Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

Lessons from Structural Biology for Understanding Drug Resistance in Gastrointestinal Stromal Tumors (GIST).

Journal of medicinal chemistry - 12 Mar 2026

Mancino Giorgia, Schulz Tom, Scrima Andrea, Müller Matthias P, Bauer Sebastian, Rauh Daniel

Abstract excerpt

Gastrointestinal stromal tumors (GISTs) are primarily driven by activating mutations in the receptor tyrosine kinases KIT or PDGFRA. Targeted therapies have significantly improved patient outcomes; however, acquired drug resistance continues to limit long-term efficacy. Secondary and tertiary mutations across distinct regions of the kinase domain affect the conformational equilibrium or directly disrupt drug...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Antineoplastic Agents
Share to Drug Resistance, Neoplasm

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Gastrointestinal Neoplasms

Share to Gastrointestinal Stromal Tumors

Share to Models, Molecular

Share to Protein Kinase Inhibitors

Share to Proto-Oncogene Proteins c-kit

Share to Receptor, Platelet-Derived Growth Factor alpha

Source

Identifiers

PMID: 41770641
DOI: 10.1021/acs.jmedchem.5c03702

Genes

KIT
PDGFRA

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 2 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Lessons from Structural Biology for Understanding Drug Resistance in Gastrointestinal Stromal Tumors (GIST).PMID 41770641Read ↗

Gastrointestinal Stromal Tumors: Molecular Mechanisms of Drug Resistance and Advances in Therapeutic Strategies.Semantic proximity Read ↗

Current Drug Resistance Mechanisms and Treatment Options in Gastrointestinal Stromal Tumors: Summary and Update.Semantic proximity Read ↗

Molecular Advances in the Treatment of Advanced Gastrointestinal Stromal Tumor.Semantic proximity Read ↗

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

Resistance to Tyrosine Kinase Inhibitors in Gastrointestinal Stromal TumorsSemantic proximity Read ↗

Targeted Therapy for Advanced Gastrointestinal Stromal Tumors: Evolution and Future Directions.Semantic proximity Read ↗

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

Targeted therapy and personalized medicine in gastrointestinal stromal tumors: drug resistance, mechanisms, and treatment strategiesSemantic proximity Read ↗

[Drug resistance mechanism and new therapy strategy progression in targeted treatment of gastrointestinal stromal tumors].Semantic proximity Read ↗

Targeting gain of function and resistance mutations in Abl and KIT by hybrid compound design.Semantic proximity Read ↗

Molecular basis for primary and secondary tyrosine kinase inhibitor resistance in gastrointestinal stromal tumor.Semantic proximity Read ↗

New targets and therapies for gastrointestinal stromal tumors.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.