BCR-ABL residues interacting with ponatinib are critical to preserve the tumorigenic potential of the oncoprotein

The BCR-ABLT315I mutation compromises survival in chronic phase chronic myelogenous leukemia patients resistant to tyrosine kinase inhibitors, in a matched pair analysis

(2013) F. E. Nicolini et al.   HAEMATOLOGICA

Ponatinib (AP24534) Is a Novel Potent Inhibitor of Oncogenic RET Mutants Associated With Thyroid Cancer

(2013) Valentina De Falco et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Explaining why Gleevec is a specific and potent inhibitor of Abl kinase

(2013) Y.-L. Lin et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Chronic myeloid leukemia: 2012 update on diagnosis, monitoring, and management

(2012) Elias Jabbour et al.   AMERICAN JOURNAL OF HEMATOLOGY

Revised AMBER Parameters for Bioorganic Phosphates

(2012) T. Steinbrecher et al.   Journal of Chemical Theory and Computation

Irreversible Protein Kinase Inhibitors: Balancing the Benefits and Risks

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

The Different Flexibility of c-Src and c-Abl Kinases Regulates the Accessibility of a Druggable Inactive Conformation

(2012) Silvia Lovera et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Ponatinib in Refractory Philadelphia Chromosome–Positive Leukemias

(2012) Jorge E. Cortes et al.   NEW ENGLAND JOURNAL OF MEDICINE

Predicting the Functional Effect of Amino Acid Substitutions and Indels

(2012) Yongwook Choi et al.   PLoS One

Chronic Myeloid Leukemia: Clinical Impact of BCR-ABL1 Mutations and Other Lesions Associated With Disease Progression

(2012) Thomas Ernst et al.   SEMINARS IN ONCOLOGY

The rise and fall of gatekeeper mutations? TheBCR-ABL1T315I paradigm

(2011) Don L. Gibbons et al.   CANCER

Detection of allosteric signal transmission by information-theoretic analysis of protein dynamics

(2011) Alessandro Pandini et al.   FASEB JOURNAL

Interplay between Kinase Domain Autophosphorylation and F-Actin Binding Domain in Regulating Imatinib Sensitivity and Nuclear Import of BCR-ABL

(2011) Martin Preyer et al.   PLoS One

Computational Modeling of Allosteric Communication Reveals Organizing Principles of Mutation-Induced Signaling in ABL and EGFR Kinases

(2011) Anshuman Dixit et al.   PLoS Computational Biology

Practical advice for determining the role of BCR-ABL mutations in guiding tyrosine kinase inhibitor therapy in patients with chronic myeloid leukemia

(2010) Elias Jabbour et al.   CANCER

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

Molecular Dynamics Simulations Show That Conformational Selection Governs the Binding Preferences of Imatinib for Several Tyrosine Kinases

(2010) Alexey Aleksandrov et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant

(2010) Wei-Sheng Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

A method and server for predicting damaging missense mutations

(2010) Ivan A Adzhubei et al.   NATURE METHODS

Understanding resistance to EGFR inhibitors—impact on future treatment strategies

(2010) Deric L. Wheeler et al.   Nature Reviews Clinical Oncology

Long-term outcome of patients with chronic myeloid leukemia treated with second-generation tyrosine kinase inhibitors after imatinib failure is predicted by the in vitro sensitivity of BCR-ABL kinase domain mutations

(2009) E. Jabbour et al.   BLOOD

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

Chronic Myeloid Leukemia: An Update of Concepts and Management Recommendations of European LeukemiaNet

(2009) Michele Baccarani et al.   JOURNAL OF CLINICAL ONCOLOGY

Predicting the effects of coding non-synonymous variants on protein function using the SIFT algorithm

(2009) Prateek Kumar et al.   Nature Protocols

Imatinib and beyond—exploring the full potential of targeted therapy for CML

(2009) Alfonso Quintás-Cardama et al.   Nature Reviews Clinical Oncology

Basis for Resistance to Imatinib in 16 BCR-ABL Mutants as Determined Using Molecular Dynamics

(2009) Tai-Sung Lee et al.   Recent Patents on Anti-Cancer Drug Discovery

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

Translation of the Philadelphia chromosome into therapy for CML

(2008) B. J. Druker   BLOOD

Molecular basis explanation for imatinib resistance of BCR-ABL due to T315I and P-loop mutations from molecular dynamics simulations

(2008) Tai-Sung Lee et al.   CANCER

Therapeutic Options Against BCR-ABL1 T315I-Positive Chronic Myelogenous Leukemia

(2008) A. Quintas-Cardama et al.   CLINICAL CANCER RESEARCH

BCR-ABL alternative splicing as a common mechanism for imatinib resistance: evidence from molecular dynamics simulations

(2008) T.-S. Lee et al.   MOLECULAR CANCER THERAPEUTICS

Activation of tyrosine kinases by mutation of the gatekeeper threonine

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

A conserved protonation-dependent switch controls drug binding in the Abl kinase

(2008) Y. Shan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA