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

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

Selecting optimal second-line tyrosine kinase inhibitor therapy for chronic myeloid leukemia patients after imatinib failure: does the BCR-ABL mutation status really matter?

(2009) S. Branford 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

Resistance to Targeted Therapies: Refining Anticancer Therapy in the Era of Molecular Oncology

(2009) L. M. Ellis et al.   CLINICAL CANCER RESEARCH

Kinase Domain Mutations in Cancer: Implications for Small Molecule Drug Design Strategies

(2009) Jack A. Bikker et al.   JOURNAL OF MEDICINAL CHEMISTRY

Through the “Gatekeeper Door”: Exploiting the Active Kinase Conformation

(2009) Fabio Zuccotto et al.   JOURNAL OF MEDICINAL CHEMISTRY