Article
AP24163 inhibits the gatekeeper mutant of BCR-ABL and suppresses in vitro resistance.
Chemical biology & drug design - 1 Feb 2010
Azam Mohammad, Powers John T, Einhorn William, Huang Wei-Sheng, Shakespeare William C, Zhu Xiaotian, Dalgarno David, Clackson Tim, Sawyer Tomi K, Daley George Q
Abstract excerpt
Mutation in the ABL kinase domain is the principal mechanism of imatinib resistance in patients with chronic myelogenous leukaemia. The second generation BCR/ABL inhibitors nilotinib and dasatinib effectively inhibit most imatinib resistance variants, but are ineffective against the gatekeeper mu...
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