Targeting the Src Pathway Enhances the Efficacy of Selective FGFR Inhibitors in Urothelial Cancers with FGFR3 Alterations

TAS-120 overcomes resistance to ATP-competitive FGFR inhibitors in patients with FGFR2 fusion-positive intrahepatic cholangiocarcinoma

(2019) Lipika Goyal et al.   Cancer Discovery

Erdafitinib in Locally Advanced or Metastatic Urothelial Carcinoma

(2019) Yohann Loriot et al.   NEW ENGLAND JOURNAL OF MEDICINE

Efficacy of BGJ398, a Fibroblast Growth Factor Receptor 1–3 Inhibitor, in Patients with Previously Treated Advanced Urothelial Carcinoma with FGFR3 Alterations

(2018) Sumanta K. Pal et al.   Cancer Discovery

Akt Activation Mediates Acquired Resistance to Fibroblast Growth Factor Receptor Inhibitor BGJ398

(2017) Jharna Datta et al.   MOLECULAR CANCER THERAPEUTICS

Collateral sensitivity networks reveal evolutionary instability and novel treatment strategies in ALK mutated non-small cell lung cancer

(2017) Andrew Dhawan et al.   Scientific Reports

Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity

(2016) Frank E. Kwarcinski et al.   ACS Chemical Biology

Phosphoproteomics in translational research: a sarcoma perspective

(2016) J. Noujaim et al.   ANNALS OF ONCOLOGY

Comprehensive Transcriptional Analysis of Early-Stage Urothelial Carcinoma

(2016) Jakob Hedegaard et al.   CANCER CELL

Exploiting Temporal Collateral Sensitivity in Tumor Clonal Evolution

(2016) Boyang Zhao et al.   CELL

Oncogenic Gene Fusion FGFR3-TACC3 Is Regulated by Tyrosine Phosphorylation

(2016) K. N. Nelson et al.   MOLECULAR CANCER RESEARCH

Combine and conquer: challenges for targeted therapy combinations in early phase trials

(2016) Juanita S. Lopez et al.   Nature Reviews Clinical Oncology

Neoadjuvant dasatinib for muscle-invasive bladder cancer with tissue analysis of biologic activity

(2016) Noah M. Hahn et al.   UROLOGIC ONCOLOGY-SEMINARS AND ORIGINAL INVESTIGATIONS

Polyclonal SecondaryFGFR2Mutations Drive Acquired Resistance to FGFR Inhibition in Patients with FGFR2 Fusion–Positive Cholangiocarcinoma

(2016) Lipika Goyal et al.   Cancer Discovery

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

(2016) Harshnira Patani et al.   Oncotarget

Effect of Thanatophoric Dysplasia Type I Mutations on FGFR3 Dimerization

(2015) Nuala Del Piccolo et al.   BIOPHYSICAL JOURNAL

Detection, Characterization, and Inhibition of FGFR-TACC Fusions in IDH Wild-type Glioma

(2015) A. L. Di Stefano et al.   CLINICAL CANCER RESEARCH

The FGFR Landscape in Cancer: Analysis of 4,853 Tumors by Next-Generation Sequencing

(2015) T. Helsten et al.   CLINICAL CANCER RESEARCH

Mechanism of Oncogenic Signal Activation by the Novel Fusion Kinase FGFR3-BAIAP2L1

(2015) Y. Nakanishi et al.   MOLECULAR CANCER THERAPEUTICS

The Effect of Mutations on Drug Sensitivity and Kinase Activity of Fibroblast Growth Factor Receptors: A Combined Experimental and Theoretical Study

(2015) Tom D. Bunney et al.   EBioMedicine

FGFR3 Translocations in Bladder Cancer: Differential Sensitivity to HSP90 Inhibition Based on Drug Metabolism

(2014) Jaime Acquaviva et al.   MOLECULAR CANCER RESEARCH

Comprehensive molecular characterization of urothelial bladder carcinoma

(2014)   NATURE

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

(2014) J Wang et al.   ONCOGENE

The tumorigenic FGFR3-TACC3 gene fusion escapes miR-99a regulation in glioblastoma

(2013) Brittany C. Parker et al.   JOURNAL OF CLINICAL INVESTIGATION

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

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

Novel Tumor Subgroups of Urothelial Carcinoma of the Bladder Defined by Integrated Genomic Analysis

(2012) C. D. Hurst 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

FGFR Genetic Alterations Predict for Sensitivity to NVP-BGJ398, a Selective Pan-FGFR Inhibitor

(2012) V. Guagnano et al.   Cancer Discovery

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 HIF-Regulated VHL-PTP1B-Src Signaling Axis Identifies a Therapeutic Target in Renal Cell Carcinoma

(2011) N. Suwaki et al.   Science Translational Medicine

Src and Caveolin-1 Reciprocally Regulate Metastasis via a Common Downstream Signaling Pathway in Bladder Cancer

(2010) S. Thomas et al.   CANCER RESEARCH

Receptor Tyrosine Kinase Coactivation Networks in Cancer

(2010) A. M. Xu et al.   CANCER RESEARCH

Drug Combination Studies and Their Synergy Quantification Using the Chou-Talalay Method

(2010) T.-C. Chou   CANCER RESEARCH

Phase I/II Study of the Src Inhibitor Dasatinib in Combination With Erlotinib in Advanced Non–Small-Cell Lung Cancer

(2010) Eric B. Haura et al.   JOURNAL OF CLINICAL ONCOLOGY

Dasatinib Is Preclinically Active against Src-Overexpressing Human Transitional Cell Carcinoma of the Urothelium with Activated Src Signaling

(2010) J. M. Levitt et al.   MOLECULAR CANCER THERAPEUTICS

A chemical and phosphoproteomic characterization of dasatinib action in lung cancer

(2010) Jiannong Li et al.   Nature Chemical Biology

Mutant fibroblast growth factor receptor 3 induces intracellular signaling and cellular transformation in a cell type- and mutation-specific manner

(2009) E di Martino et al.   ONCOGENE