Structure, activation and dysregulation of fibroblast growth factor receptor kinases: perspectives for clinical targeting

Discovery of Rogaratinib (BAY 1163877): a pan-FGFR Inhibitor

(2018) Marie-Pierre Collin et al.   ChemMedChem

Visualization of ligand-induced transmembrane signaling in the full-length human insulin receptor

(2018) Theresia Gutmann et al.   JOURNAL OF CELL BIOLOGY

Disease Variants of FGFR3 Reveal Molecular Basis for the Recognition and Additional Roles for Cdc37 in Hsp90 Chaperone System

(2018) Tom D. Bunney et al.   STRUCTURE

α-Klotho is a non-enzymatic molecular scaffold for FGF23 hormone signalling

(2018) Gaozhi Chen et al.   NATURE

Structures of β-klotho reveal a ‘zip code’-like mechanism for endocrine FGF signalling

(2018) Sangwon Lee et al.   NATURE

Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors

(2017) Ken A. Brameld et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2017) Timothy P.S. Perera et al.   MOLECULAR CANCER THERAPEUTICS

Structural Basis of TPR-Mediated Oligomerization and Activation of Oncogenic Fusion Kinases

(2017) Kuntal Pal et al.   STRUCTURE

How Hsp90 and Cdc37 Lubricate Kinase Molecular Switches

(2017) Kliment A. Verba et al.   TRENDS IN BIOCHEMICAL SCIENCES

Effects of FGFR2 kinase activation loop dynamics on catalytic activity

(2017) Jerome M. Karp et al.   PLoS Computational Biology

Elucidation of a four-site allosteric network in fibroblast growth factor receptor tyrosine kinases

(2017) Huaibin Chen et al.   eLife

A dynamic hydrophobic core orchestrates allostery in protein kinases

(2017) Jonggul Kim et al.   Science Advances

Preclinical Efficacy of the Auristatin-Based Antibody–Drug Conjugate BAY 1187982 for the Treatment of FGFR2-Positive Solid Tumors

(2016) Anette Sommer et al.   CANCER RESEARCH

First-in-human study of BLU-554, a potent, highly-selective FGFR4 inhibitor designed for hepatocellular carcinoma (HCC) with FGFR4 pathway activation

(2016) R. Kim et al.   EUROPEAN JOURNAL OF CANCER

FGFR inhibitors: Effects on cancer cells, tumor microenvironment and whole-body homeostasis (Review)

(2016) MASARU KATOH   INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE

Mechanism of FGF receptor dimerization and activation

(2016) Sarvenaz Sarabipour et al.   Nature Communications

Inhibition of the fibroblast growth factor receptor (FGFR) pathway: the current landscape and barriers to clinical application

(2016) Young Kwang Chae et al.   Oncotarget

Inhibition of FGF/FGFR autocrine signaling in mesothelioma with the FGF ligand trap, FP-1039/GSK3052230

(2016) Christina Blackwell et al.   Oncotarget

Landscape of activating cancer mutations in FGFR kinases and their differential responses to inhibitors in clinical use

(2016) Harshnira Patani et al.   Oncotarget

Characterization of FGFR signaling pathway as therapeutic targets for sarcoma patients

(2016) Wen-Ya Zhou et al.   Cancer Biology & Medicine

Preclinical Activity of ARQ 087, a Novel Inhibitor Targeting FGFR Dysregulation

(2016) Terence G. Hall et al.   PLoS One

Abstract 771: Preclinical characterization of the selective FGFR inhibitor INCB054828

(2015) Phillip CC Liu et al.   CANCER RESEARCH

Targeting FGFR Signaling in Cancer

(2015) M. Touat et al.   CLINICAL CANCER RESEARCH

Unliganded Fibroblast Growth Factor Receptor 1 Forms Density-independent Dimers

(2015) Laëtitia Comps-Agrar et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

FGFR3 Unliganded Dimer Stabilization by the Juxtamembrane Domain

(2015) Sarvenaz Sarabipour et al.   JOURNAL OF MOLECULAR BIOLOGY

Structural and dynamic insights into the energetics of activation loop rearrangement in FGFR1 kinase

(2015) Tobias Klein et al.   Nature Communications

First Selective Small Molecule Inhibitor of FGFR4 for the Treatment of Hepatocellular Carcinomas with an Activated FGFR4 Signaling Pathway

(2015) M. Hagel et al.   Cancer Discovery

Abstract 4766: Pharmacodynamic and stratification biomarker for the anti-FGFR2 antibody (BAY1179470) and the FGFR2-ADC

(2015) Christoph A. Schatz et al.   CANCER RESEARCH

Abstract LB-145: Results of a phase I study of AZD4547, an inhibitor of fibroblast growth factor receptor (FGFR), in patients with advanced solid tumors .

(2014) Fabrice Andre et al.   CANCER RESEARCH

Conformational Analysis of the DFG-Out Kinase Motif and Biochemical Profiling of Structurally Validated Type II Inhibitors

(2014) R. S. K. Vijayan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural Analysis of the Human Fibroblast Growth Factor Receptor 4 Kinase

(2014) E. Lesca et al.   JOURNAL OF MOLECULAR BIOLOGY

Kinase Regulation by Hydrophobic Spine Assembly in Cancer

(2014) Jiancheng Hu et al.   MOLECULAR AND CELLULAR BIOLOGY

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

(2014) Y. Nakanishi et al.   MOLECULAR CANCER THERAPEUTICS

Ligand-associated ERBB2/3 activation confers acquired resistance to FGFR inhibition in FGFR3-dependent cancer cells

(2014) J Wang et al.   ONCOGENE

Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors

(2014) Li Tan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Insights into FGFR Kinase Isoform Selectivity: Diverse Binding Modes of AZD4547 and Ponatinib in Complex with FGFR1 and FGFR4

(2014) Julie A. Tucker et al.   STRUCTURE

Predicting the Impact of Deleterious Mutations in the Protein Kinase Domain of FGFR2 in the Context of Function, Structure, and Pathogenesis—a Bioinformatics Approach

(2013) George Priya Doss C et al.   APPLIED BIOCHEMISTRY AND BIOTECHNOLOGY

Molecular Mechanism of SSR128129E, an Extracellularly Acting, Small-Molecule, Allosteric Inhibitor of FGF Receptor Signaling

(2013) Corentin Herbert et al.   CANCER CELL

Inhibition of Tumor Angiogenesis and Growth by a Small-Molecule Multi-FGF Receptor Blocker with Allosteric Properties

(2013) Françoise Bono et al.   CANCER CELL

Sequence Determinants of a Specific Inactive Protein Kinase Conformation

(2013) Sanjay B. Hari et al.   CHEMISTRY & BIOLOGY

FGFR2 Gene Amplification in Gastric Cancer Predicts Sensitivity to the Selective FGFR Inhibitor AZD4547

(2013) L. Xie et al.   CLINICAL CANCER RESEARCH

Exploring mechanisms of FGF signalling through the lens of structural biology

(2013) Regina Goetz et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Peripheral Reduction of FGFR4 with Antisense Oligonucleotides Increases Metabolic Rate and Lowers Adiposity in Diet-Induced Obese Mice

(2013) Xing Xian Yu et al.   PLoS One

Structural Mimicry of A-Loop Tyrosine Phosphorylation by a Pathogenic FGF Receptor 3 Mutation

(2013) Zhifeng Huang et al.   STRUCTURE

Structure of FGFR3 Transmembrane Domain Dimer: Implications for Signaling and Human Pathologies

(2013) Eduard V. Bocharov et al.   STRUCTURE

Identification of Targetable FGFR Gene Fusions in Diverse Cancers

(2013) Yi-Mi Wu et al.   Cancer Discovery

Cracking the Molecular Origin of Intrinsic Tyrosine Kinase Activity through Analysis of Pathogenic Gain-of-Function Mutations

(2013) Huaibin Chen et al.   Cell Reports

AZD4547: An Orally Bioavailable, Potent, and Selective Inhibitor of the Fibroblast Growth Factor Receptor Tyrosine Kinase Family

(2012) P. R. Gavine et al.   CANCER RESEARCH

Translating the Therapeutic Potential of AZD4547 in FGFR1-Amplified Non-Small Cell Lung Cancer through the Use of Patient-Derived Tumor Xenograft Models

(2012) J. Zhang et al.   CLINICAL CANCER RESEARCH

Oncogenic FGFR3 gene fusions in bladder cancer

(2012) Sarah V. Williams et al.   HUMAN MOLECULAR GENETICS

Tumour cell responses to new fibroblast growth factor receptor tyrosine kinase inhibitors and identification of a gatekeeper mutation in FGFR3 as a mechanism of acquired resistance

(2012) V Chell et al.   ONCOGENE

Transforming Fusions of FGFR and TACC Genes in Human Glioblastoma

(2012) D. Singh et al.   SCIENCE

The Alternatively Spliced Acid Box Region Plays a Key Role in FGF Receptor Autoinhibition

(2012) Juliya Kalinina et al.   STRUCTURE

The Physical Basis of FGFR3 Response tofgf1andfgf2

(2011) Fenghao Chen et al.   BIOCHEMISTRY

E-3810 Is a Potent Dual Inhibitor of VEGFR and FGFR that Exerts Antitumor Activity in Multiple Preclinical Models

(2011) Ezia Bello et al.   CANCER RESEARCH

Plasticity in Interactions of Fibroblast Growth Factor 1 (FGF1) N Terminus with FGF Receptors Underlies Promiscuity of FGF1

(2011) Andrew Beenken et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase

(2011) Vito Guagnano et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Novel, Selective Inhibitor of Fibroblast Growth Factor Receptors That Shows a Potent Broad Spectrum of Antitumor Activity in Several Tumor Xenograft Models

(2011) G. Zhao et al.   MOLECULAR CANCER THERAPEUTICS

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

Small molecule FGF receptor inhibitors block FGFR-dependent urothelial carcinoma growth in vitro and in vivo

(2010) F R Lamont et al.   BRITISH JOURNAL OF CANCER

Cell Signaling by Receptor Tyrosine Kinases

(2010) Mark A. Lemmon et al.   CELL

FGF signalling: diverse roles during early vertebrate embryogenesis

(2010) K. Dorey et al.   DEVELOPMENT

Asymmetric receptor contact is required for tyrosine autophosphorylation of fibroblast growth factor receptor in living cells

(2010) J. H. Bae et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of tyrosines 154 and 307 in the extracellular domain and 653 and 766 in the intracellular domain as phosphorylation sites in the heparin-binding fibroblast growth factor receptor tyrosine kinase (flg)

(2010) Jinzhao Hou et al.   PROTEIN SCIENCE

Transmembrane helix-helix interactions involved in ErbB receptor signaling

(2010) Florian Cymer et al.   Cell Adhesion & Migration

AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance

(2009) Thomas O'Hare et al.   CANCER CELL

The FGF family: biology, pathophysiology and therapy

(2009) Andrew Beenken et al.   NATURE REVIEWS DRUG DISCOVERY

The FGF23–Klotho axis: endocrine regulation of phosphate homeostasis

(2009) M. Shawkat Razzaque   Nature Reviews Endocrinology

The Precise Sequence of FGF Receptor Autophosphorylation Is Kinetically Driven and Is Disrupted by Oncogenic Mutations

(2009) E. D. Lew et al.   Science Signaling

BIBF 1120: Triple Angiokinase Inhibitor with Sustained Receptor Blockade and Good Antitumor Efficacy

(2008) F. Hilberg et al.   CANCER RESEARCH

A helix scaffold for the assembly of active protein kinases

(2008) A. P. Kornev et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA