Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation

BCR-ABL1 Compound Mutations Combining Key Kinase Domain Positions Confer Clinical Resistance to Ponatinib in Ph Chromosome-Positive Leukemia

(2014) Matthew S. Zabriskie et al.   CANCER CELL

Axitinib safety in metastatic renal cell carcinoma: suggestions for daily clinical practice based on case studies

(2014) Sergio Bracarda et al.   Expert Opinion On Drug Safety

FDA halts then allows sales of Ariad's leukemia medication

(2014) Melanie Senior   NATURE BIOTECHNOLOGY

Molecular dynamics reveal BCR-ABL1 polymutants as a unique mechanism of resistance to PAN-BCR-ABL1 kinase inhibitor therapy

(2014) Don L. Gibbons et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Substrate-Specific Conformational Regulation of the Receptor Tyrosine Kinase VEGFR2 Catalytic Domain

(2013) James Solowiej et al.   ACS Chemical Biology

Threshold Levels of ABL Tyrosine Kinase Inhibitors Retained in Chronic Myeloid Leukemia Cells Determine Their Commitment to Apoptosis

(2013) T. O'Hare et al.   CANCER RESEARCH

Clinical Pharmacology of Axitinib

(2013) Ying Chen et al.   CLINICAL PHARMACOKINETICS

Individualized Systems Medicine Strategy to Tailor Treatments for Patients with Chemorefractory Acute Myeloid Leukemia

(2013) T. Pemovska et al.   Cancer Discovery

Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors

(2012) M. McTigue et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Conformational Control Inhibition of the BCR-ABL1 Tyrosine Kinase, Including the Gatekeeper T315I Mutant, by the Switch-Control Inhibitor DCC-2036

(2011) Wayne W. Chan et al.   CANCER CELL

Comparative effectiveness of axitinib versus sorafenib in advanced renal cell carcinoma (AXIS): a randomised phase 3 trial

(2011) Brian I Rini et al.   LANCET

Comprehensive analysis of kinase inhibitor selectivity

(2011) Mindy I Davis et al.   NATURE BIOTECHNOLOGY

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

Structural Mechanism of the Pan-BCR-ABL Inhibitor Ponatinib (AP24534): Lessons for Overcoming Kinase Inhibitor Resistance

(2010) Tianjun Zhou et al.   Chemical Biology & Drug Design

Characterizing the Effects of the Juxtamembrane Domain on Vascular Endothelial Growth Factor Receptor-2 Enzymatic Activity, Autophosphorylation, and Inhibition by Axitinib

(2009) James Solowiej et al.   BIOCHEMISTRY

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

Six-year follow-up of patients receiving imatinib for the first-line treatment of chronic myeloid leukemia

(2009) A Hochhaus et al.   LEUKEMIA

Hierarchical Modeling of Activation Mechanisms in the ABL and EGFR Kinase Domains: Thermodynamic and Mechanistic Catalysts of Kinase Activation by Cancer Mutations

(2009) Anshuman Dixit et al.   PLoS Computational Biology

Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I

(2008) A. Gontarewicz et al.   BLOOD

Transient Potent BCR-ABL Inhibition Is Sufficient to Commit Chronic Myeloid Leukemia Cells Irreversibly to Apoptosis

(2008) Neil P. Shah et al.   CANCER CELL

Activity of Bosutinib, Dasatinib, and Nilotinib Against 18 Imatinib-Resistant BCR/ABL Mutants

(2008) Sara Redaelli et al.   JOURNAL OF CLINICAL ONCOLOGY

Activation of tyrosine kinases by mutation of the gatekeeper threonine

(2008) Mohammad Azam et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY