☆ 4.6 Review

Inhibitors of phosphoinositide 3-kinase (PI3K) and phosphoinositide 3-kinase-related protein kinase family (PIKK)

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2023)

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 Biotechnology & Applied Microbiology

Targeting replication stress in cancer therapy

Alexandre Andre B. A. da Costa et al.

Summary: Replication stress is a major cause of genomic instability and a vulnerability of cancer cells. Inhibiting kinases such as ATR, CHK1, WEE1, and MYT1 can target this vulnerability. In addition, inhibiting the DNA damage response can elicit an immune response. Therefore, several inhibitors are being evaluated in clinical trials to overcome therapeutic resistance and promote antitumor immunity by targeting replication stress.

NATURE REVIEWS DRUG DISCOVERY (2023)

添加到收藏夹

Article Oncology

Combining radiation and the ATR inhibitor berzosertib activates STING signaling and enhances immunotherapy via inhibiting SHP1 function in colorectal cancer

Chaofan Liu et al.

Summary: This study investigated the efficacy of combining ATR inhibitors (ATRi), irradiation (IR), and anti-PD-L1 antibodies in colorectal cancer (CRC) mouse models. The results showed that combining ATRi and IR enhanced CD8(+)T cell infiltration and improved the effectiveness of anti-PD-L1 therapy. The mechanism study revealed that IR + ATRi activated the STING signaling pathway and promoted innate immune activation, thereby facilitating immunotherapy.

CANCER COMMUNICATIONS (2023)

添加到收藏夹

Article Oncology

Phase II study of ceralasertib (AZD6738) in combination with durvalumab in patients with advanced/metastatic melanoma who have failed prior anti-PD-1 therapy

R. Kim et al.

Summary: Ceralasertib in combination with durvalumab has promising antitumor activity among patients with metastatic melanoma who have failed anti-programmed cell death protein 1 therapy, and shows stable and sustained disease control rate.

ANNALS OF ONCOLOGY (2022)

添加到收藏夹

Article Oncology

Sapanisertib plus Fulvestrant in Postmenopausal Women with Estrogen Receptor-Positive/HER2-Negative Advanced Breast Cancer after Progression on Aromatase Inhibitor

Jose A. Garcia-Saenz et al.

Summary: This phase II study examined the efficacy and toxicity of daily or weekly combination treatment of sapanisertib with fulvestrant in postmenopausal women with estrogen receptor-positive/HER2-negative advanced or metastatic breast cancer. The study found that the combination treatment resulted in a numerically longer progression-free survival compared to single-agent fulvestrant, but was associated with increased toxicity.

CLINICAL CANCER RESEARCH (2022)

添加到收藏夹

Article Oncology

Phase 1b Clinical Trial with Alpelisib plus Olaparib for Patients with Advanced Triple-Negative Breast Cancer

Felipe Batalini et al.

Summary: This study aimed to evaluate the safety and recommended dose of olaparib in combination with alpelisib in patients with breast cancer, and explore its effects on different subtypes. The results showed that this combination therapy was tolerable for pre-treated TNBC patients and demonstrated activity in non-BRCA mutant patients. Analysis of circulating-free DNA also provided important prognostic information.

CLINICAL CANCER RESEARCH (2022)

添加到收藏夹

Article Chemistry, Medicinal

Recent advances in DDR (DNA damage response) inhibitors for cancer therapy

Binbin Cheng et al.

Summary: DDR defects in cells drive tumor formation and provide targets for cancer-specific vulnerabilities. PARP inhibitors have shown success in utilizing synthetic lethality-based therapy to treat DNA-repairing deficiency cancers. Many DDR kinase inhibitors have been discovered and show promising results for cancer therapy.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Oncology

RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors

Anne Roulston et al.

Summary: RP-3500 is a novel ATR kinase inhibitor with high selectivity and efficacy in protecting genome integrity and potential anti-tumor activity in xenograft models. The use of intermittent dosing schedules maximizes tumor growth inhibition and demonstrates the reversible nature of erythroid toxicity.

MOLECULAR CANCER THERAPEUTICS (2022)

添加到收藏夹

Article Oncology

Antitumor activity of the dual PI3K/mTOR inhibitor gedatolisib and the involvement of ABCB1 in gedatolisib resistance in canine tumor cells

Yusuke Murase et al.

Summary: This study investigated the antitumor activity and resistance mechanisms of the dual PI3K/mTOR inhibitor, gedatolisib, in canine tumor cell lines. The results demonstrated the antitumor activity of gedatolisib in all cell lines, with certain cell lines exhibiting resistance. ABCB1 was found to play an important role in gedatolisib resistance, while SGK1 and PIK3CA mutations were not associated with resistance.

ONCOLOGY REPORTS (2022)

添加到收藏夹

Article Oncology

A Phase 1 Study of Sapanisertib (TAK-228) in East Asian Patients with Advanced Nonhematological Malignancies

Toshio Shimizu et al.

Summary: Sapanisertib, a highly selective inhibitor of mammalian target of rapamycin complexes 1 and 2, was found to have moderate anti-tumor effects in East Asian patients with nonhematologic malignancies. The recommended phase 2 dose of Sapanisertib in this population was 3 mg once daily, with similar pharmacokinetics and safety profiles compared to Western patients.

TARGETED ONCOLOGY (2022)

添加到收藏夹

Article Cell Biology

ATRX loss in glioma results in dysregulation of cell-cycle phase transition and ATM inhibitor radio-sensitization

Tingtin Qin et al.

Summary: ATRX deficiency leads to dysregulation of cell-cycle phase transitions in high-grade glioma cells, resulting in increased sensitivity to irradiation. The study found that ATRX binds to the regulatory elements of cell-cycle phase transition genes and loss of ATRX leads to decreased expression of Checkpoint Kinase 1, leading to early release of G2/M entry after irradiation.

CELL REPORTS (2022)

添加到收藏夹

Article Oncology

The emerging role of capivasertib in breast cancer

Angeliki Andrikopoulou et al.

Summary: Over 50% of breast tumors have genetic alterations in the PI3K pathway, with PIK3CA mutations being the most common. Capivasertib, a novel AKT inhibitor, has shown efficacy in breast cancer cell lines and in combination with paclitaxel and fulvestrant. Ongoing Phase III trials will provide further insights into the therapeutic role of capivasertib in breast cancer.

BREAST (2022)

添加到收藏夹

Review Oncology

New Treatment Options for Newly-Diagnosed and Relapsed Chronic Lymphocytic Leukemia

Elzbieta Iskierka-Jazdzewska et al.

Summary: The better understanding of CLL biology has led to the development of targeted drugs, such as BTK inhibitors, PI3K inhibitors, venetoclax, and CD20 monoclonal antibodies, which have improved the prognosis for CLL patients. These drugs show excellent efficacy and acceptable safety profiles, and can be used alone or in combination for a limited time. New reversible BTK inhibitors and promising cellular therapies offer further options for CLL treatment.

CURRENT TREATMENT OPTIONS IN ONCOLOGY (2022)

添加到收藏夹

Review Chemistry, Medicinal

Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015-2021)

Patrik Oleksak et al.

Summary: Mechanistic target of rapamycin (mTOR) is a protein kinase that regulates cell functions. Dysregulation of mTOR activity is associated with various pathological conditions. Inhibition of overactivated mTOR is a rational approach for treating human diseases. Rapamycin is a natural inhibitor of mTOR with antitumor and immunosuppressive activity. Different generations of mTOR inhibitors have been developed, including rapalogs, mTOR kinase inhibitors, and dual PI3K/mTOR inhibitors. Novel inhibitors are still being developed to better understand the role of mTOR in signaling pathways and human diseases.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Oncology

A phase III trial of alpelisib plus trastuzumab ± fulvestrant versus trastuzumab plus chemotherapy in HER2+PIK3CA-mutated breast cancer

Jose Alejandro Perez-Fidalgo et al.

Summary: ALPHABET is a phase III clinical trial that investigates the potential use of alpelisib in the treatment of certain subtypes of breast cancer. The trial aims to evaluate whether the combination of alpelisib and trastuzumab, with or without fulvestrant, is effective in treating previously treated HER2-positive PIK3CA-mutated advanced breast cancer. The study will compare this combination treatment with standard chemotherapy and trastuzumab. The primary outcome measure is investigator-assessed progression-free survival. The trial also includes additional analyses on side effects and quality of life.

FUTURE ONCOLOGY (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 Oncology

Safety and Efficacy of the mTOR Inhibitor, Vistusertib, Combined With Anastrozole in Patients With Hormone Receptor-Positive Recurrent or Metastatic Endometrial Cancer The VICTORIA Multicenter, Open-label, Phase 1/2 Randomized Clinical Trial

Pierre Heudel et al.

Summary: This study aimed to evaluate the safety and efficacy of vistusertib in combination with anastrozole for hormone receptor-positive recurrent or metastatic endometrial cancer. The results showed that the combination therapy significantly improved the 8-week progression-free rate, overall response rate, and progression-free survival, while maintaining manageable adverse events.

JAMA ONCOLOGY (2022)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα

Emily J. Hanan et al.

Summary: This study optimized a series of benzoxazepin-oxazolidinone ATP-competitive inhibitors of PI3K alpha that also induce selective degradation of the mutant p110 alpha protein. Structure-based design led to potent inhibitors with over 300-fold selectivity and further optimization of pharmacokinetic properties resulted in excellent in vivo efficacy. Clinical candidate GDC-0077 (inavolisib) is now being evaluated in a Phase III clinical trial for treating patients with PIK3CA-mutant breast cancer.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of Clinical Candidate NTQ1062 as a Potent and Bioavailable Akt Inhibitor for the Treatment of Human Tumors

Changyou Ma et al.

Summary: Akt plays critical roles in tumor cells, making it an exciting target in oncology. NTQ1062, a novel Akt inhibitor with excellent drug-like properties and potent antitumor activity, is currently undergoing clinical evaluation.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

添加到收藏夹

Article Oncology

Fulvestrant plus capivasertib versus placebo after relapse or progression on an aromatase inhibitor in metastatic, oestrogen receptor-positive, HER2-negative breast cancer (FAKTION): overall survival, updated progression-free survival, and expanded biomarker analysis from a randomised, phase 2 trial

Sacha J. Howell et al.

Summary: This study demonstrates that the addition of Capivasertib to fulvestrant improves progression-free survival and overall survival in women with aromatase inhibitor-resistant advanced breast cancer. The expanded genetic testing panel suggests that Capivasertib predominantly benefits patients with alterations in the PI3K/AKT/PTEN pathway.

LANCET ONCOLOGY (2022)

添加到收藏夹

Article Biochemistry & Molecular Biology

THO complex deficiency impairs DNA double-strand break repair via the RNA surveillance kinase SMG-1

Juliette A. Kamp et al.

Summary: This study uncovers the crosstalk between RNA surveillance and DNA repair in living animals, revealing the role of SMG-1 in this process through genetic screens and genome-wide analyses. The findings shed light on how defects in RNA processing can affect DNA repair, and highlight the importance of SMG-1 in regulating this interaction.

NUCLEIC ACIDS RESEARCH (2022)

添加到收藏夹

Article Dentistry, Oral Surgery & Medicine

Simultaneously targeting ErbB family kinases and PI3K in HPV-positive head and neck squamous cell carcinoma

Zejia Yang et al.

ORAL ONCOLOGY (2022)

添加到收藏夹

Article Oncology

Phase II study of ceralasertib (AZD6738) in combination with durvalumab in patients with advanced gastric cancer

Minsuk Kwon et al.

Summary: The combination of Ceralasertib and durvalumab has shown promising clinical activity and tolerability in patients with advanced gastric cancer (AGC). Certain patients showed better clinical responses, which were associated with loss of ATM expression and homologous repair deficiency.

JOURNAL FOR IMMUNOTHERAPY OF CANCER (2022)

添加到收藏夹

Meeting Abstract Oncology

Gene expression profiles in endocrine-resistant breast cancer

C. Schagerholm et al.

ANNALS OF ONCOLOGY (2022)

添加到收藏夹

Article Multidisciplinary Sciences

Identification and development of a subtype-selective allosteric AKT inhibitor suitable for clinical development

Natalie Page et al.

Summary: The protein kinase AKT plays a crucial role in regulating cellular functions. ALM301, a novel allosteric inhibitor of AKT1/2, has been developed with high selectivity and potent inhibition of cellular proliferation. It effectively inhibits the pAKT signaling pathway and significantly reduces tumor growth in a dose-dependent manner in an MCF-7 xenograft model.

SCIENTIFIC REPORTS (2022)

添加到收藏夹

Article Oncology

Targeting DNA damage response components induces enhanced STING-dependent type-I IFN response in ATM deficient cancer cells and drives dendritic cell activation

Marta Lopez-Pelaez et al.

Summary: This study demonstrates that targeting compensatory DNA repair pathways enhances the sensitivity of tumor cells to ATR inhibitor and DNA crosslinker, and activates dendritic cells (DCs) to increase tumor cell immunogenicity through the innate immune system activation. This provides a potential strategy to combat tumors.

ONCOIMMUNOLOGY (2022)

添加到收藏夹

Review Oncology

Targeting the DNA Damage Response and DNA Repair Pathways to Enhance Radiosensitivity in Colorectal Cancer

Siyao Deng et al.

Summary: This review focuses on the role of DNA damage response and repair pathways in radiotherapy, and the potential for enhancing the sensitivity of colorectal cancer to radiotherapy by targeting cell-cycle checkpoint proteins.

CANCERS (2022)

添加到收藏夹

Article Oncology

Combined inhibition of EZH2 and ATM is synthetic lethal in BRCA1-deficient breast cancer

Leonie Ratz et al.

Summary: This study identified the combined inhibition of EZH2 and ATM as a novel synthetic lethality-based therapy for the treatment of BRCA1-mutant breast cancer.

BREAST CANCER RESEARCH (2022)

添加到收藏夹

Review Biotechnology & Applied Microbiology

Rapamycin golden jubilee and still the miraculous drug: a potent immunosuppressant, antitumor, rejuvenative agent, and potential contributor in COVID-19 treatment

Mohamed A. Mohamed et al.

Summary: This article introduces the discovery, microbial producers, biological activities, chemical structure, production methods, and action mechanism of rapamycin. In addition, it discusses the application of rapamycin in the treatment of COVID-19, side effects and approaches to minimize them. Finally, the current status of rapamycin and its analogues in the global market and future prospects are reported.

BIORESOURCES AND BIOPROCESSING (2022)

添加到收藏夹

Review Pharmacology & Pharmacy

Recent Advances in Dual PI3K/mTOR Inhibitors for Tumour Treatment

Xianbo Wu et al.

Summary: Studies have shown that PI3K/mTOR inhibitors are effective in cancer treatment, as they can inhibit cell proliferation and promote apoptosis. These inhibitors exhibit high potency and low drug resistance, indicating they have great potential as anticancer drugs.

FRONTIERS IN PHARMACOLOGY (2022)

添加到收藏夹

Article Oncology

First-in-Human Trial of the Oral Ataxia Telangiectasia and RAD3-Related (ATR) Inhibitor BAY 1895344 in Patients with Advanced Solid Tumors

Timothy A. Yap et al.

Summary: The study demonstrated that oral ATR inhibitor BAY 1895344 is well tolerated and effective in treating patients with advanced solid tumors, with some patients achieving partial responses or stable disease, particularly in those with DDR defects such as ATM loss. Further investigation is warranted to explore its potential in this patient population.

CANCER DISCOVERY (2021)

添加到收藏夹

Article Oncology

A first-in-man phase 1 study of the DNA-dependent protein kinase inhibitor peposertib (formerly M3814) in patients with advanced solid tumours

Mark T. J. van Bussel et al.

Summary: This phase 1 trial aimed to determine the maximum-tolerated dose and recommended phase 2 dose of peposertib, a DNA-dependent protein kinase inhibitor, in patients with advanced solid tumors. Peposertib was well-tolerated and showed modest efficacy in unselected tumors, with the recommended dose declared as 400 mg twice daily. Further studies are ongoing with peposertib/chemo-radiation combinations.

BRITISH JOURNAL OF CANCER (2021)

添加到收藏夹

Meeting Abstract Hematology

Safety and Efficacy of Tenalisib Given in Combination with Romidepsin in Patients with Relapsed/Refractory T-Cell Lymphoma: Final Results from a Phase I/II Open Label Multi-Center Study

Swaminathan P. Iyer et al.

BLOOD (2021)

添加到收藏夹

Review Biochemistry & Molecular Biology

MRN complex is an essential effector of DNA damage repair

Shan Qiu et al.

Summary: This review focuses on the structure and function of the MRN complex in DNA damage repair, highlighting its important roles in DNA damage recognition, signaling, and HR or NHEJ repair processes.

JOURNAL OF ZHEJIANG UNIVERSITY-SCIENCE B (2021)

添加到收藏夹

Article Oncology

First-in-child phase I/II study of the dual mTORC1/2 inhibitor vistusertib (AZD2014) as monotherapy and in combination with topotecan-temozolomide in children with advanced malignancies: arms E and F of the AcSe-ESMART trial

Raphael J. Morscher et al.

Summary: The study aimed to investigate the use of the dual mTORC1/2 inhibitor vistusertib in relapsed/refractory pediatric patients and identified genetic alterations in the PI3K/AKT/mTOR pathway. Vistusertib was well tolerated in pediatric patients, but no significant tumor responses or prolonged stabilization were observed.

EUROPEAN JOURNAL OF CANCER (2021)

添加到收藏夹

Review Chemistry, Medicinal

Development and therapeutic potential of 2-aminothiazole derivatives in anticancer drug discovery

Seyedeh Roya Alizadeh et al.

Summary: The development of anticancer drug resistance hampers clinical efficacy, making research on small molecule antitumor agents more desirable. The 2-aminothiazole scaffold has emerged as a promising drug carrier, exhibiting potent inhibitory activity in various cancer cell lines.

MEDICINAL CHEMISTRY RESEARCH (2021)

添加到收藏夹

Article Oncology

Combination ATR and PARP Inhibitor (CAPRI): A phase 2 study of ceralasertib plus olaparib in patients with recurrent, platinum-resistant epithelial ovarian cancer

Payal D. Shah et al.

Summary: In platinum-resistant HGSOC patients, the combination therapy of olaparib plus ceralasertib was well-tolerated, with no objective responses observed. However, a signal of activity was seen particularly in diseases associated with BRCA1 mutations. Further evaluation should include alternate dosing strategies in genomically-selected populations.

GYNECOLOGIC ONCOLOGY (2021)

添加到收藏夹

Article Biochemistry & Molecular Biology

Novel Dual PI3K/mTOR Inhibitor, Apitolisib (GDC-0980), Inhibits Growth and Induces Apoptosis in Human Glioblastoma Cells

Wioleta Justyna Omeljaniuk et al.

Summary: The study found that GDC-0980 can effectively inhibit the survival of human GBM cells and induce apoptosis, independent of ER stress-mediated DR5 activation. It is suggested that GDC-0980 may block the inhibitory effect on protein synthesis through inhibiting PERK expression, leading to an intensification of translation and an increase in apoptosis. Additionally, CHOP stimulates protein synthesis and increases apoptosis.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

添加到收藏夹

Article Oncology

nab-Sirolimus for Patients With Malignant Perivascular Epithelioid Cell Tumors

Andrew J. Wagner et al.

Summary: The study evaluated the efficacy and safety of nab-sirolimus in patients with malignant PEComa, showing an overall response rate of 39% with rapid and durable responses. Patients with TSC2 mutations were more likely to achieve a positive response. nab-sirolimus was considered an important new treatment option for this disease based on response rate, disease control, and safety profile.

JOURNAL OF CLINICAL ONCOLOGY (2021)

添加到收藏夹

Article Oncology

Alpelisib plus fulvestrant for PIK3CA-mutated, hormone receptor-positive, human epidermal growth factor receptor-2enegative advanced breast cancer: final overall survival results from SOLAR-1

F. Andre et al.

Summary: The study confirmed a certain efficacy in overall survival when alpelisib was added to fulvestrant treatment in patients with PIK3CA-mutated hormone receptor-positive, human epidermal growth factor receptor-2-negative advanced breast cancer, prolonging the median survival time.

ANNALS OF ONCOLOGY (2021)

添加到收藏夹

Review Biochemistry & Molecular Biology

The Role of mTOR Signaling as a Therapeutic Target in Cancer

Nadezhda V. Popova et al.

Summary: This review summarizes the current information on the role of phosphatidylinositol-3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling in cancer as a potential target for new therapy options. The mTOR and PI3K/AKT/mTORC1 (mTOR complex 1) signaling pathways are critical for regulating fundamental cell processes, and their deregulation is implicated in cancer, metabolic dysregulation, and aging. The review also discusses recent data on the structure and function of the mTOR pathway, mechanisms of deregulation in human cancers, and the use of PI3K/AKT/mTOR inhibitors in clinical studies for cancer treatment, including issues of resistance and adverse effects.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

添加到收藏夹

Article Genetics & Heredity

Clinical experience with the AKT1 inhibitor miransertib in two children with PIK3CA-related overgrowth syndrome

Karina Forde et al.

Summary: This case series presents the use of miransertib in two pediatric patients with PROS, showing objective clinical response in one patient and improvement in key qualitative outcomes in another. Treatment was well tolerated with no significant toxicities reported, highlighting the potential therapeutic utility of miransertib in selected pediatric patients with severe PROS and demonstrating the possibility of repurposing targeted therapies for rare diseases. An open label, Phase 1/2 study of miransertib in children with PROS and PS is currently underway to more accurately assess its efficacy in treating PROS disorder.

ORPHANET JOURNAL OF RARE DISEASES (2021)

添加到收藏夹

Review Oncology

Copanlisib for the Treatment of Malignant Lymphoma: Clinical Experience and Future Perspectives

Javier Munoz et al.

Summary: Copanlisib, a highly selective PI3K inhibitor, has shown durable responses and manageable safety profile in heavily pre-treated patients with indolent lymphomas. Adverse events mainly include hyperglycemia, hypertension, and mild diarrhea, which are infusion-related and can be managed with standard therapies.

TARGETED ONCOLOGY (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 Oncology

ANETT: PhAse II trial of NEoadjuvant TAK-228 plus Tamoxifen in patients with hormone receptor-positive breast cancer

Emre Koca et al.

Summary: This trial demonstrated that the combination of tamoxifen and TAK-228 is a safe and well-tolerated neoadjuvant treatment for ER+ breast cancer, showing significant reduction in both Ki-67 and tumor size. Further evaluation in larger studies is warranted.

BREAST CANCER RESEARCH AND TREATMENT (2021)

添加到收藏夹

Article Oncology

Phase I Study of Ceralasertib (AZD6738), a Novel DNA Damage Repair Agent, in Combination with Weekly Paclitaxel in Refractory Cancer

Seung Tae Kim et al.

Summary: Ceralasertib in combination with paclitaxel showed tolerability and antitumor activity in patients with advanced malignancies, with durable responses observed in advanced melanoma patients resistant to anti-PD1/L1 treatment.

CLINICAL CANCER RESEARCH (2021)

添加到收藏夹

Article Pharmacology & Pharmacy

Umbralisib: First Approval

Sohita Dhillon et al.

Summary: Umbralisib, an oral inhibitor targeting PI3K delta and CK1 epsilon, has received its first approval in the USA for treating various haematological malignancies. Clinical studies are ongoing in multiple countries, marking an important milestone in its development.

DRUGS (2021)

添加到收藏夹

Review Chemistry, Medicinal

Phosphatidylinositol 3-kinase (PI3K) inhibitors: a recent update on inhibitor design and clinical trials (2016-2020)

Dima A. Sabbah et al.

Summary: The PI3K/AKT/mTOR signaling pathway is crucial in regulating cell growth and proliferation, making it an effective target for cancer treatment. The development of selective and mutant-specific PI3K inhibitors, as well as combination therapy with existing anticancer drugs, is important for improving efficacy and reducing toxicity in cancer treatment. Future research directions include subtype-selective PI3K inhibitors and strategies to overcome drug resistance.

EXPERT OPINION ON THERAPEUTIC PATENTS (2021)

添加到收藏夹

Review Biochemistry & Molecular Biology

PI3K Inhibitors in Cancer: Clinical Implications and Adverse Effects

Rosalin Mishra et al.

Summary: The PI3K pathway is crucial in cancer development and is a promising therapeutic target. Clinical trials are ongoing to evaluate the efficacy and potential risks associated with PI3K inhibitors in overcoming resistance to current therapies.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

添加到收藏夹

Review Biochemistry & Molecular Biology

The Multifaceted Roles of Ku70/80

Sayma Zahid et al.

Summary: DNA double-strand breaks are accidental lesions caused by various stresses and genetically programmed events. Most DSBs are repaired in mammalian cells through the classical nonhomologous end-joining pathway, with Ku playing a central role. In addition to its DNA repair function, Ku is involved in various other DNA metabolism processes.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

添加到收藏夹

Article Oncology

Phase 2 study of TAS-117, an allosteric akt inhibitor in advanced solid tumors harboring phosphatidylinositol 3-kinase/v-akt murine thymoma viral oncogene homolog gene mutations

Jii Bum Lee et al.

Summary: TAS-117, a potent and selective allosteric pan-v-akt inhibitor, showed limited antitumor activity and manageable toxicity in heavily treated cancer patients. Clinical efficacy was observed in patients with ovarian cancer harboring PIK3CA E545K mutations and in patients with breast cancer harboring PIK3CA H1047R and Akt1(E17K) mutations.

INVESTIGATIONAL NEW DRUGS (2021)

添加到收藏夹

Review Oncology

PI3Kδ Inhibitors as Immunomodulatory Agents for the Treatment of Lymphoma Patients

Chiara Tarantelli et al.

Summary: PI3K inhibitors not only directly affect cancer cells, but can also modulate immune responses, particularly focusing on the impact on T cells in the tumor microenvironment.

CANCERS (2021)

添加到收藏夹

Article Oncology

Copanlisib plus rituximab versus placebo plus rituximab in patients with relapsed indolent non-Hodgkin lymphoma (CHRONOS-3): a double-blind, randomised, placebo-controlled, phase 3 trial

Matthew J. Matasar et al.

Summary: Copanlisib plus rituximab significantly improved progression-free survival in patients with relapsed indolent non-Hodgkin lymphoma compared with placebo plus rituximab, with the most common grade 3-4 adverse events being hyperglycemia and hypertension.

LANCET ONCOLOGY (2021)

添加到收藏夹

Review Pharmacology & Pharmacy

Activation of PI3K/AKT/mTOR Pathway Causes Drug Resistance in Breast Cancer

Chao Dong et al.

Summary: Hyperactivation of the PI3K/AKT/mTOR pathway is associated with drug resistance and cancer progression in breast cancer patients. Current research is focusing on developing drugs targeting this pathway to overcome acquired resistance to standard therapies.

FRONTIERS IN PHARMACOLOGY (2021)

添加到收藏夹

Meeting Abstract Oncology

Ph I/II study of PI3K-b inhibitor GSK2636771 (G771) in combination with pembrolizumab (P) in patients (pts) with PTEN loss and melanoma or other advanced solid tumors

E. Burton et al.

ANNALS OF ONCOLOGY (2021)

添加到收藏夹

Article Oncology

Ceralasertib (AZD6738), an Oral ATR Kinase Inhibitor, in Combination with Carboplatin in Patients with Advanced Solid Tumors: A Phase I Study

Timothy A. Yap et al.

Summary: This study focused on the safety, tolerability, and preliminary antitumor activity of ceralasertib combined with carboplatin in patients with advanced solid tumors. The recommended phase II dose was determined to be ceralasertib 40 mg once daily on days 1-2 with carboplatin AUC5 every 3 weeks, showing potential for antitumor activity. Pharmacokinetic and pharmacodynamic studies confirmed the modulation of pharmacodynamic effects.

CLINICAL CANCER RESEARCH (2021)

添加到收藏夹

Article Oncology

Phase I Dose-Escalation Study of the Dual PI3K-mTORC1/2 Inhibitor Gedatolisib in Combination with Paclitaxel and Carboplatin in Patients with Advanced Solid Tumors

Ilaria Colombo et al.

Summary: This phase I study evaluated the safety, tolerability, pharmacokinetics, and preliminary activity of the PI3K/mTORC1/2 dual inhibitor gedatolisib combined with carboplatin and paclitaxel. The recommended phase II dose is gedatolisib 110 mg on days 1, 8, 15, and 22 alongside carboplatin and paclitaxel. The combination treatment showed tolerable profile and promising efficacy, particularly in clear cell ovarian cancer.

CLINICAL CANCER RESEARCH (2021)

添加到收藏夹

Article Oncology

A Phase I, Open-Label, Dose-Finding Study of GSK2636771, a PI3K beta Inhibitor, Administered with Enzalutamide in Patients with Metastatic Castration-Resistant Prostate Cancer

Debashis Sarker et al.

Summary: The study investigated the combination of enzalutamide and the PI3K beta inhibitor GSK2636771 in patients with PTEN-deficient mCRPC. Results demonstrated acceptable safety and tolerability of the drug combination, but limited antitumor activity was observed.

CLINICAL CANCER RESEARCH (2021)

添加到收藏夹

Article Oncology

Feasibility of Combining the Phosphatidylinositol 3-Kinase Inhibitor Copanlisib With Rituximab-Based Immunochemotherapy in Patients With Relapsed Indolent B-cell Lymphoma

Matthew J. Matasar et al.

Summary: Combining orally administered PI3K inhibitors with immunochemotherapy for indolent B-cell lymphoma has shown toxicity. In the Phase III CHRONOS-4 safety run-in, intravenous copanlisib plus rituximab-based immunochemotherapy was well-tolerated with no dose-limiting toxicities and high preliminary objective response rates. Copanlisib is the first PI3K inhibitor to demonstrate safe and effective combinability with immunochemotherapy, with ongoing evaluation.

CLINICAL LYMPHOMA MYELOMA & LEUKEMIA (2021)

添加到收藏夹

Article Oncology

Everolimus plus aromatase inhibitors as maintenance therapy after first-line chemotherapy: Final results of the phase III randomised MAIN-A (MAINtenance Afinitor) trial

Valentina Guarneri et al.

Summary: Despite no significant difference between maintenance everolimus combined with aromatase inhibitors and aromatase inhibitors monotherapy for patients with disease control after first-line chemotherapy, there are differences in terms of efficacy, response rate, and survival period.

EUROPEAN JOURNAL OF CANCER (2021)

添加到收藏夹

Article Oncology

The Evolving Use of Phosphatidylinositol 3-Kinase Inhibitors for the Treatment of Chronic Lymphocytic Leukemia

Benjamin L. Lampson et al.

HEMATOLOGY-ONCOLOGY CLINICS OF NORTH AMERICA (2021)

添加到收藏夹

Article Pharmacology & Pharmacy

Population Pharmacokinetics of Ipatasertib and Its Metabolite in Cancer Patients

Kenta Yoshida et al.

Summary: A population pharmacokinetic study was conducted to characterize the pharmacokinetic profiles of ipatasertib and its metabolite M1. Covariate effects of ipatasertib include decreased oral clearance with increasing age and coadministration of abiraterone, as well as decreased bioavailability with increasing weight. For M1, increased body weight was associated with an increase in both peripheral distribution volume and intercompartmental clearance. Coadministration of abiraterone was estimated to increase M1 exposure by 61% at steady state.

JOURNAL OF CLINICAL PHARMACOLOGY (2021)

添加到收藏夹

Article Oncology

The PI3K/mTOR Inhibitor Ompalisib Suppresses Nonhomologous End Joining and Sensitizes Cancer Cells to Radio- and Chemotherapy

Jie Du et al.

Summary: NHEJ, the predominant pathway for DNA repair, needs inhibitors to enhance the efficacy of radiotherapy and chemotherapy. Through screening, omipalisib was identified as an effective sensitizer for cell death induced by DNA damage, suppressing the NHEJ pathway.

MOLECULAR CANCER RESEARCH (2021)

添加到收藏夹

Article Oncology

ATR Inhibitor M6620 (VX-970) Enhances the Effect of Radiation in Non-Small Cell Lung Cancer Brain Metastasis Patient-Derived Xenografts

Andrew M. Baschnagel et al.

Summary: The study found enrichment of DDR pathways in many NSCLC patient tumors. M6620 can enhance the effect of radiation on NSCLC brain metastases, leading to improved overall survival in mice when used in combination with radiation.

MOLECULAR CANCER THERAPEUTICS (2021)

添加到收藏夹

Article Oncology

Effectiveness of Adding Everolimus to the First-line Treatment of Advanced Breast Cancer in Premenopausal Women Who Experienced Disease Progression While Receiving Selective Estrogen Receptor Modulators A Phase 2 Randomized Clinical Trial

Ying Fan et al.

Summary: The study compared the effectiveness of everolimus plus letrozole vs letrozole alone in premenopausal women with HR-positive/ERBB2-negative advanced breast cancer. Patients receiving everolimus plus letrozole had a significantly longer median progression-free survival compared with those receiving letrozole alone, indicating the effectiveness of everolimus even after disease progression with the same endocrine agent.

JAMA ONCOLOGY (2021)

添加到收藏夹

Article Pharmacology & Pharmacy

DNA-PK inhibition by M3814 enhances chemosensitivity in non-small cell lung cancer

Manni Wang et al.

Summary: The study identified that the DNA-PK inhibitor M3814 enhanced the anti-tumor effect of chemotherapy in NSCLC cell lines, providing a theoretical basis for its potential use in clinical practice to optimize NSCLC treatment.

ACTA PHARMACEUTICA SINICA B (2021)

添加到收藏夹

Article Medicine, General & Internal

Efficacy of Sirolimus Treatment in PEComa-10 Years of Practice Perspective

Tomasz Switaj et al.

Summary: The study demonstrates that sirolimus is an effective first-line treatment for PEComa patients, with a high objective response rate of 73% and disease control achieved in all patients. The 5-year overall survival rate was 65%, indicating promising long-term efficacy of targeted therapy for PEComa.

JOURNAL OF CLINICAL MEDICINE (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

Article Hematology

Integrated safety analysis of umbralisib, a dual PI3Kδ/CK1ε inhibitor, in relapsed/refractory lymphoid malignancies

Matthew S. Davids et al.

Summary: Umbralisib, a dual inhibitor of PI3K delta and CK1 epsilon, showed favorable long-term tolerability in the treatment of lymphoid malignancies. Common adverse events include diarrhea, nausea, and fatigue, with low rates of serious adverse events of special interest.

BLOOD ADVANCES (2021)

添加到收藏夹

Review Oncology

Targeting the replication stress response through synthetic lethal strategies in cancer medicine

Natalie Y. L. Ngoi et al.

Summary: The replication stress response (RSR) is crucial for maintaining genomic integrity in the presence of elevated replicative stress, with increasing dependence of cancers on RSR. Drug candidates targeting key RSR nodes show promising efficacy in early phase trials, offering potential for overcoming PARP inhibitor resistance.

TRENDS IN CANCER (2021)

添加到收藏夹

Review Hematology

Update on the role of copanlisib in hematologic malignancies

Thuy Le et al.

Summary: This article discusses the application of the PI3K inhibitor Copanlisib in the treatment of hematologic malignancies like relapsed/refractory follicular lymphoma, as well as its potential for combination therapy. Copanlisib stands out among other PI3K inhibitors for its unique potential to enhance cancer treatment outcomes.

THERAPEUTIC ADVANCES IN HEMATOLOGY (2021)

添加到收藏夹

Article Oncology

A phase I trial of temsirolimus and erlotinib in patients with refractory solid tumors

Haeseong Park et al.

Summary: The combination of temsirolimus and erlotinib showed promising efficacy in refractory solid tumor patients, with well-tolerated drug toxicity. Most patients in the dose escalation and expansion cohorts experienced disease stabilization, with no complete or partial responses observed.

CANCER CHEMOTHERAPY AND PHARMACOLOGY (2021)

添加到收藏夹

Article Oncology

Effectiveness of Adding Everolimus to the First-line Treatment of Advanced Breast Cancer in PremenopausalWomen Who Experienced Disease Progression While Receiving Selective Estrogen Receptor Modulators A Phase 2 Randomized Clinical Trial

Ying Fan et al.

Summary: The study compared the effectiveness of everolimus plus letrozole with letrozole alone in premenopausal women with HR-positive/ERBB2-negative advanced breast cancer. The results showed that combination therapy significantly prolonged progression-free survival compared to letrozole monotherapy, even after crossover.

JAMA ONCOLOGY (2021)

添加到收藏夹

Article Oncology

Phase Ib study of the MEK inhibitor cobimetinib (GDC-0973) in combination with the PI3K inhibitor pictilisib (GDC-0941) in patients with advanced solid tumors

Geoffrey Shapiro et al.

INVESTIGATIONAL NEW DRUGS (2020)

添加到收藏夹

Article Oncology

Pharmacology of the ATM Inhibitor AZD0156: Potentiation of Irradiation and Olaparib Responses Preclinically

Lucy C. Riches et al.

MOLECULAR CANCER THERAPEUTICS (2020)

添加到收藏夹

Article Oncology

A phase I study of vistusertib (dual mTORC1/2 inhibitor) in patients with previously treated glioblastoma multiforme: a CCTG study

Sarah Lapointe et al.

INVESTIGATIONAL NEW DRUGS (2020)

添加到收藏夹

Article Oncology

The Novel ATR Inhibitor BAY 1895344 Is Efficacious as Monotherapy and Combined with DNA Damage-Inducing or Repair-Compromising Therapies in Preclinical Cancer Models

Antje M. Wengner et al.

MOLECULAR CANCER THERAPEUTICS (2020)

添加到收藏夹

Article Hematology

Long-term safety and efficacy of the PI3K inhibitor copanlisib in patients with relapsed or refractory indolent lymphoma: 2-year follow-up of the CHRONOS-1 study

Martin Dreyling et al.

AMERICAN JOURNAL OF HEMATOLOGY (2020)

添加到收藏夹

Article Oncology

First-in-Human Phase I Study to Evaluate the Brain-Penetrant PI3K/mTOR Inhibitor GDC-0084 in Patients with Progressive or Recurrent High-Grade Glioma

Patrick Y. Wen et al.

CLINICAL CANCER RESEARCH (2020)

添加到收藏夹

Review Oncology

Mechanisms of resistance to mTOR inhibitors

Luigi Formisano et al.

CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY (2020)

添加到收藏夹

Review Biochemistry & Molecular Biology

Control of Akt activity and substrate phosphorylation in cells

Ivan Yudushkin

IUBMB LIFE (2020)

添加到收藏夹

Article Oncology

Capivasertib Plus Paclitaxel Versus Placebo Plus Paclitaxel As First-Line Therapy for Metastatic Triple-Negative Breast Cancer: The PAKT Trial

Peter Schmid et al.

JOURNAL OF CLINICAL 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

Article Cell Biology

Circumventing AKT-Associated Radioresistance in Oral Cancer by Novel Nanoparticle-Encapsulated Capivasertib

Liwei Lang et al.

CELLS (2020)

添加到收藏夹

Review Biochemistry & Molecular Biology

Inhibitors in AKTion: ATP-competitive vs allosteric

Glorianne Lazaro et al.

BIOCHEMICAL SOCIETY TRANSACTIONS (2020)

添加到收藏夹

Article Oncology

Preclinical and Dose-Finding Phase I Trial Results of Combined Treatment with a TORC1/2 Inhibitor (TAK-228) and Aurora A Kinase Inhibitor (Alisertib) in Solid Tumors

S. Lindsey Davis et al.

CLINICAL CANCER RESEARCH (2020)

添加到收藏夹

Article Oncology

ASCEND: Phase III, Randomized Trial of Acalabrutinib Versus Idelalisib Plus Rituximab or Bendamustine Plus Rituximab in Relapsed or Refractory Chronic Lymphocytic Leukemia

Paolo Ghia et al.

JOURNAL OF CLINICAL ONCOLOGY (2020)

添加到收藏夹

Review Biochemistry & Molecular Biology

mTOR signaling pathway and mTOR inhibitors in cancer: progress and challenges

Zhilin Zou et al.

CELL AND BIOSCIENCE (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

Article Clinical Neurology

Phase I clinical trial of temsirolimus and perifosine for recurrent glioblastoma

Thomas J. Kaley et al.

ANNALS OF CLINICAL AND TRANSLATIONAL NEUROLOGY (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

Article Oncology

Phase I Trial of First-in-Class ATR Inhibitor M6620 (VX-970) as Monotherapy or in Combination With Carboplatin in Patients With Advanced Solid Tumors

Timothy A. Yap et al.

JOURNAL OF CLINICAL ONCOLOGY (2020)

添加到收藏夹

Article Oncology

Buparlisib plus carboplatin or lomustine in patients with recurrent glioblastoma: a phase Ib/II, open-label, multicentre, randomised study

Mark Rosenthal et al.

ESMO OPEN (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 Oncology

Mouse-human co-clinical trials demonstrate superior anti-tumour effects of buparlisib (BKM120) and cetuximab combination in squamous cell carcinoma of head and neck

Hye Ryun Kim et al.

BRITISH JOURNAL OF CANCER (2020)

添加到收藏夹

Article Oncology

Everolimus plus bevacizumab is an effective first-line treatment for patients with advanced papillary variant renal cell carcinoma: Final results from a phase II trial

Darren R. Feldman et al.

CANCER (2020)

添加到收藏夹

Review Biochemistry & Molecular Biology

DNA Damage and Cancer Immunotherapy: A STING in the Tale

Timo Reislander et al.

MOLECULAR CELL (2020)

添加到收藏夹

Review Cell Biology

PI3K/AKT pathway as a key link modulates the multidrug resistance of cancers

Rui Liu et al.

CELL DEATH & DISEASE (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

Article Medicine, Research & Experimental

PI3K/AKT/mTOR signaling in gastric cancer: Epigenetics and beyond

Sadegh Fattahi et al.

LIFE SCIENCES (2020)

添加到收藏夹

Review Genetics & Heredity

DNA-PKcs: A Multi-Faceted Player in DNA Damage Response

Xiaoqiao Yue et al.

FRONTIERS IN GENETICS (2020)

添加到收藏夹

Review Oncology

The PI3K-AKT network at the interface of oncogenic signalling and cancer metabolism

Gerta Hoxhaj et al.

NATURE REVIEWS CANCER (2020)

添加到收藏夹

Article Oncology

A phase 2 study of ofatumumab (Arzerra®) in combination with a pan-AKT inhibitor (afuresertib) in previously treated patients with chronic lymphocytic leukemia (CLL)*

Christine I. Chen et al.

LEUKEMIA & LYMPHOMA (2019)

添加到收藏夹

Article Oncology

The Dual PI3K/mTOR Pathway Inhibitor GDC-0084 Achieves Antitumor Activity in PIK3CA-Mutant Breast Cancer Brain Metastases

Franziska M. Ippen et al.

CLINICAL CANCER RESEARCH (2019)

添加到收藏夹

Article Oncology

Oral MEK 1/2 Inhibitor Trametinib in Combination With AKT Inhibitor GSK2141795 in Patients With Acute Myeloid Leukemia With RAS Mutations: A Phase II Study

Brittany Knick Ragon et al.

CLINICAL LYMPHOMA MYELOMA & LEUKEMIA (2019)

添加到收藏夹

Article Respiratory System

A randomised, placebo-controlled study of omipalisib (PI3K/mTOR) in idiopathic pulmonary fibrosis

Pauline T. Lukey et al.

EUROPEAN RESPIRATORY JOURNAL (2019)

添加到收藏夹

Article Oncology

Buparlisib in Patients With Recurrent Glioblastoma Harboring Phosphatidylinositol 3-Kinase Pathway Activation: An Open-Label, Multicenter, Multi-Arm, Phase II Trial

Patrick Y. Wen et al.

JOURNAL OF CLINICAL ONCOLOGY (2019)

添加到收藏夹

Article Oncology

DYNAMO: A Phase II Study of Duvelisib (IPI-145) in Patients With Refractory Indolent Non-Hodgkin Lymphoma

Ian W. Flinn et al.

JOURNAL OF CLINICAL ONCOLOGY (2019)

添加到收藏夹

Review Genetics & Heredity

The relation between PI3K/AKT signalling pathway and cancer

Saeed Noorolyai et al.

GENE (2019)

添加到收藏夹

Article Oncology

Results from a single arm, single stage phase II trial of trametinib and GSK2141795 in persistent or recurrent cervical cancer

Joyce F. Liu et al.

GYNECOLOGIC ONCOLOGY (2019)

添加到收藏夹

Review Cell Biology

PI3K isoforms in cell signalling and vesicle trafficking

Benoit Bilanges et al.

NATURE REVIEWS MOLECULAR CELL BIOLOGY (2019)

添加到收藏夹

Review Cell Biology

Class II PI3K Functions in Cell Biology and Disease

Federico Gulluni et al.

TRENDS IN CELL BIOLOGY (2019)

添加到收藏夹

Article Pharmacology & Pharmacy

Alpelisib: First Global Approval

Anthony Markham

DRUGS (2019)

添加到收藏夹

Article Oncology

Final Results of a Randomized, Phase III Study of Rituximab With or Without Idelalisib Followed by Open-Label Idelalisib in Patients With Relapsed Chronic Lymphocytic Leukemia

Jeff P. Sharman et al.

JOURNAL OF CLINICAL ONCOLOGY (2019)

添加到收藏夹

Review Oncology

Targeting mTOR for cancer therapy

Hui Hua et al.

JOURNAL OF HEMATOLOGY & ONCOLOGY (2019)

添加到收藏夹

Review Oncology

PI3K/Akt/mTOR inhibitors in cancer: At the bench and bedside

Ali S. Alzahrani

SEMINARS IN CANCER BIOLOGY (2019)

添加到收藏夹

Article Oncology

Randomized Phase II Trial of Bevacizumab or Temsirolimus in Combination With Chemotherapy for First Relapse Rhabdomyosarcoma: A Report From the Children's Oncology Group

Leo Mascarenhas et al.

JOURNAL OF CLINICAL ONCOLOGY (2019)

添加到收藏夹

Article Oncology

Therapeutic Implications of p53 Status on Cancer Cell Fate Following Exposure to Ionizing Radiation and the DNA-PK Inhibitor M3814

Qing Sun et al.

MOLECULAR CANCER RESEARCH (2019)

添加到收藏夹

Review Oncology

mTOR: Role in cancer, metastasis and drug resistance

Avaniyapuram Kannan Murugan

SEMINARS IN CANCER BIOLOGY (2019)

添加到收藏夹

Review Biochemistry & Molecular Biology

For Better or Worse: The Potential for Dose Limiting the On-Target Toxicity of PI 3-Kinase Inhibitors

Christina M. Buchanan et al.

BIOMOLECULES (2019)

添加到收藏夹

Article Hematology

Combination trial of duvelisib (IPI-145) with rituximab or bendamustine/rituximab in patients with non-Hodgkin lymphoma or chronic lymphocytic leukemia

Ian W. Flinn et al.

AMERICAN JOURNAL OF HEMATOLOGY (2019)

添加到收藏夹

Review Oncology

Management of toxicity to isoform α-specific PI3K inhibitors

S. E. Nunnery et al.

ANNALS OF ONCOLOGY (2019)

添加到收藏夹

Review Biochemistry & Molecular Biology

New insights into the evolutionary conservation of the sole PIKK pseudokinase Tra1/TRRAP

Alberto Elias-Villalobos et al.

BIOCHEMICAL SOCIETY TRANSACTIONS (2019)

添加到收藏夹

Meeting Abstract Hematology

Akt Inhibition Differently Controls PRC2 Components and Synergizes with Dual EZH2/1 Inhibitor in the Treatment of Multiple Myeloma

Mohamed Rizk et al.

BLOOD (2019)

添加到收藏夹

Review Pharmacology & Pharmacy

Targeting AKT for cancer therapy

Maryam Shariati et al.

EXPERT OPINION ON INVESTIGATIONAL DRUGS (2019)

添加到收藏夹

Article Oncology

Co-targeting PI3K/Akt and MAPK/ERK pathways leads to an enhanced antitumor effect on human hypopharyngeal squamous cell carcinoma

Xiaolin Peng et al.

JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY (2019)

添加到收藏夹

Article Biochemistry & Molecular Biology

Inhibition of phosphatidylinositol 3-kinase by PX-866 suppresses temozolomide-induced autophagy and promotes apoptosis in glioblastoma cells

Bryan G. Harder et al.

MOLECULAR MEDICINE (2019)

添加到收藏夹

Article Oncology

Phase IB Dose Escalation and Expansion Study of AKT Inhibitor Afuresertib with Carboplatin and Paclitaxel in Recurrent Platinum-resistant Ovarian Cancer

Sarah P. Blagden et al.

CLINICAL CANCER RESEARCH (2019)

添加到收藏夹

Article Oncology

Safety lead-in of the MEK inhibitor trametinib in combination with GSK2141795, an AKT inhibitor, in patients with recurrent endometrial cancer: An NRG Oncology/GOG study

Shannon N. Westin et al.

GYNECOLOGIC ONCOLOGY (2019)

添加到收藏夹

Article Genetics & Heredity

Pharmacodynamic Study of Miransertib in Individuals with Proteus Syndrome

Kim M. Keppler-Noreuil et al.

AMERICAN JOURNAL OF HUMAN GENETICS (2019)

添加到收藏夹

Article Oncology

Phase 1 Dose Escalation Study of the Allosteric AKT Inhibitor BAY 1125976 in Advanced Solid Cancer-Lack of Association between Activating AKT Mutation and AKT Inhibition-Derived Efficacy

Andreas Schneeweiss et al.

CANCERS (2019)

添加到收藏夹

Article Oncology

First-In-Human Phase I Study Of A Dual mTOR Kinase And DNA-PK Inhibitor (CC-115) In Advanced Malignancy

Pamela Munster et al.

CANCER MANAGEMENT AND RESEARCH (2019)

添加到收藏夹

Article Oncology

Phase II trial of AKT inhibitor MK-2206 in patients with advanced breast cancer who have tumors with PIK3CA or AKT mutations, and/or PTEN loss/PTEN mutation

Yan Xing et al.

BREAST CANCER RESEARCH (2019)

添加到收藏夹

Review Biochemistry & Molecular Biology

Class II PI3Ks at the Intersection between Signal Transduction and Membrane Trafficking

Jean Piero Margaria et al.

BIOMOLECULES (2019)

添加到收藏夹

Article Oncology

Phase II Study of BEZ235 versus Everolimus in Patients with Mammalian Target of Rapamycin Inhibitor-Naive Advanced Pancreatic Neuroendocrine Tumors

Ramon Salazar et al.

ONCOLOGIST (2018)

添加到收藏夹

Article Oncology

Dual MEK/AKT inhibition with trametinib and GSK2141795 does not yield clinical benefit in metastatic NRAS-mutant and wild-type melanoma

Alain P. Algazi et al.

PIGMENT CELL & MELANOMA RESEARCH (2018)

添加到收藏夹

Article Oncology

Vistusertib (dual m-TORC1/2 inhibitor) in combination with paclitaxel in patients with high-grade serous ovarian and squamous non-small-cell lung cancer

B. Basu et al.

ANNALS OF ONCOLOGY (2018)

添加到收藏夹

Editorial Material Oncology

From checkpoint to checkpoint: DNA damage ATR/Chk1 checkpoint signalling elicits PD-L1 immune checkpoint activation

Kent W. Mouw et al.

BRITISH JOURNAL OF CANCER (2018)

添加到收藏夹

Article Pharmacology & Pharmacy

Antitumor efficacy of liposome-encapsulated NVP-BEZ 235 in combination with irreversible electroporation

Li Tian et al.

DRUG DELIVERY (2018)

添加到收藏夹

Article Biochemistry & Molecular Biology

Phosphatidylinositol 3-kinase and isoforms play key roles in metastasis of prostate cancer DU145 cells

Zhe Zhang et al.

FASEB JOURNAL (2018)

添加到收藏夹

Article Chemistry, Medicinal

The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2H-pyran-4-yl)-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one)

Kurt G. Pike et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

添加到收藏夹

Article Oncology

Phase I Trial of a Tablet Formulation of Pilaralisib, a Pan-Class I PI3K Inhibitor, in Patients with Advanced Solid Tumors

Gerald Edelman et al.

ONCOLOGIST (2018)

添加到收藏夹

Article Multidisciplinary Sciences

Buparlisib is a brain penetrable pan-PI3K inhibitor

Mark C. de Gooijer et al.

SCIENTIFIC REPORTS (2018)

添加到收藏夹

Article Hematology

Voxtalisib (XL765) in patients with relapsed or refractory non-Hodgkin lymphoma or chronic lymphocytic leukaemia: an open-label, phase 2 trial

Jennifer R. Brown et al.

LANCET HAEMATOLOGY (2018)

添加到收藏夹

Review Endocrinology & Metabolism

PTEN: Tumor Suppressor and Metabolic Regulator

Chien-Yu Chen et al.

FRONTIERS IN ENDOCRINOLOGY (2018)

添加到收藏夹

Article Multidisciplinary Sciences

The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models

Stephen T. Durant et al.

SCIENCE ADVANCES (2018)

添加到收藏夹

Article Hematology

Duvelisib, an oral dual PI3K-, inhibitor, shows clinical and pharmacodynamic activity in chronic lymphocytic leukemia and small lymphocytic lymphoma in a phase 1 study

Susan O'Brien et al.

AMERICAN JOURNAL OF HEMATOLOGY (2018)

添加到收藏夹

Article Multidisciplinary Sciences

Suppression of insulin feedback enhances the efficacy of PI3K inhibitors

Benjamin D. Hopkins et al.

NATURE (2018)

添加到收藏夹

Article Hematology

The phase 3 DUO trial: duvelisib vs ofatumumab in relapsed and refractory CLL/SLL

Ian W. Flinn et al.

BLOOD (2018)

添加到收藏夹

Article Oncology

A phase Ib dose-escalation and expansion study of the oral MEK inhibitor pimasertib and PI3K/MTOR inhibitor voxtalisib in patients with advanced solid tumours

Alison M. Schram et al.

BRITISH JOURNAL OF CANCER (2018)

添加到收藏夹

Article Pharmacology & Pharmacy

Duvelisib: First Global Approval

Hannah A. Blair

DRUGS (2018)

添加到收藏夹

Review Medicine, General & Internal

Phosphatidylinositol 3-Kinase, Growth Disorders, and Cancer

Marcus D. Goncalves et al.

NEW ENGLAND JOURNAL OF MEDICINE (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

Synthetically Lethal Interactions of ATM, ATR, and DNA-PKcs

Omar L. Kantidze et al.

TRENDS IN CANCER (2018)

添加到收藏夹

Article Hematology

Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies

Changchun Deng et al.

BLOOD (2017)

添加到收藏夹

Article Oncology

BAY 1125976, a selective allosteric AKT1/2 inhibitor, exhibits high efficacy on AKT signaling-dependent tumor growth in mouse models

Oliver Politz et al.

INTERNATIONAL JOURNAL OF CANCER (2017)

添加到收藏夹

Article Oncology

Phase Ia/Ib study of the pan-class I PI3K inhibitor pictilisib (GDC-0941) administered as a single agent in Japanese patients with solid tumors and in combination in Japanese patients with non-squamous non-small cell lung cancer

Noboru Yamamoto et al.

INVESTIGATIONAL NEW DRUGS (2017)

添加到收藏夹

Editorial Material Pharmacology & Pharmacy

Duvelisib: a phosphoinositide-3 kinase/inhibitor for chronic lymphocytic leukemia

Hima V. Vangapandu et al.

EXPERT OPINION ON INVESTIGATIONAL DRUGS (2017)

添加到收藏夹

Article Oncology

AKT Inhibition in Solid Tumors With AKT1 Mutations

David M. Hyman et al.

JOURNAL OF CLINICAL ONCOLOGY (2017)

添加到收藏夹

Article Oncology

Buparlisib plus fulvestrant versus placebo plus fulvestrant in postmenopausal, hormone receptor-positive, HER2-negative, advanced breast cancer (BELLE-2): a randomised, double-blind, placebo-controlled, phase 3 trial

Jose Baselga et al.

LANCET ONCOLOGY (2017)

添加到收藏夹

Article Oncology

Ipatasertib plus paclitaxel versus placebo plus paclitaxel as first-line therapy for metastatic triple-negative breast cancer (LOTUS): a multicentre, randomised, double-blind, placebo-controlled, phase 2 trial

Sung-Bae Kim et al.

LANCET ONCOLOGY (2017)

添加到收藏夹

Review Biochemistry & Molecular Biology

ATM, ATR, and DNA-PK: The Trinity at the Heart of the DNA Damage Response

Andrew N. Blackford et al.

MOLECULAR CELL (2017)

添加到收藏夹

Article Oncology

A Phase I Dose-Escalation Study of the Safety and Pharmacokinetics of Pictilisib in Combination with Erlotinib in Patients with Advanced Solid Tumors

Stephen Leong et al.

ONCOLOGIST (2017)

添加到收藏夹

Article Oncology

Phase I Dose-Escalation Study of Pilaralisib (SAR245408, XL147) in Combination with Paclitaxel and Carboplatin in Patients with Solid Tumors

Jennifer Wheler et al.

ONCOLOGIST (2017)

添加到收藏夹

Article Oncology

A Phase I Study of Abiraterone Acetate Combined with BEZ235, a Dual PI3K/mTOR Inhibitor, in Metastatic Castration Resistant Prostate Cancer

Xiao X. Wei et al.

ONCOLOGIST (2017)

添加到收藏夹

Review Pharmacology & Pharmacy

Maximising the potential of MKT inhibitors as anti-cancer treatments

Jessica S. Brown et al.

PHARMACOLOGY & THERAPEUTICS (2017)

添加到收藏夹

Article Oncology

A Multi-Arm Phase I Study of the PI3K/mTOR Inhibitors PF-04691502 and Gedatolisib (PF-05212384) plus Irinotecan or the MEK Inhibitor PD-0325901 in Advanced Cancer

Zev A. Wainberg et al.

TARGETED ONCOLOGY (2017)

添加到收藏夹

Article Oncology

CC-115, a dual inhibitor of mTOR kinase and DNA-PK, blocks DNA damage repair pathways and selectively inhibits ATM-deficient cell growth in vitro

Toshiya Tsuji et al.

ONCOTARGET (2017)

添加到收藏夹

Article Multidisciplinary Sciences

AKT1 and AKT2 isoforms play distinct roles during breast cancer progression through the regulation of specific downstream proteins

Marina Riggio et al.

SCIENTIFIC REPORTS (2017)

添加到收藏夹

Article Oncology

A First-Time-in-Human Study of GSK2636771, a Phosphoinositide 3 Kinase Beta-Selective Inhibitor, in Patients with Advanced Solid Tumors

Joaquin Mateo et al.

CLINICAL CANCER RESEARCH (2017)

添加到收藏夹

Article Oncology

Phase II study of copanlisib, a PI3K inhibitor, in relapsed or refractory, indolent or aggressive lymphoma

M. Dreyling et al.

ANNALS OF ONCOLOGY (2017)

添加到收藏夹

Review Biochemistry & Molecular Biology

The PI3K Pathway in Human Disease

David A. Fruman et al.

CELL (2017)

添加到收藏夹

Article Oncology

TAK-228 (formerly MLN0128), an investigational dual TORC1/2 inhibitor plus paclitaxel, with/without trastuzumab, in patients with advanced solid malignancies

Howard A. Burris et al.

CANCER CHEMOTHERAPY AND PHARMACOLOGY (2017)

添加到收藏夹

Article Hematology

Akt inhibitor MK-2206 in combination with bendamustine and rituximab in relapsed or refractory chronic lymphocytic leukemia: Results from the N1087 alliance study

Jeremy T. Larsen et al.

AMERICAN JOURNAL OF HEMATOLOGY (2017)

添加到收藏夹

Article Oncology

A randomized phase 2 study of MK-2206 versus everolimus in refractory renal cell carcinoma

E. Jonasch et al.

ANNALS OF ONCOLOGY (2017)

添加到收藏夹

Review Biochemistry & Molecular Biology

mTOR Signaling in Growth, Metabolism, and Disease

Robert A. Saxton et al.

CELL (2017)

添加到收藏夹

Article Hematology

ATR inhibition induces synthetic lethality and overcomes chemoresistance in TP53- or ATM-defective chronic lymphocytic leukemia cells

Marwan Kwok et al.

BLOOD (2016)

添加到收藏夹

Article Oncology

First-in-Human Phase I Study of GSK2126458, an Oral Pan-Class I Phosphatidylinositol-3-Kinase Inhibitor, in Patients with Advanced Solid Tumor Malignancies

Pamela Munster et al.

CLINICAL CANCER RESEARCH (2016)

添加到收藏夹

Article Biochemistry & Molecular Biology

Combinatorial PX-866 and Raloxifene Decrease Rb Phosphorylation, Cyclin E2 Transcription, and Proliferation of MCF-7 Breast Cancer Cells

Gregory W. Peek et al.

JOURNAL OF CELLULAR BIOCHEMISTRY (2016)

添加到收藏夹

Article Oncology

Pictilisib PI3Kinase inhibitor (a phosphatidylinositol 3-kinase [PI3K] inhibitor) plus paclitaxel for the treatment of hormone receptor-positive, HER2-negative, locally recurrent, or metastatic breast cancer: interim analysis of the multicentre, placebo-controlled, phase II randomised PEGGY study

P. Vuylsteke et al.

ANNALS OF ONCOLOGY (2016)

添加到收藏夹

Article Hematology

Dual TORK/DNA-PK inhibition blocks critical signaling pathways in chronic lymphocytic leukemia

Rachel Thijssen et al.

BLOOD (2016)

添加到收藏夹

Article Hematology

Idelalisib given front-line for treatment of chronic lymphocytic leukemia causes frequent immune-mediated hepatotoxicity

Benjamin L. Lampson et al.

BLOOD (2016)

添加到收藏夹

Article Oncology

A phase 1b study of the Akt-inhibitor MK-2206 in combination with weekly paclitaxel and trastuzumab in patients with advanced HER2-amplified solid tumor malignancies

Amy Jo Chien et al.

BREAST CANCER RESEARCH AND TREATMENT (2016)

添加到收藏夹

Article Oncology

Phase I Study of Apitolisib (GDC-0980), Dual Phosphatidylinositol-3-Kinase and Mammalian Target of Rapamycin Kinase Inhibitor, in Patients with Advanced Solid Tumors

Saoirse O. Dolly et al.

CLINICAL CANCER RESEARCH (2016)

添加到收藏夹

Article Oncology

Mutations in TSC1, TSC2, and MTOR Are Associated with Response to Rapalogs in Patients with Metastatic Renal Cell Carcinoma

David J. Kwiatkowski et al.

CLINICAL CANCER RESEARCH (2016)

添加到收藏夹

Article Oncology

A Randomized, Phase II Trial of Cetuximab With or Without PX-866, an Irreversible Oral Phosphatidylinositol 3-Kinase Inhibitor, in Patients With Metastatic Colorectal Carcinoma

Daniel W. Bowles et al.

CLINICAL COLORECTAL CANCER (2016)

添加到收藏夹

Article Urology & Nephrology

A Randomised Phase 2 Study of AZD2014 Versus Everolimus in Patients with VEGF-Refractory Metastatic Clear Cell Renal Cancer

Thomas Powles et al.

EUROPEAN UROLOGY (2016)

添加到收藏夹

Article Oncology

A randomized phase II non-comparative study of PF-04691502 and gedatolisib (PF-05212384) in patients with recurrent endometrial cancer

Josep Maria del Campo et al.

GYNECOLOGIC ONCOLOGY (2016)

添加到收藏夹

Article Oncology

Invention of a novel photodynamic therapy for tumors using a photosensitizing PI3K inhibitor

Yushi Hayashida et al.

INTERNATIONAL JOURNAL OF CANCER (2016)

添加到收藏夹

Article Oncology

A phase Ib dose-escalation study of the MEK inhibitor trametinib in combination with the PI3K/mTOR inhibitor GSK2126458 in patients with advanced solid tumors

J. E. Grilley-Olson et al.

INVESTIGATIONAL NEW DRUGS (2016)

添加到收藏夹

Article Oncology

Phase II Randomized Preoperative Window-of-Opportunity Study of the PI3K Inhibitor Pictilisib Plus Anastrozole Compared With Anastrozole Alone in Patients With Estrogen Receptor-Positive Breast Cancer

Peter Schmid et al.

JOURNAL OF CLINICAL ONCOLOGY (2016)

添加到收藏夹

Article Oncology

Pictilisib for oestrogen receptor-positive, aromatase inhibitor-resistant, advanced or metastatic breast cancer (FERGI): a randomised, double-blind, placebo-controlled, phase 2 trial

Ian E. Krop et al.

LANCET ONCOLOGY (2016)

添加到收藏夹

Article Biochemistry & Molecular Biology

Design, Synthesis and Biological Evaluation of Novel Benzothiazole Derivatives as Selective PI3Kβ Inhibitors

Shuang Cao et al.

MOLECULES (2016)

添加到收藏夹

Article Oncology

A Phase Ib Study of BEZ235, a Dual Inhibitor of Phosphatidylinositol 3-Kinase (PI3K) and Mammalian Target of Rapamycin (mTOR), in Patients With Advanced Renal Cell Carcinoma

Maria I. Carlo et al.

ONCOLOGIST (2016)

添加到收藏夹

Article Chemistry, Medicinal

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR

Timothy P. Heffron et al.

ACS MEDICINAL CHEMISTRY LETTERS (2016)

添加到收藏夹

Review Neurosciences

Mammalian Target of Rapamycin: Its Role in Early Neural Development and in Adult and Aged Brain Function

Carla Garza-Lombo et al.

FRONTIERS IN CELLULAR NEUROSCIENCE (2016)

添加到收藏夹

Review Chemistry, Multidisciplinary

PI3K isoform-selective inhibitors: next-generation targeted cancer therapies

Xiang Wang et al.

ACTA PHARMACOLOGICA SINICA (2015)

添加到收藏夹

Article Oncology

Phase I/II dose-escalation study of PI3K inhibitors pilaralisib or voxtalisib in combination with letrozole in patients with hormone-receptor-positive and HER2-negative metastatic breast cancer refractory to a non-steroidal aromatase inhibitor

Kimberly Blackwell et al.

BREAST CANCER RESEARCH AND TREATMENT (2015)

添加到收藏夹

Article Hematology

Phase II study of an AKT inhibitor MK2206 in patients with relapsed or refractory lymphoma

Yasuhiro Oki et al.

BRITISH JOURNAL OF HAEMATOLOGY (2015)

添加到收藏夹

Article Oncology

Phase I Trial of the Pan-PI3K Inhibitor Pilaralisib (SAR245408/XL147) in Patients with Chronic Lymphocytic Leukemia (CLL) or Relapsed/Refractory Lymphoma

Jennifer R. Brown et al.

CLINICAL CANCER RESEARCH (2015)

添加到收藏夹

Article Oncology

Phase II study of the PI3K inhibitor pilaralisib (SAR245408; XL147) in patients with advanced or recurrent endometrial carcinoma

Ursula Matulonis et al.

GYNECOLOGIC ONCOLOGY (2015)

添加到收藏夹

Article Immunology

DNA Damage Primes the Type I Interferon System via the Cytosolic DNA Sensor STING to Promote Anti-Microbial Innate Immunity

Anetta Hartlova et al.

IMMUNITY (2015)

添加到收藏夹

Article Oncology

Randomized Phase II Trial of Ridaforolimus in Advanced Endometrial Carcinoma

Amit M. Oza et al.

JOURNAL OF CLINICAL ONCOLOGY (2015)

添加到收藏夹

Review Oncology

Management of adverse events associated with idelalisib treatment: expert panel opinion

Steven E. Coutre et al.

LEUKEMIA & LYMPHOMA (2015)

添加到收藏夹

Article Oncology

The Selective PI3K Inhibitor XL147 (SAR245408) Inhibits Tumor Growth and Survival and Potentiates the Activity of Chemotherapeutic Agents in Preclinical Tumor Models

Paul Foster et al.

MOLECULAR CANCER THERAPEUTICS (2015)

添加到收藏夹

Article Oncology

AZD2014, an Inhibitor of mTORC1 and mTORC2, Is Highly Effective in ER+ Breast Cancer When Administered Using Intermittent or Continuous Schedules

Sylvie M. Guichard et al.

MOLECULAR CANCER THERAPEUTICS (2015)

添加到收藏夹

Review Biochemistry & Molecular Biology

Targeting the DNA Damage Response in Cancer

Mark J. O'Connor

MOLECULAR CELL (2015)

添加到收藏夹

Article Oncology

Phase I dose-escalation study of the PI3K/mTOR inhibitor voxtalisib (SAR245409, XL765) plus temozolomide with or without radiotherapy in patients with high-grade glioma

Patrick Y. Wen et al.

NEURO-ONCOLOGY (2015)

添加到收藏夹

Article Oncology

A randomized, phase 2 trial of docetaxel with or without PX-866, an irreversible oral phosphatidylinositol 3-kinase inhibitor, in patients with relapsed or metastatic head and neck squamous cell cancer

Antonio Jimeno et al.

ORAL ONCOLOGY (2015)

添加到收藏夹

Article Oncology

A putative biomarker signature for clinically effective AKT inhibition: correlation of in vitro, in vivo and clinical data identifies the importance of modulation of the mTORC1 pathway

Azadeh Cheraghchi-Bashi et al.

ONCOTARGET (2015)

添加到收藏夹

Article Oncology

A randomized, phase II trial of cetuximab with or without PX-866, an irreversible oral phosphatidylinositol 3-kinase inhibitor, in patients with relapsed or metastatic head and neck squamous cell cancer

A. Jimeno et al.

ANNALS OF ONCOLOGY (2015)

添加到收藏夹

Article Oncology

Phase I study of the MEK inhibitor trametinib in combination with the AKT inhibitor afuresertib in patients with solid tumors and multiple myeloma

Anthony W. Tolcher et al.

CANCER CHEMOTHERAPY AND PHARMACOLOGY (2015)

添加到收藏夹

Article Chemistry, Medicinal

Phosphatidylinositol 3-Kinase (PI3K) and Phosphatidylinositol 3-Kinase-Related Kinase (PIKK) Inhibitors: Importance of the Morpholine Ring

Martin Andrs et al.

JOURNAL OF MEDICINAL CHEMISTRY (2015)

添加到收藏夹

Review Oncology

PI3K in cancer: divergent roles of isoforms, modes of activation and therapeutic targeting

Lauren M. Thorpe et al.

NATURE REVIEWS CANCER (2015)

添加到收藏夹

Article Hematology

The novel AKT inhibitor afuresertib shows favorable safety, pharmacokinetics, and clinical activity in multiple myeloma

Andrew Spencer et al.

BLOOD (2014)

添加到收藏夹

Article Oncology

Targeting Akt3 Signaling in Triple-Negative Breast Cancer

Y. Rebecca Chin et al.

CANCER RESEARCH (2014)

添加到收藏夹

Review Oncology

Targeting the PI3K/AKT/mTOR pathway in estrogen receptor-positive breast cancer

Eva Maria Ciruelos Gil

CANCER TREATMENT REVIEWS (2014)

添加到收藏夹

Article Biochemistry & Molecular Biology

Spatial Control of the TSC Complex Integrates Insulin and Nutrient Regulation of mTORC1 at the Lysosome

Suchithra Menon et al.

CELL (2014)

添加到收藏夹

Article Oncology

Phase I Safety, Pharmacokinetic, and Pharmacodynamic Study of SAR245408 (XL147), an Oral Pan-Class I PI3K Inhibitor, in Patients with Advanced Solid Tumors

Geoffrey I. Shapiro et al.

CLINICAL CANCER RESEARCH (2014)

添加到收藏夹

Article Pharmacology & Pharmacy

Idelalisib: First Global Approval

Anthony Markham

DRUGS (2014)

添加到收藏夹

Article Oncology

A Randomized, Phase 2 Trial of Docetaxel with or without PX-866, an Irreversible Oral Phosphatidylinositol 3-Kinase Inhibitor, in Patients with Relapsed or Metastatic Non-Small-Cell Lung Cancer

Benjamin Levy et al.

JOURNAL OF THORACIC ONCOLOGY (2014)

添加到收藏夹

Article Medicine, General & Internal

Idelalisib and Rituximab in Relapsed Chronic Lymphocytic Leukemia

Richard R. Furman et al.

NEW ENGLAND JOURNAL OF MEDICINE (2014)

添加到收藏夹

Article Cell Biology

Assessing PIK3CA and PTEN in Early-Phase Trials with PI3K/AKT/mTOR Inhibitors

Filip Janku et al.

CELL REPORTS (2014)

添加到收藏夹

Article Oncology

Class III PI3K Vps34: essential roles in autophagy, endocytosis, and heart and liver function

Nadia Jaber et al.

INOSITOL PHOSPHOLIPID SIGNALING IN PHYSIOLOGY AND DISEASE (2013)

添加到收藏夹

Article Oncology

Ridaforolimus as a single agent in advanced endometrial cancer: results of a single-arm, phase 2 trial

N. Colombo et al.

BRITISH JOURNAL OF CANCER (2013)

添加到收藏夹

Article Oncology

Results of an International Randomized Phase III Trial of the Mammalian Target of Rapamycin Inhibitor Ridaforolimus Versus Placebo to Control Metastatic Sarcomas in Patients After Benefit From Prior Chemotherapy

George D. Demetri et al.

JOURNAL OF CLINICAL ONCOLOGY (2013)

添加到收藏夹

Article Oncology

BAY 80-6946 Is a Highly Selective Intravenous PI3K Inhibitor with Potent p110α and p110δ Activities in Tumor Cell Lines and Xenograft Models

Ningshu Liu et al.

MOLECULAR CANCER THERAPEUTICS (2013)

添加到收藏夹

Article Cell Biology

Sinl phosphorylation impairs mTORC2 complex integrity and inhibits downstream Akt signalling to suppress tumorigenesis

Pengda Liu et al.

NATURE CELL BIOLOGY (2013)

添加到收藏夹

Article Pharmacology & Pharmacy

Ridaforolimus in advanced or metastatic soft tissue and bone sarcomas

Monica M. Mita et al.

EXPERT REVIEW OF CLINICAL PHARMACOLOGY (2013)

添加到收藏夹

Review Medicine, General & Internal

Clinical development of phosphatidylinositol 3-kinase inhibitors for cancer treatment

Irene Brana et al.

BMC MEDICINE (2012)

添加到收藏夹

Review Oncology

Development of PI3K/AKT/mTOR Pathway Inhibitors and Their Application in Personalized Therapy for Non-Small-Cell Lung Cancer

Vassiliki Papadimitrakopoulou

JOURNAL OF THORACIC ONCOLOGY (2012)

添加到收藏夹

Article Biology

DNA-PK is a DNA sensor for IRF-3-dependent innate immunity

Brian J. Ferguson et al.

ELIFE (2012)

添加到收藏夹

Meeting Abstract Hematology

TAS-117, a Novel Selective Akt Inhibitor Demonstrates Significant Growth Inhibition in Multiple Myeloma Cells in Vitro and in Vivo

Naoya Mimura et al.

BLOOD (2012)

添加到收藏夹

Review Biochemistry & Molecular Biology

Akt, FoxO and regulation of apoptosis

Xinbo Zhang et al.

BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH (2011)

添加到收藏夹

Article Biochemistry & Molecular Biology

Domains of Tra1 Important for Activator Recruitment and Transcription Coactivator Functions of SAGA and NuA4 Complexes

Bruce A. Knutson et al.

MOLECULAR AND CELLULAR BIOLOGY (2011)

添加到收藏夹

Article Oncology

GDC-0980 Is a Novel Class I PI3K/mTOR Kinase Inhibitor with Robust Activity in Cancer Models Driven by the PI3K Pathway

Jeffrey J. Wallin et al.

MOLECULAR CANCER THERAPEUTICS (2011)

添加到收藏夹

Article Oncology

PIK3CA Mutations in Patients with Advanced Cancers Treated with PI3K/AKT/mTOR Axis Inhibitors

Filip Janku et al.

MOLECULAR CANCER THERAPEUTICS (2011)

添加到收藏夹

Review Biochemistry & Molecular Biology

Targeting abnormal DNA double strand break repair in cancer

Feyruz V. Rassool et al.

CELLULAR AND MOLECULAR LIFE SCIENCES (2010)

添加到收藏夹

Article Oncology

Predictive Biomarkers of Sensitivity to the Phosphatidylinositol 3′ Kinase Inhibitor GDC-0941 in Breast Cancer Preclinical Models

Carol O'Brien et al.

CLINICAL CANCER RESEARCH (2010)

添加到收藏夹

Article Oncology

MK-2206, an Allosteric Akt Inhibitor, Enhances Antitumor Efficacy by Standard Chemotherapeutic Agents or Molecular Targeted Drugs In vitro and In vivo

Hiroshi Hirai et al.

MOLECULAR CANCER THERAPEUTICS (2010)

添加到收藏夹

Article Oncology

Akt1 and Akt2 Play Distinct Roles in the Initiation and Metastatic Phases of Mammary Tumor Progression

Rachelle L. Dillon et al.

CANCER RESEARCH (2009)

添加到收藏夹

Article Biochemistry & Molecular Biology

DEPTOR Is an mTOR Inhibitor Frequently Overexpressed in Multiple Myeloma Cells and Required for Their Survival

Timothy R. Peterson et al.

CELL (2009)

添加到收藏夹

Review Cell Biology

PIK3CA mutations in human solid tumors Role in sensitivity to various therapeutic approaches

Giovanni Ligresti et al.

CELL CYCLE (2009)

添加到收藏夹

Review Biochemistry & Molecular Biology

Emerging common themes in regulation of PIKKs and PI3Ks

Harri Lempiaeinen et al.

EMBO JOURNAL (2009)

添加到收藏夹

Review Multidisciplinary Sciences

The cancer genome

Michael R. Stratton et al.

NATURE (2009)

添加到收藏夹

Review Biotechnology & Applied Microbiology

Targeting the phosphoinositide 3-kinase pathway in cancer

Pixu Liu et al.

NATURE REVIEWS DRUG DISCOVERY (2009)

添加到收藏夹

Article Multidisciplinary Sciences

Rapamycin differentially inhibits S6Ks and 4E-BP1 to mediate cell-type-specific repression of mRNA translation

Andrew Y. Choo et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2008)

添加到收藏夹

Article Multidisciplinary Sciences

Helical domain and kinase domain mutations in p110α of phosphatidylinositol 3-kinase induce gain of function by different mechanisms

Li Zhao et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2008)

添加到收藏夹

Article Oncology

The phosphatidylinositol 3-kinase inhibitor, PX-866, is a potent inhibitor of cancer cell motility and growth in three-dimensional cultures

Amy L. Howes et al.

MOLECULAR CANCER THERAPEUTICS (2007)

添加到收藏夹

Article Biochemistry & Molecular Biology

Identification of Protor as a novel Rictor-binding component of mTOR complex-2

Laura R. Pearce et al.

BIOCHEMICAL JOURNAL (2007)

添加到收藏夹

Article Biochemistry & Molecular Biology

PRAS40 regulates mTORC1 kinase activity by functioning as a direct inhibitor of substrate binding

Lifu Wang et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2007)

添加到收藏夹

Article Biochemistry & Molecular Biology

mSin1 is necessary for Akt/PKB phosphorylation, and its isoforms define three distinct mTORC2s

Maria A. Frias et al.

CURRENT BIOLOGY (2006)

添加到收藏夹

Article Biochemistry & Molecular Biology

Prolonged rapamycin treatment inhibits mTORC2 assembly and Akt/PKB

DD Sarbassov et al.

MOLECULAR CELL (2006)

添加到收藏夹

Article Biochemistry & Molecular Biology

TopBP1 activates the ATR-ATRIP complex

A Kumagai et al.

CELL (2006)

添加到收藏夹

Review Biochemistry & Molecular Biology

TOR signaling in growth and metabolism

S Wullschleger et al.

CELL (2006)

添加到收藏夹

Review Biochemistry & Molecular Biology

TOR signaling in growth and metabolism

Stephan Wullschleger et al.

CELL (2006)

添加到收藏夹

Article Biochemistry & Molecular Biology

The role of SMG-1 in nonsense-mediated mRNA decay

A Yamashita et al.

BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS (2005)

添加到收藏夹

Article Biochemistry & Molecular Biology

Role of the PDK1-PKB-GSK3 pathway in regulating glycogen synthase and glucose uptake in the heart

A Mora et al.

FEBS LETTERS (2005)

添加到收藏夹

Article Multidisciplinary Sciences

Conserved modes of recruitment of ATM, ATR and DNA-PKcs to sites of DNA damage

J Falck et al.

NATURE (2005)

添加到收藏夹

Article Multidisciplinary Sciences

Phosphorylation and regulation of Akt/PKB by the rictor-mTOR complex

DD Sarbassov et al.

SCIENCE (2005)

添加到收藏夹

Article Biochemistry & Molecular Biology

Structure, regulation and function of PKB/AKT - a major therapeutic target

M Hanada et al.

BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS (2004)

添加到收藏夹

Article Biochemistry & Molecular Biology

SMG-1 is a phosphatidylinositol kinase-related protein kinase required for nonsense-mediated mRNA decay in Caenorhabditis elegans

A Grimson et al.

MOLECULAR AND CELLULAR BIOLOGY (2004)

添加到收藏夹

Review Cell Biology

Upstream and downstream of mTOR

N Hay et al.

GENES & DEVELOPMENT (2004)

添加到收藏夹

Article Biochemistry & Molecular Biology

Rictor, a novel binding partner of mTOR, defines a rapamycin-insensitive and raptor-independent pathway that regulates the cytoskeleton

DD Sarbassov et al.

CURRENT BIOLOGY (2004)

添加到收藏夹

Article Cell Biology

The TSC1-2 tumor suppressor controls insulin-PI3K signaling via regulation of IRS proteins

LS Harrington et al.

JOURNAL OF CELL BIOLOGY (2004)

添加到收藏夹

Article Multidisciplinary Sciences

Sensing DNA damage through ATRIP recognition of RPA-ssDNA complexes

L Zou et al.

SCIENCE (2003)

添加到收藏夹

Review Immunology

PI3K in lymphocyte development, differentiation and activation

K Okkenhaug et al.

NATURE REVIEWS IMMUNOLOGY (2003)

添加到收藏夹

Review Biochemistry & Molecular Biology

Structural insight into substrate specificity and regulatory mechanisms of phosphoinositide 3-kinases

S Djordjevic et al.

TRENDS IN BIOCHEMICAL SCIENCES (2002)

添加到收藏夹

Article Biochemistry & Molecular Biology

MTOR interacts with Raptor to form a nutrient-sensitive complex that signals to the cell growth machinery

DH Kim et al.

CELL (2002)

添加到收藏夹

Article Biochemistry & Molecular Biology

Akt enhances Mdm2-mediated ubiquitination and degradation of p53

Y Ogawara et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2002)

添加到收藏夹

Article Biochemistry & Molecular Biology

The essential cofactor TRRAP recruits the histone acetyltransferase hGCN5 to c-Myc

SB McMahon et al.

MOLECULAR AND CELLULAR BIOLOGY (2000)

添加到收藏夹

© Peeref 2019-2024. All rights reserved.