☆ 4.6 Review

The Importance of the Pyrazole Scaffold in the Design of Protein Kinases Inhibitors as Targeted Anticancer Therapies

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Article Oncology

FDA Approval Summary: Pralsetinib for the Treatment of Lung and Thyroid Cancers With RET Gene Mutations or Fusions

Janice Kim et al.

Summary: The FDA granted accelerated approval for pralsetinib for non-small cell lung cancer and thyroid cancer, based on substantial overall response rates and durable responses in patients with RET-altered tumors. However, the product label includes warnings and precautions for various adverse events and risks.

CLINICAL CANCER RESEARCH (2021)

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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)

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Review Biochemistry & Molecular Biology

Therapeutic Targeting of the Gas6/Axl Signaling Pathway in Cancer

Mai Tanaka et al.

Summary: Dysregulated signaling pathways in cancer cells and the tumor microenvironment, including the Axl and Gas6 pathways, have led to the development of therapeutic agents targeting the Gas6/Axl pathway. Promising results have been observed in both preclinical and clinical settings, indicating potential clinical efficacy of targeting Gas6 and Axl.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

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Review Oncology

Targeted therapy in advanced non-small cell lung cancer: current advances and future trends

Umair Majeed et al.

Summary: Lung cancer remains a leading cause of cancer mortality, with non-small cell lung cancer being the most common type. Targeted therapy can provide durable responses, and advances in molecular and immunohistochemical techniques allow for personalized medicine.

JOURNAL OF HEMATOLOGY & ONCOLOGY (2021)

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Review Oncology

Targeting Akt in cancer for precision therapy

Hui Hua et al.

Summary: Biomarkers-guided precision therapeutics has revolutionized the clinical development and administration of molecular-targeted anticancer agents. Tailored precision cancer therapy exhibits better response rate compared to unselective treatment. Protein kinases have critical roles in cell signaling, metabolism, proliferation, survival and migration. Aberrant activation of protein kinases is critical for tumor growth and progression. Consequently, protein kinases are key targets for molecular targeted cancer therapy. The serine/threonine kinase Akt is frequently activated in various types of cancer. Activation of Akt promotes tumor progression and drug resistance. Since the first Akt inhibitor was reported in 2000, many Akt inhibitors have been developed and evaluated in either early or late stage of clinical trials, which take advantage of liquid biopsy and genomic or molecular profiling to realize personalized cancer therapy. Two inhibitors, capivasertib and ipatasertib, are being tested in phase III clinical trials for cancer therapy. This article highlights recent progress of Akt signaling pathway, reviews the up-to-date data from clinical studies of Akt inhibitors and discusses the potential biomarkers that may help personalized treatment of cancer with Akt inhibitors. Additionally, it also discusses how Akt may confer the vulnerability of cancer cells to some kinds of anticancer agents.

JOURNAL OF HEMATOLOGY & ONCOLOGY (2021)

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Review Pharmacology & Pharmacy

Hydrophobic and polar interactions of FDA-approved small molecule protein kinase inhibitors with their target enzymes

Robert Roskoski

Summary: Dysregulation and mutations of protein kinases are involved in various diseases, making targeted inhibitors increasingly important for treatments. FDA-approved drugs mainly interact with kinase residues in the small lobe and hinge-linker region, with type IIA inhibitors having the most hydrophobic interactions with their targets. Further studies on protein kinase signaling pathways hold promise for biomedical breakthroughs.

PHARMACOLOGICAL RESEARCH (2021)

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Article Chemistry, Medicinal

Discovery of Potent, Selective Triazolothiadiazole-Containing c-Met Inhibitors

Qing Tang et al.

Summary: In this study, a novel series of highly potent and selective triazolothiadiazole c-Met inhibitors were developed, with compound 23 showing excellent kinase selectivity and dose-dependent antitumor efficacy in a SNU-5 gastric cancer xenograft model.

ACS MEDICINAL CHEMISTRY LETTERS (2021)

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Review Oncology

Untwining Anti-Tumor and Immunosuppressive Effects of JAK Inhibitors-A Strategy for Hematological Malignancies?

Klara Klein et al.

Summary: The JAK-STAT pathway is aberrantly activated in many cancers, and inhibition of this pathway via JAK inhibitors suppresses the immune system. This review article provides an overview of the effects of JAKinibs on immune cells in hematological malignancies and discusses their potential use in diseases where lymphocytes are the source of malignancy. A robust immune profiling is necessary to maximize the benefit for JAKinib-treated patients.

CANCERS (2021)

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Review Pharmacology & Pharmacy

Second-Generation Antimitotics in Cancer Clinical Trials

Pedro Novais et al.

Summary: Mitosis is a promising target for inhibiting cancer cell proliferation, with traditional antimitotics facing limitations such as resistance and toxicity. Second-generation antimitotics, targeting mitotic and SAC components, have attracted interest for overcoming these limitations. While many inhibitors have entered clinical trials, their efficacy as monotherapy is limited, leading to emerging interest in combination therapies.

PHARMACEUTICS (2021)

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Article Oncology

The L730V/I RET roof mutations display different activities toward pralsetinib and selpercatinib

Tao Shen et al.

Summary: Recently FDA-approved pralsetinib and selpercatinib are RET-selective protein tyrosine kinase inhibitors for treating RET-altered cancers. Selpercatinib was found to effectively inhibit certain resistant mutations that were strongly resistant to pralsetinib, showing better activity in those cases.

NPJ PRECISION ONCOLOGY (2021)

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Review Chemistry, Medicinal

Novel Receptor Tyrosine Kinase Pathway Inhibitors for Targeted Radionuclide Therapy of Glioblastoma

Julie Bolcaen et al.

Summary: Glioblastoma, a deadly brain tumor with high treatment resistance, has been explored with receptor tyrosine kinase inhibitors (RTKIs) to potentially improve prognosis and develop personalized targeted therapy. Approved RTKIs in clinics alongside radiopharmaceuticals in trials offer new avenues for theranostic applications in GB treatment.

PHARMACEUTICALS (2021)

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Review Biochemistry & Molecular Biology

The JAK/STAT signaling pathway: from bench to clinic

Xiaoyi Hu et al.

Summary: The JAK/STAT signaling pathway is a crucial cellular signal transduction pathway, associated with various cancers and autoimmune diseases. Researchers discussed the composition, activation, and regulation of this pathway, as well as its role in diseases.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2021)

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Review Chemistry, Multidisciplinary

Current progress, challenges and future prospects of indazoles as protein kinase inhibitors for the treatment of cancer

Nitin Tandon et al.

Summary: The indazole core is commonly used in medicinal chemistry, especially in the synthesis of kinase inhibitors. Indazole derivatives have been proven to be effective as specific kinase inhibitors and are utilized for targeted treatment of various cancers.

RSC ADVANCES (2021)

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Review Biochemistry & Molecular Biology

Small molecules in targeted cancer therapy: advances, challenges, and future perspectives

Lei Zhong et al.

Summary: Targeted therapeutic drugs have become mainstream cancer treatments due to their advantages in efficacy and safety, but still face challenges such as low response rate and drug resistance. A comprehensive review was conducted on small-molecule targeted anti-cancer drugs to promote their development, discussing current challenges and providing insights and perspectives for future research and development.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2021)

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Review Oncology

Oncogenic mechanism-based pharmaceutical validation of therapeutics targeting MET receptor tyrosine kinase

Hang-Ping Yao et al.

Summary: Aberrant expression and activation of the MET receptor tyrosine kinase contribute to cancer initiation and progression, making MET an attractive pharmaceutical target for oncological intervention. Over the past 20 years, various MET-targeting therapeutics have been intensively investigated with mixed outcomes, highlighting the importance of mechanism-based validation for selecting lead candidates for clinical trials and the need for new strategies to validate novel biotherapeutics.

THERAPEUTIC ADVANCES IN MEDICAL ONCOLOGY (2021)

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Review Oncology

Prexasertib, a checkpoint kinase inhibitor: from preclinical data to clinical development

Gesuino Angius et al.

CANCER CHEMOTHERAPY AND PHARMACOLOGY (2020)

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Article Oncology

A First-in-Human Phase I Study to Evaluate the ERK1/2 Inhibitor GDC-0994 in Patients with Advanced Solid Tumors

Andrea Varga et al.

CLINICAL CANCER RESEARCH (2020)

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Article Dermatology

Molecular and Cellular Responses to the TYK2/JAK1 Inhibitor PF-06700841 Reveal Reduction of Skin Inflammation in Plaque Psoriasis

Karen M. Page et al.

JOURNAL OF INVESTIGATIVE DERMATOLOGY (2020)

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Article Chemistry, Medicinal

Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent

Osamu Kurasawa et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

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Review Biochemistry & Molecular Biology

Revisiting the Structure and Chemistry of 3(5)-Substituted Pyrazoles

Alina Secrieru et al.

MOLECULES (2020)

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Article Biochemistry & Molecular Biology

Antitumor activity of crizotinib in lung cancers harboring a MET exon 14 alteration

Alexander Drilon et al.

NATURE MEDICINE (2020)

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Review Pharmacology & Pharmacy

The role of fibroblast growth factor receptor (FGFR) protein-tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2020)

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Review Cell Biology

The Function of the HGF/c-Met Axis in Hepatocellular Carcinoma

Haiyu Wang et al.

FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY (2020)

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Article Biochemistry & Molecular Biology

Insight into the Therapeutic Selectivity of the Irreversible EGFR Tyrosine Kinase Inhibitor Osimertinib through Enzyme Kinetic Studies

Xiang Zhai et al.

BIOCHEMISTRY (2020)

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Review Biochemistry & Molecular Biology

Overview of recent developments of pyrazole derivatives as an anticancer agent in different cell line

Fatima Ezzahra Bennani et al.

BIOORGANIC CHEMISTRY (2020)

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Review Chemistry, Medicinal

Janus kinases (JAKs): The efficient therapeutic targets for autoimmune diseases and myeloproliferative disorders

Pengfei Xu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

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Article Oncology

Phase II Study of AZD4547 in Patients With Tumors Harboring Aberrations in the FGFR Pathway: Results From the NCI-MATCH Trial (EAY131) Subprotocol W

Young K. Chae et al.

JOURNAL OF CLINICAL ONCOLOGY (2020)

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Article Chemistry, Medicinal

Bioisosteric Discovery of NPA101.3, a Second-Generation RET/VEGFR2 Inhibitor Optimized for Single-Agent Polypharmacology

Marialuisa Moccia et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

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Review Biotechnology & Applied Microbiology

MET Oncogene in Non-Small Cell Lung Cancer: Mechanism of MET Dysregulation and Agents Targeting the HGF/c-Met Axis

Hongge Liang et al.

ONCOTARGETS AND THERAPY (2020)

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Review Biochemistry & Molecular Biology

RAF kinase dimerization: implications for drug discovery and clinical outcomes

Tilman Brummer et al.

ONCOGENE (2020)

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Article Oncology

Phase II Multicenter, Open-Label Study of Oral ENMD-2076 for the Treatment of Patients with Advanced Fibrolamellar Carcinoma

Ghassan K. Abou-Alfa et al.

ONCOLOGIST (2020)

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Article Biochemistry & Molecular Biology

How ATP-Competitive Inhibitors Allosterically Modulate Tyrosine Kinases That Contain a Src-like Regulatory Architecture

Linglan Fang et al.

ACS CHEMICAL BIOLOGY (2020)

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Review Oncology

A BRAF new world

Daniele Frisone et al.

CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY (2020)

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Review Biochemistry & Molecular Biology

A review on progression of epidermal growth factor receptor (EGFR) inhibitors as an efficient approach in cancer targeted therapy

Adileh Ayati et al.

BIOORGANIC CHEMISTRY (2020)

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Article Biochemistry & Molecular Biology

Structural optimization of imidazothiazole derivatives affords a new promising series as B-Raf V600E inhibitors; synthesis, in vitro assay and in silico screening

Usama M. Ammar et al.

BIOORGANIC CHEMISTRY (2020)

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Review Pharmacology & Pharmacy

Emerging MET tyrosine kinase inhibitors for the treatment of non-small cell lung cancer

Toshio Fujino et al.

EXPERT OPINION ON EMERGING DRUGS (2020)

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Review Biochemistry & Molecular Biology

Bcr-Abl Tyrosine Kinase Inhibitors in the Treatment of Pediatric CML

Francesca Carofiglio et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)

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Article Oncology

Erdafitinib Antagonizes ABCB1-Mediated Multidrug Resistance in Cancer Cells

Weiguo Feng et al.

FRONTIERS IN ONCOLOGY (2020)

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Article Biochemistry & Molecular Biology

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

Colin Bournez et al.

MOLECULES (2020)

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Review Biochemistry & Molecular Biology

Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry

Chiara Brullo et al.

MOLECULES (2020)

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Article Oncology

Improving the odds of success in antitumoral drug development using scoring approaches towards heterocyclic scaffolds

George Nicolae Daniel Ion et al.

ONCOLOGY REPORTS (2020)

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Article Pharmacology & Pharmacy

Akt-targeted therapy as a promising strategy to overcome drug resistance in breast cancer – A comprehensive review from chemotherapy to immunotherapy

Parham Jabbarzadeh Kaboli et al.

PHARMACOLOGICAL RESEARCH (2020)

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Article Chemistry, Medicinal

Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands

Janina Niggenaber et al.

ACS MEDICINAL CHEMISTRY LETTERS (2020)

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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)

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Review Biochemistry & Molecular Biology

Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold

Daniel J. Baillache et al.

RSC MEDICINAL CHEMISTRY (2020)

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Review Oncology

Clinical Development of BRAF plus MEK Inhibitor Combinations

Vivek Subbiah et al.

TRENDS IN CANCER (2020)

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Article Chemistry, Multidisciplinary

Ultrasound-assisted synthesis and anticancer evaluation of new pyrazole derivatives as cell cycle inhibitors

George Mihai Nitulescu et al.

ARABIAN JOURNAL OF CHEMISTRY (2019)

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Review Pharmacology & Pharmacy

Properties of FDA-approved small molecule protein kinase inhibitors

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2019)

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Article Multidisciplinary Sciences

Defining a new nomenclature for the structures of active and inactive kinases

Vivek Modi et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2019)

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Review Pharmacology & Pharmacy

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

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2019)

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Article Oncology

ATP-Competitive Inhibitors Midostaurin and Avapritinib Have Distinct Resistance Profiles in Exon 17-Mutant KIT

Beth Apsel Winger et al.

CANCER RESEARCH (2019)

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Article Pharmacology & Pharmacy

Erdafitinib: First Global Approval

Anthony Markham

DRUGS (2019)

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Review Cell Biology

Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors

Shuyan Dai et al.

CELLS (2019)

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Article Chemistry, Medicinal

Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors

Gavin W. Collie et al.

ACS MEDICINAL CHEMISTRY LETTERS (2019)

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Review Oncology

Targeting Oncogenic BRAF: Past, Present, and Future

Aubhishek Zaman et al.

CANCERS (2019)

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Review Oncology

BRAF Mutations and the Utility of RAF and MEK Inhibitors in Primary Brain Tumors

Karisa C. Schreck et al.

CANCERS (2019)

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Review Oncology

BCR-ABL Independent Mechanisms of Resistance in Chronic Myeloid Leukemia

Federica Loscocco et al.

FRONTIERS IN ONCOLOGY (2019)

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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)

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Review Pharmacology & Pharmacy

Hepatocellular carcinoma: an update on investigational drugs in phase I and II clinical trials

Anne Noonan et al.

EXPERT OPINION ON INVESTIGATIONAL DRUGS (2019)

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Article Multidisciplinary Sciences

Exploration of the selective binding mechanism of protein kinase Aurora A selectivity via a comprehensive molecular modeling study

Zhe Zhang et al.

PEERJ (2019)

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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)

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Article Oncology

YH25448, an Irreversible EGFR-TKI with Potent Intracranial Activity in EGFR Mutant Non-Small Cell Lung Cancer

Jiyeon Yun et al.

CLINICAL CANCER RESEARCH (2019)

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Review Public, Environmental & Occupational Health

Safety and Tolerability of c-MET Inhibitors in Cancer

Alberto Puccini et al.

DRUG SAFETY (2019)

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Article Biochemistry & Molecular Biology

Design, synthesis, in vitro anticancer evaluation, kinase inhibitory effects, and pharmacokinetic profile of new 1,3,4-triarylpyrazole derivatives possessing terminal sulfonamide moiety

Mohammed S. Abdel-Maksoud et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2019)

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Review Pharmacology & Pharmacy

Cyclin-dependent protein serine/threonine kinase inhibitors as anticancer drugs

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2019)

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Article Chemistry, Medicinal

Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning

Mark E. Schnute et al.

ACS MEDICINAL CHEMISTRY LETTERS (2019)

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Review Chemistry, Multidisciplinary

Recent developments in synthetic chemistry and biological activities of pyrazole derivatives

Muhammad Faisal et al.

JOURNAL OF CHEMICAL SCIENCES (2019)

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Article Oncology

Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models

Jing Ai et al.

MOLECULAR CANCER THERAPEUTICS (2018)

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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)

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Article Chemistry, Medicinal

Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors

Haoliang Yuan et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

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Review Chemistry, Medicinal

Recent advances in the discovery of small molecule c-Met Kinase inhibitors

Palak K. Parikh et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

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Review Biochemistry & Molecular Biology

Kinase-targeted cancer therapies: progress, challenges and future directions

Khushwant S. Bhullar et al.

MOLECULAR CANCER (2018)

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Review Biochemistry & Molecular Biology

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

Khalid Karrouchi et al.

MOLECULES (2018)

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Article Oncology

Precision Targeted Therapy with BLU-667 for RET-Driven Cancers

Vivek Subbiah et al.

CANCER DISCOVERY (2018)

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Review Oncology

A comprehensive review of protein kinase inhibitors for cancer therapy

Radhamani Kannaiyan et al.

EXPERT REVIEW OF ANTICANCER THERAPY (2018)

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Review Cell Biology

The functional diversity of Aurora kinases: a comprehensive review

Estelle Willems et al.

CELL DIVISION (2018)

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Article Chemistry, Multidisciplinary

Nature and Hierarchy of Hydrogen-Bonding Interactions in Binary Complexes of Azoles with Water and Hydrogen Peroxide

Neha Chopra et al.

ACS OMEGA (2018)

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Article Hematology

Phase 1 dose-finding study of rebastinib (DCC-2036) in patients with relapsed chronic myeloid leukemia and acute myeloid leukemia

Jorge Cortes et al.

HAEMATOLOGICA (2017)

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Article Chemistry, Medicinal

Approved and Experimental Small-Molecule Oncology Kinase Inhibitor Drugs: A Mid-2016 Overview

Peter M. Fischer

MEDICINAL RESEARCH REVIEWS (2017)

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Article Oncology

A phase IIa study of afuresertib, an oral pan-AKT inhibitor, in patients with Langerhans cell histiocytosis

Robert J. Arceci et al.

PEDIATRIC BLOOD & CANCER (2017)

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Article Hematology

Phase 1 dose-finding study of rebastinib (DCC-2036) in patients with relapsed chronic myeloid leukemia and acute myeloid leukemia

Jorge Cortes et al.

HAEMATOLOGICA (2017)

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Article Chemistry, Medicinal

Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor

Lyamin Z. Bendjeddou et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2017)

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Review Oncology

Syk inhibitors in clinical development for hematological malignancies

Delong Liu et al.

JOURNAL OF HEMATOLOGY & ONCOLOGY (2017)

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Article Chemistry, Medicinal

Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR

Simon Planken et al.

JOURNAL OF MEDICINAL CHEMISTRY (2017)

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Article Oncology

A phase 1 study of the Janus kinase 2 (JAK2)V617F inhibitor, gandotinib (LY2784544), in patients with primary myelofibrosis, polycythemia vera, and essential thrombocythemia

Srdan Verstovsek et al.

LEUKEMIA RESEARCH (2017)

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Article Oncology

Discovery and Pharmacological Characterization of JNJ-42756493 (Erdafitinib), a Functionally Selective Small-Molecule FGFR Family Inhibitor

Timothy P. S. Perera et al.

MOLECULAR CANCER THERAPEUTICS (2017)

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Article Biochemistry & Molecular Biology

Assessing Scaffold Diversity of Kinase Inhibitors Using Alternative Scaffold Concepts and Estimating the Scaffold Hopping Potential for Different Kinases

Dilyana Dimova et al.

MOLECULES (2017)

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Article Oncology

A Phase 1 Study of LY2874455, an Oral Selective pan-FGFR Inhibitor, in Patients with Advanced Cancer

Michael Michael et al.

TARGETED ONCOLOGY (2017)

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Review Oncology

Aurora kinases: novel therapy targets in cancers

Anqun Tang et al.

ONCOTARGET (2017)

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Article Biochemistry & Molecular Biology

2-Aminomethylthieno[3,2-d]pyrimidin-4(3H)-ones bearing 3-methylpyrazole hinge binding moiety: Highly potent, selective, and time -dependent inhibitors of Cdc7 kinase

Osamu Kurasawa et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2017)

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Article Chemistry, Medicinal

Recent progress towards clinically relevant ATP-competitive Akt inhibitors

Bayard R. Huck et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2017)

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Article Hematology

Merestinib blocks Mnk kinase activity in acute myeloid leukemia progenitors and exhibits antileukemic effects in vitro and in vivo

Ewa M. Kosciuczuk et al.

BLOOD (2016)

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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)

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Review Biochemical Research Methods

Cell signaling regulation by protein phosphorylation: a multivariate, heterogeneous, and context-dependent process

Evan K. Day et al.

CURRENT OPINION IN BIOTECHNOLOGY (2016)

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Review Pharmacology & Pharmacy

MET INHIBITION AND MERESTINIB (LY-2801653) FOR CANCER TREATMENT

P. A. Prins et al.

DRUGS OF THE FUTURE (2016)

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Article Chemistry, Medicinal

Design, synthesis, broad-spectrum antiproliferative activity, and kinase inhibitory effect of triarylpyrazole derivatives possessing arylamides or arylureas moieties

Mahmoud M. Gamal El-Din et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2016)

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Article Biochemistry & Molecular Biology

Design, synthesis, and in vitro antiproliferative and kinase inhibitory effects of pyrimidinylpyrazole derivatives terminating with arylsulfonamido or cyclic sulfamide substituents

Mahmoud M. Gamal El-Din et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2016)

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Article Chemistry, Medicinal

Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development

James F. Blake et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

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Article Chemistry, Multidisciplinary

How a Kinase Inhibitor Withstands Gatekeeper Residue Mutations

Jagannath Mondal et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2016)

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Review Oncology

cMET Exon 14 Skipping: From the Structure to the Clinic

Nele Van der Steen et al.

JOURNAL OF THORACIC ONCOLOGY (2016)

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Review Pharmacology & Pharmacy

Classification of small molecule protein kinase inhibitors based upon the structures of their drug-enzyme complexes

Robert Roskoski

PHARMACOLOGICAL RESEARCH (2016)

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Review Pharmacology & Pharmacy

Pyrazolo[3,4-d]pyrimidine based scaffold derivatives targeting kinases as anticancer agents

Nasser S. M. Ismail et al.

FUTURE JOURNAL OF PHARMACEUTICAL SCIENCES (2016)

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Meeting Abstract Oncology

Anti-tumor activity of TAK-659, a dual inhibitor of SYK and FLT-3 kinases, in AML models

Jie Yu et al.

JOURNAL OF CLINICAL ONCOLOGY (2016)

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Article Oncology

The MET Inhibitor AZD6094 (Savolitinib, HMPL-504) Induces Regression in Papillary Renal Cell Carcinoma Patient-Derived Xenograft Models

Alwin G. Schuller et al.

CLINICAL CANCER RESEARCH (2015)

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Review Pharmacology & Pharmacy

Privileged scaffolds in lead generation

Hongyu Zhao et al.

EXPERT OPINION ON DRUG DISCOVERY (2015)

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Article Oncology

LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms

Constance King et al.

MOLECULAR CANCER THERAPEUTICS (2015)

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Article Oncology

Volitinib, a potent and highly selective c-Met inhibitor, effectively blocks c-Met signaling and growth in c-MET amplified gastric cancer patient-derived tumor xenograft models

Paul R. Gavine et al.

MOLECULAR ONCOLOGY (2015)

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Meeting Abstract Hematology

Blu-285, a Potent and Selective Inhibitor for Hematologic Malignancies with KIT Exon 17 Mutations

Erica Evans et al.

BLOOD (2015)

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Article Oncology

Dramatic Antitumor Effects of the Dual MET/RON Small-Molecule Inhibitor LY2801653 in Non-Small Cell Lung Cancer

Ichiro Kawada et al.

CANCER RESEARCH (2014)

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Article Oncology

Abstract 971: Synergistic effect of c-Met inhibitor volitinib in combination with EGFR inhibitor Gefitnib on EGFR-TKI resistant NSCLC model HCC827C4R harboring acquiredMetgene amplification.

Feng Zhou et al.

CANCER RESEARCH (2014)

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Meeting Abstract Oncology

Preclinical evaluation of LY2801653, an orally bioavailable small molecule oncokinase inhibitor, in cholangiocarcinoma models

Sau-Chi Betty Yan et al.

CANCER RESEARCH (2014)

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Review Immunology

Protein kinase inhibitors in the treatment of inflammatory and autoimmune diseases

H. Patterson et al.

CLINICAL AND EXPERIMENTAL IMMUNOLOGY (2014)

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Meeting Abstract Oncology

Using modelling & simulation to integrate mouse PK-PD-efficacy with preliminary human PK data to inform the Phase II doses and schedule for the experimental c-Met inhibitor AZD6094 (Volitinib)

R. Jones et al.

EUROPEAN JOURNAL OF CANCER (2014)

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Article Chemistry, Medicinal

KLIFS: A Knowledge-Based Structural Database To Navigate Kinase-Ligand Interaction Space

Oscar P. J. van Linden et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

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Article Chemistry, Medicinal

Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal-Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer

Hong Jia et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

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Article Oncology

Characterization of the Activity of the PI3K/mTOR Inhibitor XL765 (SAR245409) in Tumor Models with Diverse Genetic Alterations Affecting the PI3K Pathway

Peiwen Yu et al.

MOLECULAR CANCER THERAPEUTICS (2014)

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Article Oncology

The Fibroblast Growth Factor Receptor Genetic Status as a Potential Predictor of the Sensitivity to CH5183284/Debio 1347, a Novel Selective FGFR Inhibitor

Yoshito Nakanishi et al.

MOLECULAR CANCER THERAPEUTICS (2014)

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Article Multidisciplinary Sciences

Discovery of Novel AKT Inhibitors with Enhanced Anti-Tumor Effects in Combination with the MEK Inhibitor

Melissa Dumble et al.

PLOS ONE (2014)

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Article Oncology

Effect of NS-018, a selective JAK2V617F inhibitor, in a murine model of myelofibrosis

Y. Nakaya et al.

BLOOD CANCER JOURNAL (2014)

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Meeting Abstract Oncology

First-in-human phase I study of a selective c-Met inhibitor volitinib (HMP504/AZD6094) in patients with advanced solid tumors

Hui Kong Gan et al.

JOURNAL OF CLINICAL ONCOLOGY (2014)

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Article Biochemistry & Molecular Biology

New Potential Antitumor Pyrazole Derivatives: Synthesis and Cytotoxic Evaluation

George Mihai Nitulescu et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2013)

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Article Oncology

LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models

S. Betty Yan et al.

INVESTIGATIONAL NEW DRUGS (2013)

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Article Oncology

Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F

L. Ma et al.

BLOOD CANCER JOURNAL (2013)

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Article Chemistry, Medicinal

Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families

Michael L. Curtin et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2012)

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Article Oncology

Phase I study of the Aurora B kinase inhibitor barasertib (AZD1152) to assess the pharmacokinetics, metabolism and excretion in patients with acute myeloid leukemia

Mike Dennis et al.

CANCER CHEMOTHERAPY AND PHARMACOLOGY (2012)

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Article Chemistry, Medicinal

Discovery of a Novel Class of Exquisitely Selective Mesenchymal-Epithelial Transition Factor (c-MET) Protein Kinase Inhibitors and Identification of the Clinical Candidate 2-(4-(1-(Quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the Treatment of Cancer

J. Jean Cui et al.

JOURNAL OF MEDICINAL CHEMISTRY (2012)

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Article Oncology

Conformational Control Inhibition of the BCR-ABL1 Tyrosine Kinase, Including the Gatekeeper T315I Mutant, by the Switch-Control Inhibitor DCC-2036

Wayne W. Chan et al.

CANCER CELL (2011)

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A novel and selective c-Met inhibitor against subcutaneous xenograft and othotopic brain tumor models

Yumin Cui et al.

CANCER RESEARCH (2011)

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Article Chemistry, Medicinal

Structure Based Drug Design of Crizotinib (PF-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal-Epithelial Transition Factor (c-MET) Kinase and Anaplastic Lymphoma Kinase (ALK)

J. Jean Cui et al.

JOURNAL OF MEDICINAL CHEMISTRY (2011)

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Article Oncology

ENMD-2076 Is an Orally Active Kinase Inhibitor with Antiangiogenic and Antiproliferative Mechanisms of Action

Graham C. Fletcher et al.

MOLECULAR CANCER THERAPEUTICS (2011)

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Review Biochemistry & Molecular Biology

RAF protein-serine/threonine kinases: Structure and regulation

Robert Roskoski

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2010)

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Article Biochemistry & Molecular Biology

Crystal structure of an Aurora-A mutant that mimics Aurora-B bound to MLN8054: insights into selectivity and drug design

Charlotte A. Dodson et al.

BIOCHEMICAL JOURNAL (2010)

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Article Biochemistry & Molecular Biology

Defining the conserved internal architecture of a protein kinase

Alexandr P. Kornev et al.

BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS (2010)

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Article Hematology

Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms

Alfonso Quintas-Cardama et al.

BLOOD (2010)

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Targeting Cell Division Cycle 7 Kinase: A New Approach for Cancer Therapy

Alessia Montagnoli et al.

CLINICAL CANCER RESEARCH (2010)

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Article Biochemistry & Molecular Biology

cAMP-dependent protein kinase: Crystallographic insights into substrate recognition and phosphotransfer

Madhusudan et al.

PROTEIN SCIENCE (2010)

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Article Chemistry, Medicinal

The discovery of the potent aurora inhibitor MK-0457 (VX-680)

David Bebbington et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)

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Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity

Steven Howard et al.

JOURNAL OF MEDICINAL CHEMISTRY (2009)

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Article Biochemistry & Molecular Biology

Targeting phosphoinositide 3-kinase - Moving towards therapy

Romina Marone et al.

BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS (2008)

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Article Biochemistry & Molecular Biology

Modulation of kinase-inhibitor interactions by auxiliary protein binding: Crystallography studies on Aurora A interactions with VX-680 and with TPX2

Baoguang Zhao et al.

PROTEIN SCIENCE (2008)

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Article Chemistry, Medicinal

Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase

Andrew A. Mortlock et al.

JOURNAL OF MEDICINAL CHEMISTRY (2007)

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Article Multidisciplinary Sciences

The gatekeeper residue controls autoactivation of ERK2 via a pathway of intramolecular connectivity

Michelle A. Emrick et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2006)

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Article Chemistry, Medicinal

Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: Synthesis and SAR studies

Xiaodong Lin et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2006)

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Article Chemistry, Medicinal

Are target-family-privileged substructures truly privileged?

DM Schnur et al.

JOURNAL OF MEDICINAL CHEMISTRY (2006)

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A single amino-acid change in ERK1/2 makes the enzyme susceptible to PP1 derivatives

S Endo et al.

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2006)

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Article Biochemistry & Molecular Biology

Crystal structures of proto-oncogene kinase pim1: A target of aberrant somatic hypermutations in diffuse large cell lymphoma

A Kumar et al.

JOURNAL OF MOLECULAR BIOLOGY (2005)

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Review Oncology

Mechanisms of BCR-ABL in the pathogenesis of chronic myelogenous leukaemia

R Ren

NATURE REVIEWS CANCER (2005)

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Article Chemistry, Medicinal

Structure-activity relationships of the p38α MAP kinase inhibitor 1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea (BIRB 796)

J Regan et al.

JOURNAL OF MEDICINAL CHEMISTRY (2003)

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Identification of novel ERK2 substrates through use of an engineered kinase and ATP analogs

ST Eblen et al.

JOURNAL OF BIOLOGICAL CHEMISTRY (2003)

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