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Article

Imatinib can act as an Allosteric Activator of Abl Kinase.

Journal of molecular biology - 30 Jan 2022

Xie Tao, Saleh Tamjeed, Rossi Paolo, Miller Darcie, Kalodimos Charalampos G

Abstract excerpt

Imatinib is an ATP-competitive inhibitor of Bcr-Abl kinase and the first drug approved for chronic myelogenous leukemia (CML) treatment. Here we show that imatinib binds to a secondary, allosteric site located in the myristoyl pocket of Abl to function as an activator of the kinase activity. Abl transitions between an assembled, inhibited state and an extended, activated state. The equilibrium is regulated by the...

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Share to Drug Resistance, Neoplasm
Share to Allosteric Regulation
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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Antineoplastic Agents

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Share to Leukemia, Myelogenous, Chronic, BCR-ABL Positive

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Source

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Identifiers

PMID: 34774565
DOI: 10.1016/j.jmb.2021.167349
PMCID: PMC8752476

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 4 Sept 2026.

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