Related references
Note: Only part of the references are listed.A recent update on small-molecule kinase inhibitors for targeted cancer therapy and their therapeutic insights from mass spectrometry-based proteomic analysis
Pey Yee Lee et al.
FEBS JOURNAL (2023)
Discovery of octahydropyrrolo [3,2-b] pyridin derivative as a highly selective Type I inhibitor of FGFR3 over VEGFR2 by high-throughput virtual screening
Xin Wang et al.
JOURNAL OF CELLULAR BIOCHEMISTRY (2023)
Properties of FDA-approved small molecule protein kinase inhibitors: A 2023 update
Robert Roskoski Jr
PHARMACOLOGICAL RESEARCH (2023)
Fluorine-containing drugs approved by the FDA in 2021
Jingrui He et al.
CHINESE CHEMICAL LETTERS (2023)
New insights about the PDGF/PDGFR signaling pathway as a promising target to develop cancer therapeutic strategies
Pratibha Pandey et al.
BIOMEDICINE & PHARMACOTHERAPY (2023)
Pirtobrutinib: First Approval
Susan J. J. Keam
DRUGS (2023)
Amino-Pyrazoles in Medicinal Chemistry: A Review
Matteo Lusardi et al.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2023)
Development and Therapeutic Implications of Tyrosine Kinase 2 Inhibitors
Kuojun Zhang et al.
JOURNAL OF MEDICINAL CHEMISTRY (2023)
Aurora B Inhibitors as Cancer Therapeutics
Antal H. Kovacs et al.
MOLECULES (2023)
Ruxolitinib Cream 1.5%: A Review in Mild to Moderate Atopic Dermatitis
Sheridan M. Hoy
AMERICAN JOURNAL OF CLINICAL DERMATOLOGY (2023)
Synthesis and biological evaluation of novel aromatic amide derivatives as potential BCR-ABL inhibitors
Xiujun Wang et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2023)
Current scenario of pyrazole hybrids with in vivo therapeutic potential against cancers
Zhi Xu et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2023)
Janus kinase 1 inhibitor INCB054707 for patients with moderate-to-severe hidradenitis suppurativa: results from two phase II studies
Afsaneh Alavi et al.
BRITISH JOURNAL OF DERMATOLOGY (2022)
Momelotinib: an emerging treatment for myelofibrosis patients with anemia
Helen T. Chifotides et al.
JOURNAL OF HEMATOLOGY & ONCOLOGY (2022)
Small Molecule Kinase Inhibitor Drugs (1995-2021): Medical Indication, Pharmacology, and Synthesis
Cecilia C. Ayala-Aguilera et al.
JOURNAL OF MEDICINAL CHEMISTRY (2022)
Evaluation of Substituted Pyrazole-Based Kinase Inhibitors in One Decade (2011-2020): Current Status and Future Prospects
Mohammed I. El-Gamal et al.
MOLECULES (2022)
Assessment of Effects of Investigational TAK-931, an Oral Cell Division Cycle 7 Kinase Inhibitor on the QTc Intervals in Patients With Advanced Solid Tumors
Xiaofei Zhou et al.
CLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT (2022)
BCR-ABL1 Tyrosine Kinase Complex Signaling Transduction: Challenges to Overcome Resistance in Chronic Myeloid Leukemia
Gustavo P. Amarante-Mendes et al.
PHARMACEUTICS (2022)
Recent Progress in Anticancer Agents Incorporating Pyrazole Scaffold
Satbir Mor et al.
MINI-REVIEWS IN MEDICINAL CHEMISTRY (2022)
A kinase inhibitor which specifically targets the ABL myristate pocket (STAMP), but unlike asciminib crosses the blood-brain barrier
Paul W. Manley et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2022)
Recent advances in B-RAF inhibitors as anticancer agents
Pathan Shahebaaz Khan et al.
BIOORGANIC CHEMISTRY (2022)
Development of asciminib, a novel allosteric inhibitor of BCR-ABL1
Delphine Rea et al.
CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY (2022)
JAK inhibitors in crohn's disease: ready to go?
Cecilia Dell'Avalle et al.
EXPERT OPINION ON INVESTIGATIONAL DRUGS (2022)
The Dawn of Allosteric BCR-ABL1 Drugs: From a Phenotypic Screening Hit to an Approved Drug
Mingxing Teng et al.
JOURNAL OF MEDICINAL CHEMISTRY (2022)
Quantitative and Qualitative Analysis of the Anti-Proliferative Potential of the Pyrazole Scaffold in the Design of Anticancer Agents
George Mihai Nitulescu
MOLECULES (2022)
Targeting BCR-Abl in the treatment of Philadelphia-chromosome positive chronic myelogenous leukemia
Robert Roskoski
PHARMACOLOGICAL RESEARCH (2022)
Molecular docking/dynamic simulations, MEP, ADME-TOX-based analysis of xanthone derivatives as CHK1 inhibitors
Ahlem Belkadi et al.
STRUCTURAL CHEMISTRY (2022)
Pirtobrutinib inhibits wild-type and mutant Bruton's tyrosine kinase-mediated signaling in chronic lymphocytic leukemia
Burcu Aslan et al.
BLOOD CANCER JOURNAL (2022)
Signaling Pathway and Small-Molecule Drug Discovery of FGFR: A Comprehensive Review
Jia Zheng et al.
FRONTIERS IN CHEMISTRY (2022)
A Comprehensive Overview of Globally Approved JAK Inhibitors
Ahmed M. Shawky et al.
PHARMACEUTICS (2022)
A Review of the Recent Development in the Synthesis and Biological Evaluations of Pyrazole Derivatives
Oluwakemi Ebenezer et al.
BIOMEDICINES (2022)
Development of pyrazolo[3,4-d]pyrimidin-4-one scaffold as novel CDK2 inhibitors: Design, synthesis, and biological evaluation
Fan Xie et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2022)
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML
You-lu Pan et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)
Foretinib can overcome common on-target resistance mutations after capmatinib/tepotinib treatment in NSCLCs with MET exon 14 skipping mutation
Toshio Fujino et al.
JOURNAL OF HEMATOLOGY & ONCOLOGY (2022)
Beyond Crizotinib: A Systematic Review and Meta-Analysis of the Next-Generation ALK Inhibitors as First-Line Treatment for ALK-Translocated Lung Cancer
Emilio Francesco Giunta et al.
FRONTIERS IN ONCOLOGY (2022)
The Latest FDA-Approved Pharmaceuticals Containing Fragments of Tailor-Made Amino Acids and Fluorine
Qian Wang et al.
PHARMACEUTICALS (2022)
AT9283, 1-Cyclopropyl-3-(3-(5-(Morpholinomethyl)-1H-Benzo[d] Imidazole-2-yl)-1H-Pyrazol-4-yl) Urea, Inhibits Syk to Suppress Mast Cell-Mediated Allergic Response
Su Jeong Kim et al.
BIOMOLECULES & THERAPEUTICS (2022)
Novel Therapies for Unmet Clinical Needs in Myelodysplastic Syndromes
Giulio Cassanello et al.
CANCERS (2022)
Safety, Tolerability, and Pharmacokinetics of TAK-931, a Cell Division Cycle 7 Inhibitor, in Patients with Advanced Solid Tumors: A Phase I First-in-Human Study
Yasutoshi Kuboki et al.
CANCER RESEARCH COMMUNICATIONS (2022)
Encorafenib plus cetuximab for the treatment of BRAF-V600E-mutated metastatic colorectal cancer
Javierd Ros et al.
THERAPEUTIC ADVANCES IN GASTROENTEROLOGY (2022)
Lazertinib: on the Way to Its Throne
Jiyun Lee et al.
YONSEI MEDICAL JOURNAL (2022)
Spotlight on Tepotinib and Capmatinib for Non-Small Cell Lung Cancer with MET Exon 14 Skipping Mutation
Danielle Brazel et al.
LUNG CANCER-TARGETS AND THERAPY (2022)
New Directions and Challenges in Targeted Therapies of Advanced Bladder Cancer: The Role of FGFR Inhibitors
Katarzyna Szklener et al.
CANCERS (2022)
Insights into the modular design of kinase inhibitors and application to Abl and Axl
Sameer Phadke et al.
RSC MEDICINAL CHEMISTRY (2022)
A provider's guide to primary myelofibrosis: pathophysiology, diagnosis, and management
Benjamin Garmezy et al.
BLOOD REVIEWS (2021)
Recent advances in Bcr-Abl tyrosine kinase inhibitors for overriding T315I mutation
Juan Liu et al.
CHEMICAL BIOLOGY & DRUG DESIGN (2021)
Preclinical Comparison of the Blood-brain barrier Permeability of Osimertinib with Other EGFR TKIs
Nicola Colclough et al.
CLINICAL CANCER RESEARCH (2021)
Beyond Osimertinib: The Development of Third-Generation EGFR Tyrosine Kinase Inhibitors For Advanced EGFR plus NSCLC
Misako Nagasaka et al.
JOURNAL OF THORACIC ONCOLOGY (2021)
Indazole scaffold: a generalist for marketed and clinical drugs
Yaquan Cao et al.
MEDICINAL CHEMISTRY RESEARCH (2021)
Kinase Inhibitor Scaffold Hopping with Deep Learning Approaches
Lizhao Hu et al.
JOURNAL OF CHEMICAL INFORMATION AND MODELING (2021)
Structural basis of acquired resistance to selpercatinib and pralsetinib mediated by non-gatekeeper RET mutations
V Subbiah et al.
ANNALS OF ONCOLOGY (2021)
Globally Approved EGFR Inhibitors: Insights into Their Syntheses, Target Kinases, Biological Activities, Receptor Interactions, and Metabolism
Mohammed A. S. Abourehab et al.
MOLECULES (2021)
Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof
Ryan R. Davis et al.
JOURNAL OF MEDICINAL CHEMISTRY (2021)
Second-Generation Jak2 Inhibitors for Advanced Prostate Cancer: Are We Ready for Clinical Development?
Paul Beinhoff et al.
CANCERS (2021)
Baricitinib: From Rheumatoid Arthritis to COVID-19
Sara Assadiasl et al.
JOURNAL OF CLINICAL PHARMACOLOGY (2021)
Targeting Phosphatases and Kinases: How to Checkmate Cancer
Alice Turdo et al.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY (2021)
The Fellowship of Privileged Scaffolds-One Structure to Inhibit Them All
Marcin Skorenski et al.
PHARMACEUTICALS (2021)
Aurora Kinase B Inhibition: A Potential Therapeutic Strategy for Cancer
Naheed Arfin Borah et al.
MOLECULES (2021)
AKT Inhibitors: New Weapons in the Fight Against Breast Cancer?
Federica Martorana et al.
FRONTIERS IN PHARMACOLOGY (2021)
Heterocyclic Compounds: Pharmacology of Pyrazole Analogs From Rational Structural Considerations
Rafael Fernades Costa et al.
FRONTIERS IN PHARMACOLOGY (2021)
BIRB796, an Inhibitor of p38 Mitogen-Activated Protein Kinase, Inhibits Proliferation and Invasion in Glioblastoma Cells
Linyao Zhao et al.
ACS OMEGA (2021)
Future prospects for mitosis-targeted antitumor therapies
Alfonso Serrano-del Valle et al.
BIOCHEMICAL PHARMACOLOGY (2021)
FDA Approval Summary: Pralsetinib for the Treatment of Lung and Thyroid Cancers With RET Gene Mutations or Fusions
Janice Kim et al.
CLINICAL CANCER RESEARCH (2021)
Lazertinib: First Approval
Sohita Dhillon
DRUGS (2021)
Therapeutic Targeting of the Gas6/Axl Signaling Pathway in Cancer
Mai Tanaka et al.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)
Targeted therapy in advanced non-small cell lung cancer: current advances and future trends
Umair Majeed et al.
JOURNAL OF HEMATOLOGY & ONCOLOGY (2021)
Targeting Akt in cancer for precision therapy
Hui Hua et al.
JOURNAL OF HEMATOLOGY & ONCOLOGY (2021)
Hydrophobic and polar interactions of FDA-approved small molecule protein kinase inhibitors with their target enzymes
Robert Roskoski
PHARMACOLOGICAL RESEARCH (2021)
Discovery of Potent, Selective Triazolothiadiazole-Containing c-Met Inhibitors
Qing Tang et al.
ACS MEDICINAL CHEMISTRY LETTERS (2021)
Untwining Anti-Tumor and Immunosuppressive Effects of JAK Inhibitors-A Strategy for Hematological Malignancies?
Klara Klein et al.
CANCERS (2021)
Second-Generation Antimitotics in Cancer Clinical Trials
Pedro Novais et al.
PHARMACEUTICS (2021)
The L730V/I RET roof mutations display different activities toward pralsetinib and selpercatinib
Tao Shen et al.
NPJ PRECISION ONCOLOGY (2021)
Novel Receptor Tyrosine Kinase Pathway Inhibitors for Targeted Radionuclide Therapy of Glioblastoma
Julie Bolcaen et al.
PHARMACEUTICALS (2021)
The JAK/STAT signaling pathway: from bench to clinic
Xiaoyi Hu et al.
SIGNAL TRANSDUCTION AND TARGETED THERAPY (2021)
Current progress, challenges and future prospects of indazoles as protein kinase inhibitors for the treatment of cancer
Nitin Tandon et al.
RSC ADVANCES (2021)
Small molecules in targeted cancer therapy: advances, challenges, and future perspectives
Lei Zhong et al.
SIGNAL TRANSDUCTION AND TARGETED THERAPY (2021)
Oncogenic mechanism-based pharmaceutical validation of therapeutics targeting MET receptor tyrosine kinase
Hang-Ping Yao et al.
THERAPEUTIC ADVANCES IN MEDICAL ONCOLOGY (2021)
Prexasertib, a checkpoint kinase inhibitor: from preclinical data to clinical development
Gesuino Angius et al.
CANCER CHEMOTHERAPY AND PHARMACOLOGY (2020)
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)
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)
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)
Revisiting the Structure and Chemistry of 3(5)-Substituted Pyrazoles
Alina Secrieru et al.
MOLECULES (2020)
Antitumor activity of crizotinib in lung cancers harboring a MET exon 14 alteration
Alexander Drilon et al.
NATURE MEDICINE (2020)
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)
The Function of the HGF/c-Met Axis in Hepatocellular Carcinoma
Haiyu Wang et al.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY (2020)
Insight into the Therapeutic Selectivity of the Irreversible EGFR Tyrosine Kinase Inhibitor Osimertinib through Enzyme Kinetic Studies
Xiang Zhai et al.
BIOCHEMISTRY (2020)
Overview of recent developments of pyrazole derivatives as an anticancer agent in different cell line
Fatima Ezzahra Bennani et al.
BIOORGANIC CHEMISTRY (2020)
Janus kinases (JAKs): The efficient therapeutic targets for autoimmune diseases and myeloproliferative disorders
Pengfei Xu et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)
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)
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)
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)
RAF kinase dimerization: implications for drug discovery and clinical outcomes
Tilman Brummer et al.
ONCOGENE (2020)
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)
How ATP-Competitive Inhibitors Allosterically Modulate Tyrosine Kinases That Contain a Src-like Regulatory Architecture
Linglan Fang et al.
ACS CHEMICAL BIOLOGY (2020)
A BRAF new world
Daniele Frisone et al.
CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY (2020)
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)
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)
Emerging MET tyrosine kinase inhibitors for the treatment of non-small cell lung cancer
Toshio Fujino et al.
EXPERT OPINION ON EMERGING DRUGS (2020)
Bcr-Abl Tyrosine Kinase Inhibitors in the Treatment of Pediatric CML
Francesca Carofiglio et al.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)
Erdafitinib Antagonizes ABCB1-Mediated Multidrug Resistance in Cancer Cells
Weiguo Feng et al.
FRONTIERS IN ONCOLOGY (2020)
Comparative Assessment of Protein Kinase Inhibitors in Public Databases and in PKIDB
Colin Bournez et al.
MOLECULES (2020)
Pyrazolyl-Ureas as Interesting Scaffold in Medicinal Chemistry
Chiara Brullo et al.
MOLECULES (2020)
Improving the odds of success in antitumoral drug development using scoring approaches towards heterocyclic scaffolds
George Nicolae Daniel Ion et al.
ONCOLOGY REPORTS (2020)
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)
Complex Crystal Structures of EGFR with Third-Generation Kinase Inhibitors and Simultaneously Bound Allosteric Ligands
Janina Niggenaber et al.
ACS MEDICINAL CHEMISTRY LETTERS (2020)
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)
Recent developments in anticancer kinase inhibitors based on the pyrazolo[3,4-d]pyrimidine scaffold
Daniel J. Baillache et al.
RSC MEDICINAL CHEMISTRY (2020)
Clinical Development of BRAF plus MEK Inhibitor Combinations
Vivek Subbiah et al.
TRENDS IN CANCER (2020)
Ultrasound-assisted synthesis and anticancer evaluation of new pyrazole derivatives as cell cycle inhibitors
George Mihai Nitulescu et al.
ARABIAN JOURNAL OF CHEMISTRY (2019)
Properties of FDA-approved small molecule protein kinase inhibitors
Robert Roskoski
PHARMACOLOGICAL RESEARCH (2019)
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)
Targeting ERK1/2 protein-serine/threonine kinases in human cancers
Robert Roskoski
PHARMACOLOGICAL RESEARCH (2019)
ATP-Competitive Inhibitors Midostaurin and Avapritinib Have Distinct Resistance Profiles in Exon 17-Mutant KIT
Beth Apsel Winger et al.
CANCER RESEARCH (2019)
Fibroblast Growth Factor Receptors (FGFRs): Structures and Small Molecule Inhibitors
Shuyan Dai et al.
CELLS (2019)
Structural and Molecular Insight into Resistance Mechanisms of First Generation cMET Inhibitors
Gavin W. Collie et al.
ACS MEDICINAL CHEMISTRY LETTERS (2019)
Targeting Oncogenic BRAF: Past, Present, and Future
Aubhishek Zaman et al.
CANCERS (2019)
BRAF Mutations and the Utility of RAF and MEK Inhibitors in Primary Brain Tumors
Karisa C. Schreck et al.
CANCERS (2019)
BCR-ABL Independent Mechanisms of Resistance in Chronic Myeloid Leukemia
Federica Loscocco et al.
FRONTIERS IN ONCOLOGY (2019)
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)
Hepatocellular carcinoma: an update on investigational drugs in phase I and II clinical trials
Anne Noonan et al.
EXPERT OPINION ON INVESTIGATIONAL DRUGS (2019)
Exploration of the selective binding mechanism of protein kinase Aurora A selectivity via a comprehensive molecular modeling study
Zhe Zhang et al.
PEERJ (2019)
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)
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)
Safety and Tolerability of c-MET Inhibitors in Cancer
Alberto Puccini et al.
DRUG SAFETY (2019)
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)
Cyclin-dependent protein serine/threonine kinase inhibitors as anticancer drugs
Robert Roskoski
PHARMACOLOGICAL RESEARCH (2019)
Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning
Mark E. Schnute et al.
ACS MEDICINAL CHEMISTRY LETTERS (2019)
Recent developments in synthetic chemistry and biological activities of pyrazole derivatives
Muhammad Faisal et al.
JOURNAL OF CHEMICAL SCIENCES (2019)
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)
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)
Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors
Haoliang Yuan et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)
Recent advances in the discovery of small molecule c-Met Kinase inhibitors
Palak K. Parikh et al.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)
Kinase-targeted cancer therapies: progress, challenges and future directions
Khushwant S. Bhullar et al.
MOLECULAR CANCER (2018)
Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review
Khalid Karrouchi et al.
MOLECULES (2018)
Precision Targeted Therapy with BLU-667 for RET-Driven Cancers
Vivek Subbiah et al.
CANCER DISCOVERY (2018)
A comprehensive review of protein kinase inhibitors for cancer therapy
Radhamani Kannaiyan et al.
EXPERT REVIEW OF ANTICANCER THERAPY (2018)
The functional diversity of Aurora kinases: a comprehensive review
Estelle Willems et al.
CELL DIVISION (2018)
Nature and Hierarchy of Hydrogen-Bonding Interactions in Binary Complexes of Azoles with Water and Hydrogen Peroxide
Neha Chopra et al.
ACS OMEGA (2018)
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)
Approved and Experimental Small-Molecule Oncology Kinase Inhibitor Drugs: A Mid-2016 Overview
Peter M. Fischer
MEDICINAL RESEARCH REVIEWS (2017)
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)
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)
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)
Syk inhibitors in clinical development for hematological malignancies
Delong Liu et al.
JOURNAL OF HEMATOLOGY & ONCOLOGY (2017)
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)
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)
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)
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)
A Phase 1 Study of LY2874455, an Oral Selective pan-FGFR Inhibitor, in Patients with Advanced Cancer
Michael Michael et al.
TARGETED ONCOLOGY (2017)
Aurora kinases: novel therapy targets in cancers
Anqun Tang et al.
ONCOTARGET (2017)
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)
Recent progress towards clinically relevant ATP-competitive Akt inhibitors
Bayard R. Huck et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2017)
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)
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)
Cell signaling regulation by protein phosphorylation: a multivariate, heterogeneous, and context-dependent process
Evan K. Day et al.
CURRENT OPINION IN BIOTECHNOLOGY (2016)
MET INHIBITION AND MERESTINIB (LY-2801653) FOR CANCER TREATMENT
P. A. Prins et al.
DRUGS OF THE FUTURE (2016)
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)
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)
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)
How a Kinase Inhibitor Withstands Gatekeeper Residue Mutations
Jagannath Mondal et al.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2016)
cMET Exon 14 Skipping: From the Structure to the Clinic
Nele Van der Steen et al.
JOURNAL OF THORACIC ONCOLOGY (2016)
Classification of small molecule protein kinase inhibitors based upon the structures of their drug-enzyme complexes
Robert Roskoski
PHARMACOLOGICAL RESEARCH (2016)
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)
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)
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)
Privileged scaffolds in lead generation
Hongyu Zhao et al.
EXPERT OPINION ON DRUG DISCOVERY (2015)
LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms
Constance King et al.
MOLECULAR CANCER THERAPEUTICS (2015)
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)
Blu-285, a Potent and Selective Inhibitor for Hematologic Malignancies with KIT Exon 17 Mutations
Erica Evans et al.
BLOOD (2015)
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)
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)
Preclinical evaluation of LY2801653, an orally bioavailable small molecule oncokinase inhibitor, in cholangiocarcinoma models
Sau-Chi Betty Yan et al.
CANCER RESEARCH (2014)
Protein kinase inhibitors in the treatment of inflammatory and autoimmune diseases
H. Patterson et al.
CLINICAL AND EXPERIMENTAL IMMUNOLOGY (2014)
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)
KLIFS: A Knowledge-Based Structural Database To Navigate Kinase-Ligand Interaction Space
Oscar P. J. van Linden et al.
JOURNAL OF MEDICINAL CHEMISTRY (2014)
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)
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)
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)
Discovery of Novel AKT Inhibitors with Enhanced Anti-Tumor Effects in Combination with the MEK Inhibitor
Melissa Dumble et al.
PLOS ONE (2014)
Effect of NS-018, a selective JAK2V617F inhibitor, in a murine model of myelofibrosis
Y. Nakaya et al.
BLOOD CANCER JOURNAL (2014)
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)
New Potential Antitumor Pyrazole Derivatives: Synthesis and Cytotoxic Evaluation
George Mihai Nitulescu et al.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2013)
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)
Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F
L. Ma et al.
BLOOD CANCER JOURNAL (2013)
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families
Michael L. Curtin et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2012)
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)
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)
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)
A novel and selective c-Met inhibitor against subcutaneous xenograft and othotopic brain tumor models
Yumin Cui et al.
CANCER RESEARCH (2011)
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)
ENMD-2076 Is an Orally Active Kinase Inhibitor with Antiangiogenic and Antiproliferative Mechanisms of Action
Graham C. Fletcher et al.
MOLECULAR CANCER THERAPEUTICS (2011)
RAF protein-serine/threonine kinases: Structure and regulation
Robert Roskoski
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2010)
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)
Defining the conserved internal architecture of a protein kinase
Alexandr P. Kornev et al.
BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS (2010)
Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms
Alfonso Quintas-Cardama et al.
BLOOD (2010)
Targeting Cell Division Cycle 7 Kinase: A New Approach for Cancer Therapy
Alessia Montagnoli et al.
CLINICAL CANCER RESEARCH (2010)
cAMP-dependent protein kinase: Crystallographic insights into substrate recognition and phosphotransfer
Madhusudan et al.
PROTEIN SCIENCE (2010)
The discovery of the potent aurora inhibitor MK-0457 (VX-680)
David Bebbington et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)
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)
Targeting phosphoinositide 3-kinase - Moving towards therapy
Romina Marone et al.
BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS (2008)
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)
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)
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)
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: Synthesis and SAR studies
Xiaodong Lin et al.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2006)
Are target-family-privileged substructures truly privileged?
DM Schnur et al.
JOURNAL OF MEDICINAL CHEMISTRY (2006)
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)
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)
Mechanisms of BCR-ABL in the pathogenesis of chronic myelogenous leukaemia
R Ren
NATURE REVIEWS CANCER (2005)
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)
Identification of novel ERK2 substrates through use of an engineered kinase and ATP analogs
ST Eblen et al.
JOURNAL OF BIOLOGICAL CHEMISTRY (2003)