ATP-Competitive Inhibitors Midostaurin and Avapritinib Have Distinct Resistance Profiles in Exon 17-Mutant KIT.

doi:10.1158/0008-5472.CAN-18-3139

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Article

ATP-Competitive Inhibitors Midostaurin and Avapritinib Have Distinct Resistance Profiles in Exon 17-Mutant KIT.

Cancer research - 15 Aug 2019

Apsel Winger Beth, Cortopassi Wilian A, Garrido Ruiz Diego, Ding Lucky, Jang Kibeom, Leyte-Vidal Ariel, Zhang Na, Esteve-Puig Rosaura, Jacobson Matthew P, Shah Neil P

Abstract excerpt

KIT is a type-3 receptor tyrosine kinase that is frequently mutated at exon 11 or 17 in a variety of cancers. First-generation KIT tyrosine kinase inhibitors (TKI) are ineffective against KIT exon 17 mutations, which favor an active conformation that prevents these TKIs from binding. The ATP-competitive inhibitors, midostaurin and avapritinib, which target the active kinase conformation, were developed to inhibit...

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Topics

Antineoplastic Agents
Cell Line
Drug Resistance, Neoplasm
Exons
Humans
Molecular Docking Simulation

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

Molecular Dynamics Simulation

Mutation

Protein Kinase Inhibitors

Proto-Oncogene Proteins c-kit

Pyrazoles

Pyrroles

Staurosporine

Triazines

Avapritinib

Source

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Identifiers

PMID: 31270078
DOI: 10.1158/0008-5472.CAN-18-3139
PMCID: PMC6697585

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