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

FGF receptor genes and breast cancer susceptibility: results from the Breast Cancer Association Consortium

(2014) D Agarwal et al.   BRITISH JOURNAL OF CANCER

Drug Resistance via Feedback Activation of Stat3 in Oncogene-Addicted Cancer Cells

(2014) Ho-June Lee et al.   CANCER CELL

Abstract 5195: Kidney injury molecule-1: a novel therapeutic target in renal cell carcinoma.

(2014) Venkata Sabbisetti et al.   CANCER RESEARCH

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

(2014) J Wang et al.   ONCOGENE

Fibroblast growth factor receptor 4 (FGFR4): a targetable regulator of drug resistance in colorectal cancer

(2014) R C Turkington et al.   Cell Death & Disease

Functional roles of fibroblast growth factor receptors (FGFRs) signaling in human cancers

(2013) Kai Hung Tiong et al.   APOPTOSIS

Associations with growth factor genes (FGF1, FGF2, PDGFB, FGFR2, NRG2, EGF, ERBB2) with breast cancer risk and survival: the Breast Cancer Health Disparities Study

(2013) Martha L. Slattery et al.   BREAST CANCER RESEARCH AND TREATMENT

The Cancer-Associated FGFR4-G388R Polymorphism Enhances Pancreatic Insulin Secretion and Modifies the Risk of Diabetes

(2013) Shereen Ezzat et al.   Cell Metabolism

Identification of FGFR4 as a Potential Therapeutic Target for Advanced-Stage, High-Grade Serous Ovarian Cancer

(2013) T. M. Zaid et al.   CLINICAL CANCER RESEARCH

Integrative and Comparative Genomic Analysis of Lung Squamous Cell Carcinomas in East Asian Patients

(2013) Youngwook Kim et al.   JOURNAL OF CLINICAL ONCOLOGY

Identification of recurrentFGFR3fusion genes in lung cancer through kinome-centred RNA sequencing

(2013) Ian J Majewski et al.   JOURNAL OF PATHOLOGY

FGF Receptors: Cancer Biology and Therapeutics

(2013) Masaru Katoh et al.   MEDICINAL RESEARCH REVIEWS

Activation of the FGF2-FGFR1 Autocrine Pathway: A Novel Mechanism of Acquired Resistance to Gefitinib in NSCLC

(2013) Hideki Terai et al.   MOLECULAR CANCER RESEARCH

Activating Somatic FGFR2 Mutations in Breast Cancer

(2013) Nadine Reintjes et al.   PLoS One

FGFR4 Role in Epithelial-Mesenchymal Transition and Its Therapeutic Value in Colorectal Cancer

(2013) Alberto Peláez-García et al.   PLoS One

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

(2013) Zhifeng Huang et al.   STRUCTURE

Fibroblast growth factor receptor 4 Gly388Arg polymorphism in Chinese gastric cancer patients

(2013) Yan-Ying Shen   WORLD JOURNAL OF GASTROENTEROLOGY

Identification of Targetable FGFR Gene Fusions in Diverse Cancers

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

Parallel RNA Interference Screens Identify EGFR Activation as an Escape Mechanism in FGFR3-Mutant Cancer

(2013) M. T. Herrera-Abreu et al.   Cancer Discovery

Fibroblast Growth Factor Receptor Inhibitors as a Cancer Treatment: From a Biologic Rationale to Medical Perspectives

(2013) Maria Vittoria Dieci et al.   Cancer Discovery

A randomised controlled trial of a theory-based intervention to improve sun protective behaviour in adolescents ('you can still be HOT in the shade'): study protocol

(2012) Anna L Hawkes et al.   BMC CANCER

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

Molecular Pathways: Fibroblast Growth Factor Signaling: A New Therapeutic Opportunity in Cancer

(2012) A. N. Brooks et al.   CLINICAL CANCER RESEARCH

The Clinical Effect of the Dual-Targeting Strategy Involving PI3K/AKT/mTOR and RAS/MEK/ERK Pathways in Patients with Advanced Cancer

(2012) T. Shimizu et al.   CLINICAL CANCER RESEARCH

Fgfr-Ras-MAPK signaling is required for apical constriction via apical positioning of Rho-associated kinase during mechanosensory organ formation

(2012) M. J. Harding et al.   DEVELOPMENT

Screening therapeutic EMT blocking agents in a three-dimensional microenvironment

(2012) Amir R. Aref et al.   Integrative Biology

Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting Epidermal Growth Factor Receptor Threonine790 → Methionine790 Mutant

(2012) Shaohua Chang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Systems-wide RNAi analysis of CASP8AP2/FLASH shows transcriptional deregulation of the replication-dependent histone genes and extensive effects on the transcriptome of colorectal cancer cells

(2012) Amanda B Hummon et al.   Molecular Cancer

Fibroblast Growth Factor Receptor 2 IIIc as a Therapeutic Target for Colorectal Cancer Cells

(2012) Y. Matsuda et al.   MOLECULAR CANCER THERAPEUTICS

Identification of new ALK and RET gene fusions from colorectal and lung cancer biopsies

(2012) Doron Lipson et al.   NATURE MEDICINE

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

Targeting Fibroblast Growth Factor Receptor Signaling in Hepatocellular Carcinoma

(2012) Ann-Lii Cheng et al.   ONCOLOGY

Targeting FGFR4 Inhibits Hepatocellular Carcinoma in Preclinical Mouse Models

(2012) Dorothy M. French et al.   PLoS One

Ensemble Analysis of Angiogenic Growth in Three-Dimensional Microfluidic Cell Cultures

(2012) Waleed A. Farahat et al.   PLoS One

Transforming Fusions of FGFR and TACC Genes in Human Glioblastoma

(2012) D. Singh et al.   SCIENCE

The t(4;14) translocation and FGFR3 overexpression in multiple myeloma: prognostic implications and current clinical strategies

(2012) A Kalff et al.   Blood Cancer Journal

Foreword Target Therapy for Cancer: Anti-cancer Drugs Targeting Growth-Factor Signaling Molecules

(2011) Fumiaki Ito   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Fibroblast growth factor receptor 4 regulates proliferation and antiapoptosis during gastric cancer progression

(2011) Yan Wei Ye et al.   CANCER

High-Throughput Kinase Profiling: A More Efficient Approach toward the Discovery of New Kinase Inhibitors

(2011) Chandrasekhar V. Miduturu et al.   CHEMISTRY & BIOLOGY

Oncogene Mutation Profiling of Pediatric Solid Tumors Reveals Significant Subsets of Embryonal Rhabdomyosarcoma and Neuroblastoma with Mutated Genes in Growth Signaling Pathways

(2011) N. Shukla et al.   CLINICAL CANCER RESEARCH

The kinase inhibitor TKI258 is active against the novel CUX1-FGFR1 fusion detected in a patient with T-lymphoblastic leukemia/lymphoma and t(7;8)(q22;p11)

(2011) B. Wasag et al.   HAEMATOLOGICA

Cysteine Mapping in Conformationally Distinct Kinase Nucleotide Binding Sites: Application to the Design of Selective Covalent Inhibitors

(2011) Emeline Leproult et al.   JOURNAL OF MEDICINAL 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

FGFR2 alterations in endometrial carcinoma

(2011) Sonia Gatius et al.   MODERN PATHOLOGY

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

Overexpression of fibroblast growth factor receptors FGFR1 and FGFR2 in renal cell carcinoma

(2011) Ilya Tsimafeyeu et al.   SCANDINAVIAN JOURNAL OF UROLOGY AND NEPHROLOGY

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

PHENIX: a comprehensive Python-based system for macromolecular structure solution

(2010) Paul D. Adams et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFR , Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants

(2010) E. Weisberg et al.   BLOOD

Inhibition of FGFR2 and FGFR1 increases cisplatin sensitivity in ovarian cancer

(2010) Claire Cole et al.   CANCER BIOLOGY & THERAPY

Targeting Fibroblast Growth Factor Receptors Blocks PI3K/AKT Signaling, Induces Apoptosis, and Impairs Mammary Tumor Outgrowth and Metastasis

(2010) J. H. Dey et al.   CANCER RESEARCH

A Structure-Guided Approach to Creating Covalent FGFR Inhibitors

(2010) Wenjun Zhou et al.   CHEMISTRY & BIOLOGY

Overexpression of KLF13 and FGFR3 in Oral Cancer Cells

(2010) B.J. Henson et al.   CYTOGENETIC AND GENOME RESEARCH

Rapidly Acquired Resistance to EGFR Tyrosine Kinase Inhibitors in NSCLC Cell Lines through De-Repression of FGFR2 and FGFR3 Expression

(2010) Kathryn E. Ware et al.   PLoS One

Frequent and Focal FGFR1 Amplification Associates with Therapeutically Tractable FGFR1 Dependency in Squamous Cell Lung Cancer

(2010) J. Weiss et al.   Science Translational Medicine

The fibroblast growth factor receptor signaling pathway as a mediator of intrinsic resistance to EGFR-specific tyrosine kinase inhibitors in non-small cell lung cancer

(2009) Scott A. Kono et al.   DRUG RESISTANCE UPDATES

Nilotinib: A second-generation tyrosine kinase inhibitor for chronic myeloid leukemia

(2009) Massimo Breccia et al.   LEUKEMIA RESEARCH

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

(2009) Wenjun Zhou et al.   NATURE

The FGFR4 Y367C mutant is a dominant oncogene in MDA-MB453 breast cancer cells

(2009) A Roidl et al.   ONCOGENE

Mechanisms of resistance to tyrosine kinase inhibitors in chronic myeloid leukemia and recent therapeutic strategies to overcome resistance

(2009) D. Bixby et al.   Hematology-American Society of Hematology Education Program

Overexpression of the fibroblast growth factor receptor 2-IIIc in Kaposi's sarcoma

(2008) Francesca Cottoni et al.   JOURNAL OF DERMATOLOGICAL SCIENCE

Fibroblast growth factor receptor 4 regulates proliferation, anti-apoptosis and alpha-fetoprotein secretion during hepatocellular carcinoma progression and represents a potential target for therapeutic intervention

(2008) Han Kiat Ho et al.   JOURNAL OF HEPATOLOGY

The roles of the FGF signal in zebrafish embryos analyzed using constitutive activation and dominant-negative suppression of different FGF receptors

(2008) Satoshi Ota et al.   MECHANISMS OF DEVELOPMENT

High-throughput kinase profiling as a platform for drug discovery

(2008) David M. Goldstein et al.   NATURE REVIEWS DRUG DISCOVERY

BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models

(2008) D Li et al.   ONCOGENE

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

(2008) C.-H. Yun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Achondroplasia: From genotype to phenotype

(2007) Pascal Richette et al.   JOINT BONE SPINE