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Article

The Dawn of Allosteric BCR-ABL1 Drugs: From a Phenotypic Screening Hit to an Approved Drug.

Journal of medicinal chemistry - 9 Jun 2022

Teng Mingxing, Luskin Marlise R, Cowan-Jacob Sandra W, Ding Qiang, Fabbro Doriano, Gray Nathanael S

Abstract excerpt

Chronic myeloid leukemia (CML) is driven by the constitutive activity of the BCR-ABL1 fusion oncoprotein. Despite the great success of drugs that target the BCR-ABL1 ATP-binding site in transforming CML into a manageable disease, emerging resistance point mutations impair inhibitor binding, thereby limiting the effectiveness of these drugs. Recently, allosteric inhibitors that interact with the ABL1...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 35609336
DOI: 10.1021/acs.jmedchem.2c00373

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 3 Sept 2026.

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