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Article

Structure-based scaffold hopping reveals strategies to overcome oncogenic KIT and PDGFRA mutation-driven drug-resistance in GIST.

Nature communications - 6 Aug 2026

Schulz T, Beerbaum M, Scrima A, Jantzen H, Teuber A, Mühlenberg T, Ebel L, Garcia-Fossa F, George A, Berner N, Weisner J, Müller M P, Wilhelm S, Sievers S, Bauer S, Rauh D

Abstract excerpt

Gastrointestinal stromal tumors (GIST) are the most common mesenchymal tumors of the gastrointestinal tract. Current tyrosine kinase inhibitors (TKIs) targeting oncogenic KIT and PDGFRA have improved patient outcomes, yet off-target toxicities and drug resistance mutations remain major clinical challenges. Many approved TKIs, often repurposed from other cancer indications, harbor diverse hinge-binding motifs that...

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Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

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Share to Proto-Oncogene Proteins c-kit

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Source

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Identifiers

PMID: 42562826
DOI: 10.1038/s41467-026-76340-7
PMCID: PMC13448667

Genes

PDGFRA
KIT

Variants

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 23 Oct 2026.

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Structure-based scaffold hopping reveals strategies to overcome oncogenic KIT and PDGFRA mutation-driven drug-resistance in GIST.PMID 42562826Read ↗

Structure-based Scaffold Hopping Reveals Strategies to Overcome Oncogenic KIT and PDGFRA Mutation-Driven Drug-Resistance in GISTSemantic proximity Read ↗

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