TAS-120 Cancer Target Binding: Defining Reactivity and Revealing the First Fibroblast Growth Factor Receptor 1 (FGFR1) Irreversible Structure

O-001Efficacy of TAS-120, an irreversible fibroblast growth factor receptor (FGFR) inhibitor, in cholangiocarcinoma patients with FGFR pathway alterations who were previously treated with chemotherapy and other FGFR inhibitors

(2018) F Meric-Bernstam et al.   ANNALS OF ONCOLOGY

Structure-based design of targeted covalent inhibitors

(2018) Richard Lonsdale et al.   CHEMICAL SOCIETY REVIEWS

Discovery of Potent Irreversible Pan-Fibroblast Growth Factor Receptor (FGFR) Inhibitors

(2018) Yuming Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

2-Oxo-3, 4-dihydropyrimido[4, 5- d ]pyrimidinyl derivatives as new irreversible pan fibroblast growth factor receptor (FGFR) inhibitors

(2017) Xueqiang Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

Targeted Covalent Inhibitors for Drug Design

(2016) Thomas A. Baillie   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Fibroblast Growth Factor Receptor (FGFR): A New Target for Non-small Cell Lung Cancer Therapy

(2016) Federica Biello et al.   Anti-Cancer Agents in Medicinal Chemistry

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

(2016) MASARU KATOH   INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE

The ins and outs of selective kinase inhibitor development

(2015) Susanne Müller et al.   Nature Chemical Biology

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

X-ray origins: protection or paranoia?

(2015) Natalie Johnson et al.   Acta Crystallographica A-Foundation and Advances

SHELXT– Integrated space-group and crystal-structure determination

(2015) George M. Sheldrick   Acta Crystallographica A-Foundation and Advances

A neutron-diffraction study of the low-cycle fatigue behaviour of an austenitic stainless steel 316

(2015) Adelaide Dubreuil et al.   ACTA CRYSTALLOGRAPHICA SECTION A

DFG-out Mode of Inhibition by an Irreversible Type-1 Inhibitor Capable of Overcoming Gate-Keeper Mutations in FGF Receptors

(2014) Zhifeng Huang et al.   ACS Chemical Biology

A Fragment-Based Method to Discover Irreversible Covalent Inhibitors of Cysteine Proteases

(2014) Stefan G. Kathman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Cell-based strategies to manage leukemia relapse: efficacy and feasibility of immunotherapy approaches

(2014) A Rambaldi et al.   LEUKEMIA

Abstract A270: TAS-120, a highly potent and selective irreversible FGFR inhibitor, is effective in tumors harboring various FGFR gene abnormalities.

(2014) H. Ochiiwa et al.   MOLECULAR CANCER THERAPEUTICS

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

Fibroblast growth factor receptors, developmental corruption and malignant disease

(2013) F. C. Kelleher et al.   CARCINOGENESIS

Developing Irreversible Inhibitors of the Protein Kinase Cysteinome

(2013) Qingsong Liu et al.   CHEMISTRY & BIOLOGY

Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance

(2013) P. A. Schwartz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeting Receptor Tyrosine Kinase Pathways in Hepatocellular Carcinoma

(2012) Hung Huynh et al.   Anti-Cancer Agents in Medicinal Chemistry

Irreversible Protein Kinase Inhibitors: Balancing the Benefits and Risks

(2012) Tjeerd Barf et al.   JOURNAL OF MEDICINAL CHEMISTRY

Anticancer molecules targeting fibroblast growth factor receptors

(2012) Guang Liang et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Protein identification using MS/MS data

(2011) John S. Cottrell   Journal of Proteomics

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

Construction of recombinant FGFR1 containing full-length gene and its potential application

(2010) Yali Zhou et al.   PLASMID