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Article

Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.

Journal of medicinal chemistry - 25 Jul 2013

Richters André, Ketzer Julia, Getlik Matthäus, Grütter Christian, Schneider Ralf, Heuckmann Johannes M, Heynck Stefanie, Sos Martin L, Gupta Anu, Unger Anke, Schultz-Fademrecht Carsten, Thomas Roman K, Bauer Sebastian, Rauh Daniel

Abstract excerpt

Mutations in the catalytic domain at the gatekeeper position represent the most prominent drug-resistant variants of kinases and significantly impair the efficacy of targeted cancer therapies. Understanding the mechanisms of drug resistance at the molecular and atomic levels will aid in the desig...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Drug Resistance, Neoplasm

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

Share to Protein Kinase Inhibitors

Share to Proto-Oncogene Proteins c-abl

Share to Proto-Oncogene Proteins c-kit

Share to Structure-Activity Relationship

Source

Identifiers

PMID: 23773153
DOI: 10.1021/jm4004076

Genes

KIT

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 4 Sept 2026. Prepared record publication-23773153-2026-09-04.2. Manifest publication-graph-cohort-2026-09-04.2.

Source receipt: PubMed via Helena Literature Corpus, retrieved 4 Sept 2026.

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