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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 mutant, T315I. Gatekeeper mutation activates the kinase by stabilizing the hydrophobic spine. Here, we describe that the...

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Source

Identifiers

PMID: 20028401
DOI: 10.1111/j.1747-0285.2009.00911.x

Genes

BCR

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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