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

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 agains...

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Publicat a:J Clin Invest
Autors principals: 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.
Format: Artigo
Idioma:Inglês
Publicat: American Society for Clinical Investigation 2020
Matèries:
Concise Communication
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC7108888/
https://ncbi.nlm.nih.gov/pubmed/32149729
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1172/JCI127907
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