The 1.65 Å resolution structure of the complex of AZD4547 with the kinase domain of FGFR1 displays exquisite molecular recognition

Conformation-Selective Inhibitors Reveal Differences in the Activation and Phosphate-Binding Loops of the Tyrosine Kinases Abl and Src

(2013) Sanjay B. Hari et al.   ACS Chemical Biology

How good are my data and what is the resolution?

(2013) Philip R. Evans et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Type II Kinase Inhibitors: An Opportunity in Cancer for Rational Design

(2013) Javier Blanc et al.   Anti-Cancer Agents in Medicinal Chemistry

FGFR1 Kinase Inhibitors: Close Regioisomers Adopt Divergent Binding Modes and Display Distinct Biophysical Signatures

(2013) Tobias Klein et al.   ACS Medicinal Chemistry Letters

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

(2013) Maria Vittoria Dieci et al.   Cancer Discovery

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

Brivanib: a review of development

(2012) Tina Chou et al.   Future Oncology

Protein–Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase

(2012) Richard A. Norman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Pazopanib for soft-tissue sarcoma: a PALETTE of data emerges

(2012) Isabelle Ray-Coquard et al.   Nature Reviews Clinical Oncology

Anticancer molecules targeting fibroblast growth factor receptors

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

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

(2012) V. Guagnano et al.   Cancer Discovery

REFMAC5 for the refinement of macromolecular crystal structures

(2011) Garib N. Murshudov et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Upregulated FGFR1 expression is associated with the transition of hormone-naive to castrate-resistant prostate cancer

(2011) K Armstrong et al.   BRITISH JOURNAL OF CANCER

The European Medicines Agency Review of Pazopanib for the Treatment of Advanced Renal Cell Carcinoma: Summary of the Scientific Assessment of the Committee for Medicinal Products for Human Use

(2011) M. Nieto et al.   CLINICAL CANCER RESEARCH

FGFR Signaling Promotes the Growth of Triple-Negative and Basal-Like Breast Cancer Cell Lines Both In Vitro and In Vivo

(2011) Rachel Sharpe et al.   CLINICAL CANCER RESEARCH

Phase I/II and Pharmacodynamic Study of Dovitinib (TKI258), an Inhibitor of Fibroblast Growth Factor Receptors and VEGF Receptors, in Patients with Advanced Melanoma

(2011) K. B. Kim et al.   CLINICAL CANCER RESEARCH

Pazopanib: a promising new agent in the treatment of soft tissue sarcomas

(2011) Bernd Kasper et al.   Future Oncology

Understanding the Impact of the P-loop Conformation on Kinase Selectivity

(2011) Cristiano R. W. Guimarães et al.   Journal of Chemical Information and Modeling

Randomized Phase II Placebo-Controlled Trial of Maintenance Therapy Using the Oral Triple Angiokinase Inhibitor BIBF 1120 After Chemotherapy for Relapsed Ovarian Cancer

(2011) Jonathan A. Ledermann et al.   JOURNAL OF CLINICAL ONCOLOGY

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

XDS

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Features and development ofCoot

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

A Structure-Guided Approach to Creating Covalent FGFR Inhibitors

(2010) Wenjun Zhou et al.   CHEMISTRY & BIOLOGY

Non-ATP Competitive Protein Kinase Inhibitors

(2010) L. Garuti et al.   CURRENT MEDICINAL CHEMISTRY

MolProbity: all-atom structure validation for macromolecular crystallography

(2009) Vincent B. Chen et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Equally Potent Inhibition of c-Src and Abl by Compounds that Recognize Inactive Kinase Conformations

(2009) M. A. Seeliger et al.   CANCER RESEARCH

The FGF family: biology, pathophysiology and therapy

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

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

(2008) F. Hilberg et al.   CANCER RESEARCH

Small Molecule Recognition of c-Src via the Imatinib-Binding Conformation

(2008) Arvin C. Dar et al.   CHEMISTRY & BIOLOGY

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

(2008) J. Tsai et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA