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Article

Targeting AML-associated FLT3 mutations with a type I kinase inhibitor.

The Journal of clinical investigation - 1 Apr 2020

Jones LaQuita M, Melgar Katelyn, Bolanos Lyndsey, Hueneman Kathleen, Walker Morgan M, Jiang Jian-Kang, Wilson Kelli M, Zhang Xiaohu, Shen Jian, Jiang Fan, Sutter Patrick, Wang Amy, Xu Xin, Tawa Gregory J, Hoyt Scott B, Wunderlich Mark, O'Brien Eric, Perentesis John P, Starczynowski Daniel T, Thomas Craig J

Abstract excerpt

Tyrosine kinase domain (TKD) mutations contribute to acquired resistance to FMS-like tyrosine kinase 3 (FLT3) inhibitors used to treat FLT3-mutant acute myeloid leukemia (AML). We report a cocrystal structure of FLT3 with a type I inhibitor, NCGC1481, that retained potent binding and activity against FLT3 TKD and gatekeeper mutations. Relative to the current generation of advanced FLT3 inhibitors, NCGC1481...

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Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

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Identifiers

PMID: 32149729
DOI: 10.1172/JCI127907
PMCID: PMC7108888

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