhibitor in Patients with Relapsed/Refractory T-Cell Lymphoma

Auris Huen et al.

CANCERS (2020)

添加到收藏夹

Review Biochemistry & Molecular Biology

Targeting Casein Kinase 1 (CK1) in Hematological Cancers

Pavlina Janovska et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Checkpoint Kinase 1 Pharmacological Inhibition Synergizes with DNA-Damaging Agents and Overcomes Platinum Resistance in Basal-Like Breast Cancer

Cristina Nieto-Jimenez et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)

添加到收藏夹

Article Multidisciplinary Sciences

Pharmacological inhibition of hematopoietic progenitor kinase 1 positively regulates T-cell function

Yun Wang et al.

PLOS ONE (2020)

添加到收藏夹

Review Cell Biology

Pathological Functions of LRRK2 in Parkinson's Disease

Ga Ram Jeong et al.

CELLS (2020)

添加到收藏夹

Review Chemistry, Medicinal

Systemic review on B-RafV600E mutation as potential therapeutic target for the treatment of cancer

Jaydeepsinh Chavda et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

添加到收藏夹

Article Pharmacology & Pharmacy

An update on ripasudil for the treatment of glaucoma and ocular hypertension

V Testa et al.

DRUGS OF TODAY (2020)

添加到收藏夹

Article Physiology

Soluble guanylate cyclase stimulator praliciguat attenuates inflammation, fibrosis, and end-organ damage in the Dahl model of cardiorenal failure

Courtney M. Shea et al.

AMERICAN JOURNAL OF PHYSIOLOGY-RENAL PHYSIOLOGY (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Structural and strategic landscape of PIKK protein family and their inhibitors: an overview

Deekshi Angira et al.

FRONTIERS IN BIOSCIENCE-LANDMARK (2020)

添加到收藏夹

Article Biochemistry & Molecular Biology

Evolution of PIKK family kinase inhibitors: A new age cancer therapeutics

Althaf Shaik et al.

FRONTIERS IN BIOSCIENCE-LANDMARK (2020)

添加到收藏夹

Article Medicine, Research & Experimental

Ras-Mediated Activation of the Raf Family K nases

Elizabeth M. Terrell et al.

COLD SPRING HARBOR PERSPECTIVES IN MEDICINE (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

Dual-specificity MAP kinase phosphatases in health and disease

Ole-Morten Seternes et al.

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH (2019)

添加到收藏夹

Article Oncology

AS602801 Sensitizes Ovarian Cancer Stem Cells to Paclitaxel by Down-regulating MDR1

Masahiro Yamamoto et al.

ANTICANCER RESEARCH (2019)

添加到收藏夹

Review Pharmacology & Pharmacy

An Update on the Association of Protein Kinases with Cardiovascular Diseases

Fakhra Amin et al.

CURRENT PHARMACEUTICAL DESIGN (2019)

添加到收藏夹

Review Cardiac & Cardiovascular Systems

CaMKII signaling in heart diseases: Emerging role in diabetic cardiomyopathy

Bence Hegyi et al.

JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY (2019)

添加到收藏夹

Review Chemistry, Medicinal

Targeting ROCK/LIMK/cofilin signaling pathway in cancer

Mee-Hyun Lee et al.

ARCHIVES OF PHARMACAL RESEARCH (2019)

添加到收藏夹

Article Medicine, General & Internal

Alpelisib for PIK3CA-Mutated, Hormone Receptor-Positive Advanced Breast Cancer

Fabrice Andre et al.

NEW ENGLAND JOURNAL OF MEDICINE (2019)

添加到收藏夹

Review Pharmacology & Pharmacy

Targeting ERK1/2 protein-serine/threonine kinases in human cancers

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2019)

添加到收藏夹

Article Endocrinology & Metabolism

Distinct Effects of Carrageenan and High-Fat Consumption on the Mechanisms of Insulin Resistance in Nonobese and Obese Models of Type 2 Diabetes

Sumit Bhattacharyya et al.

JOURNAL OF DIABETES RESEARCH (2019)

添加到收藏夹

Article Oncology

Huzhangoside A Suppresses Tumor Growth through Inhibition of Pyruvate Dehydrogenase Kinase Activity

Choong-Hwan Kwak et al.

CANCERS (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

Downregulation of A2AR by siRNA loaded PEG-chitosan-lactate nanoparticles restores the T cell mediated anti-tumor responses through blockage of PKA/CREB signaling pathway

Ali Masjedi et al.

INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES (2019)

添加到收藏夹

Article Medicine, Research & Experimental

Sotrastaurin attenuates the stemness of gastric cancer cells by targeting PKCδ

Yuan Yuan et al.

BIOMEDICINE & PHARMACOTHERAPY (2019)

添加到收藏夹

Article Oncology

Phase I trial of pimasertib monotherapy in Japanese patients with solid tumors and those with hepatocellular carcinoma

K. Yamazaki et al.

CANCER CHEMOTHERAPY AND PHARMACOLOGY (2019)

添加到收藏夹

Article Oncology

Small molecule inhibitor agerafenib effectively suppresses neuroblastoma tumor growth in mouse models via inhibiting ERK MAPK signaling

Hui Li et al.

CANCER LETTERS (2019)

添加到收藏夹

Article Cell Biology

IGFs Potentiate TAC3-induced SLα Expression via Upregulation of TACR3 Expression in Grass Carp Pituitary Cells

Guangfu Hu et al.

CELLS (2019)

添加到收藏夹

Article Respiratory System

Phase II Study of Single/Repeated Doses of Acumapimod (BCT197) to Treat Acute Exacerbations of COPD

Irina R. Strambu et al.

COPD-JOURNAL OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (2019)

添加到收藏夹

Article Chemistry, Medicinal

INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ)

Eddy W. Yue et al.

ACS MEDICINAL CHEMISTRY LETTERS (2019)

添加到收藏夹

Review Pharmacology & Pharmacy

Ribociclib in HR+/HER2-Advanced or Metastatic Breast Cancer Patients

Kaitlin Rascon et al.

ANNALS OF PHARMACOTHERAPY (2019)

添加到收藏夹

Review Cell Biology

MAP4K Family Kinases and DUSP Family Phosphatases in T-Cell Signaling and Systemic Lupus Erythematosus

Huai-Chia Chuang et al.

CELLS (2019)

添加到收藏夹

Article Oncology

Cobimetinib in malignant melanoma: how to MEK an impact on long-term survival

Alice Indini et al.

FUTURE ONCOLOGY (2019)

添加到收藏夹

Article Cell Biology

Vascular endothelial growth factor-C promotes human mesenchymal stem cell migration via an ERK-and FAK-dependent mechanism

Masakazu Ishii et al.

MOLECULAR AND CELLULAR BIOCHEMISTRY (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

iEKPD 2.0: an update with rich annotations for eukaryotic protein kinases, protein phosphatases and proteins containing phosphoprotein-binding domains

Yaping Guo et al.

NUCLEIC ACIDS RESEARCH (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

B-Raf deficiency impairs tumor initiation and progression in a murine breast cancer model

Martin Koehler et al.

ONCOGENE (2019)

添加到收藏夹

Review Cell Biology

MAP4K3/GLK in autoimmune disease, cancer and aging

Huai-Chia Chuang et al.

JOURNAL OF BIOMEDICAL SCIENCE (2019)

添加到收藏夹

Article Pharmacology & Pharmacy

Characterizing the Sources of Pharmacokinetic Variability for TAK-117 (Serabelisib), an Investigational Phosphoinositide 3-Kinase Alpha Inhibitor: A Clinical Biopharmaceutics Study to Inform Development Strategy

Chirag G. Patel et al.

CLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT (2019)

添加到收藏夹

Article Multidisciplinary Sciences

Effect of CHK1 Inhibition on CPX-351 Cytotoxicity in vitro and ex vivo

Nicole D. Vincelette et al.

SCIENTIFIC REPORTS (2019)

添加到收藏夹

Review Cell Biology

PIKKing a way to regulate inflammation

Hazel Quek et al.

IMMUNOLOGY AND CELL BIOLOGY (2018)

添加到收藏夹

Article Oncology

Clinical pharmacodynamic/exposure characterisation of the multikinase inhibitor ilorasertib (ABT-348) in a phase 1 dose-escalation trial

Michael L. Maitland et al.

BRITISH JOURNAL OF CANCER (2018)

添加到收藏夹

News Item Oncology

Refametinib in RAS-mutated hepatocellular cancer

Manjulika Das

LANCET ONCOLOGY (2018)

添加到收藏夹

Article Oncology

Elongation factor-2 kinase (eEF-2K) expression is associated with poor patient survival and promotes proliferation, invasion and tumor growth of lung cancer

Haci Ahmet Bircan et al.

LUNG CANCER (2018)

添加到收藏夹

Article Neurosciences

Dysregulated phosphorylation of Rab GTPases by LRRK2 induces neurodegeneration

Ga Ram Jeong et al.

MOLECULAR NEURODEGENERATION (2018)

添加到收藏夹

Review Oncology

Protein kinase C (PKC) isoforms in cancer, tumor promotion and tumor suppression

Noah Isakov

SEMINARS IN CANCER BIOLOGY (2018)

添加到收藏夹

Review Oncology

AGC kinases, mechanisms of regulation and innovative drug development

Alejandro E. Leroux et al.

SEMINARS IN CANCER BIOLOGY (2018)

添加到收藏夹

Article Cell Biology

Crosstalk between PKCα and PI3K/AKT Signaling Is Tumor Suppressive in the Endometrium

Alice H. Hsu et al.

CELL REPORTS (2018)

添加到收藏夹

Article Dermatology

Targeting Tropomyosin Receptor Kinase in Cutaneous CYLD Defective Tumors With Pegcantratinib The TRAC Randomized Clinical Trial

Marina Danilenko et al.

JAMA DERMATOLOGY (2018)

添加到收藏夹

Article Oncology

AS602801, an Anti-Cancer Stem Cell Drug Candidate, Suppresses Gap-junction Communication Between Lung Cancer Stem Cells and Astrocytes

Kenta Kuramoto et al.

ANTICANCER RESEARCH (2018)

添加到收藏夹

Review Pharmacology & Pharmacy

Targeting oncogenic Raf protein-serine/threonine kinases in human cancers

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2018)

添加到收藏夹

Article Cell Biology

AMPK-dependent and independent actions of P2X7 in regulation of mitochondrial and lysosomal functions in microglia

Ponarulselvam Sekar et al.

CELL COMMUNICATION AND SIGNALING (2018)

添加到收藏夹

Article Multidisciplinary Sciences

Miransertib (ARQ 092), an orally-available, selective Akt inhibitor is effective against Leishmania

Devki Nandan et al.

PLOS ONE (2018)

添加到收藏夹

Review Oncology

Targeting B cell receptor signalling in cancer: preclinical and clinical advances

Jan A. Burger et al.

NATURE REVIEWS CANCER (2018)

添加到收藏夹

Article Hematology

ARQ 092, an orally-available, selective AKT inhibitor, attenuates neutrophil-platelet interactions in sickle cell disease

Kyungho Kim et al.

HAEMATOLOGICA (2017)

添加到收藏夹

Article Hematology

ARQ 092, an orally-available, selective AKT inhibitor, attenuates neutrophil-platelet interactions in sickle cell disease

Kyungho Kim et al.

HAEMATOLOGICA (2017)

添加到收藏夹

Article Chemistry, Medicinal

The Discovery of a Dual TTK Protein Kinase/CDC2-Like Kinase (CLK2) Inhibitor for the Treatment of Triple Negative Breast Cancer Initiated from a Phenotypic Screen

Jennifer R. Riggs et al.

JOURNAL OF MEDICINAL CHEMISTRY (2017)

添加到收藏夹

Review Oncology

LIM kinases: cofilin and beyond

Chloe Prunier et al.

ONCOTARGET (2017)

添加到收藏夹

Article Biology

Systematic proteomic analysis of LRRK2-mediated Rab GTPase phosphorylation establishes a connection to ciliogenesis

Martin Steger et al.

ELIFE (2017)

添加到收藏夹

Review Neurosciences

The effects of Chinese medicines on cAMP/PKA signaling in central nervous system dysfunction

Lin Li et al.

BRAIN RESEARCH BULLETIN (2017)

添加到收藏夹

Article Cardiac & Cardiovascular Systems

Toll-like receptor 2 dominance over Toll-like receptor 4 in stressful conditions for its detrimental role in the heart

Ashim K. Bagchi et al.

AMERICAN JOURNAL OF PHYSIOLOGY-HEART AND CIRCULATORY PHYSIOLOGY (2017)

添加到收藏夹

Article Oncology

Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia

Lohith Bachegowda et al.

CANCER RESEARCH (2016)

添加到收藏夹

Review Cell Biology

Overview of CDK9 as a target in cancer research

Fatima Morales et al.

CELL CYCLE (2016)

添加到收藏夹

Article Chemistry, Medicinal

Further investigation of Paprotrain: Towards the conception of selective and multi-targeted CNS kinase inhibitors

Christophe Labriere et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2016)

添加到收藏夹

Article Biochemistry & Molecular Biology

Cerebellar Ataxia and Coenzyme Q Deficiency through Loss of Unorthodox Kinase Activity

Jonathan A. Stefely et al.

MOLECULAR CELL (2016)

添加到收藏夹

Article Critical Care Medicine

A Randomized Dose-Escalation Study of the Safety and Anti-Inflammatory Activity of the p38 Mitogen-Activated Protein Kinase Inhibitor Dilmapimod in Severe Trauma Subjects at Risk for Acute Respiratory Distress Syndrome

Jason D. Christie et al.

CRITICAL CARE MEDICINE (2015)

添加到收藏夹

Review Oncology

Clinical activity of alvocidib (flavopiridol) in acute myeloid leukemia

Joshua F. Zeidner et al.

LEUKEMIA RESEARCH (2015)

添加到收藏夹

Review Pharmacology & Pharmacy

Glycogen synthase kinase-3 (GSK3): Regulation, actions, and diseases

Eleonore Beurel et al.

PHARMACOLOGY & THERAPEUTICS (2015)

添加到收藏夹

Article Oncology

LIM kinase inhibitors disrupt mitotic microtubule organization and impair tumor cell proliferation

Katerina Mardilovich et al.

ONCOTARGET (2015)

添加到收藏夹

Article Biochemistry & Molecular Biology

Involvement of the Na+/Ca2+ exchanger isoform 1 (NCX1) in Neuronal Growth Factor (NGF)-induced Neuronal Differentiation through Ca2+-dependent Akt Phosphorylation

Agnese Secondo et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2015)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of N-((4-([1,2,4]Triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): A Highly Potent, Selective, and Orally Bioavailable Inhibitor of TGF-β Type I Receptor Kinase as Cancer Immunotherapeutic/Antifibrotic Agent

Cheng Hua Jin et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

添加到收藏夹

Article Pharmacology & Pharmacy

Activator or inhibitor? GSK-3 as a new drug target

Fumi Takahashi-Yanaga

BIOCHEMICAL PHARMACOLOGY (2013)

添加到收藏夹

Article Biochemistry & Molecular Biology

Dynamic Ubiquitination of the Mitogen-activated Protein Kinase Kinase (MAPKK) Ste7 Determines Mitogen-activated Protein Kinase (MAPK) Specificity

Jillian H. Hurst et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2013)

添加到收藏夹

Article Cardiac & Cardiovascular Systems

Guanylyl cyclase (GC)-A and GC-B activities in ventricles and cardiomyocytes from failed and non-failed human hearts: GC-A is inactive in the failed cardiomyocyte

Deborah M. Dickey et al.

JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY (2012)

添加到收藏夹

Review Cell Biology

Integrated regulation of PIKK-mediated stress responses by AAA plus proteins RUVBL1 and RUVBL2

Natsuko Izumi et al.

NUCLEUS (2012)

添加到收藏夹

Review Microbiology

Activation and Function of the MAPKs and Their Substrates, the MAPK-Activated Protein Kinases

Marie Cargnello et al.

MICROBIOLOGY AND MOLECULAR BIOLOGY REVIEWS (2011)

添加到收藏夹

Review Biochemistry & Molecular Biology

The alpha-kinase family: an exceptional branch on the protein kinase tree

Jeroen Middelbeek et al.

CELLULAR AND MOLECULAR LIFE SCIENCES (2010)

添加到收藏夹

Review Cell Biology

Tel2: a common partner of PIK-related kinases and a link between DNA checkpoint and nutritional response?

Junko Kanoh et al.

GENES TO CELLS (2007)

添加到收藏夹

Review Biochemistry & Molecular Biology

The MEK/ERK cascade: From signaling specificity to diverse functions

Yoav D. Shaul et al.

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH (2007)

添加到收藏夹

Review Biochemistry & Molecular Biology

Differential regulation and properties of MAPKs

M. Raman et al.

ONCOGENE (2007)

添加到收藏夹

Review Biochemistry & Molecular Biology

Differential regulation of MAP kinase signalling by dual-specificity protein phosphatases

D. M. Owens et al.

ONCOGENE (2007)

添加到收藏夹

Review Biochemistry & Molecular Biology

A family portrait of the RIO kinases

N LaRonde-LeBlanc et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2005)

添加到收藏夹

Review Biochemistry & Molecular Biology

Alpha-kinases: analysis of the family and comparison with conventional protein kinases

D Drennan et al.

PROGRESS IN BIOPHYSICS & MOLECULAR BIOLOGY (2004)

添加到收藏夹

Article Biochemistry & Molecular Biology

Characterization of OSR1, a member of the mammalian Ste20p/germinal center kinase subfamily

W Chen et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2004)

添加到收藏夹

Article Biochemistry & Molecular Biology

DNA-dependent protein kinase (DNA-PK) phosphorylates nuclear DNA helicase II/RNA helicase A and hnRNP proteins in an RNA-dependent manner

SS Zhang et al.

NUCLEIC ACIDS RESEARCH (2004)

添加到收藏夹

Article Biochemistry & Molecular Biology

Embryonic lethality and fetal liver apoptosis in mice lacking the c-raf-1 gene

M Mikula et al.

EMBO JOURNAL (2001)

添加到收藏夹

© Peeref 2019-2024. All rights reserved.