Article

Structure-based Scaffold Hopping Reveals Strategies to Overcome Oncogenic KIT and PDGFRA Mutation-Driven Drug-Resistance in GIST

2026-01-07

Abstract excerpt

<title>Abstract</title> <p> 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 dive...

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Literature Corpus work: 30820c85-3e2c-53ac-a0b4-966b55b12ea6
DOI: 10.21203/rs.3.rs-8307571/v1

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