Article
Structural mechanism of the Pan-BCR-ABL inhibitor ponatinib (AP24534): lessons for overcoming kinase inhibitor resistance.
Chemical biology & drug design - 1 Jan 2011
Zhou Tianjun, Commodore Lois, Huang Wei-Sheng, Wang Yihan, Thomas Mathew, Keats Jeff, Xu Qihong, Rivera Victor M, Shakespeare William C, Clackson Tim, Dalgarno David C, Zhu Xiaotian
Abstract excerpt
The BCR-ABL inhibitor imatinib has revolutionized the treatment of chronic myeloid leukemia. However, drug resistance caused by kinase domain mutations has necessitated the development of new mutation-resistant inhibitors, most recently against the T315I gatekeeper residue mutation. Ponatinib (AP24534) inhibits both native and mutant BCR-ABL, including T315I, acting as a pan-BCR-ABL inhibitor. Here, we undertook...
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