Ontology highlight
ABSTRACT:
SUBMITTER: Zorn JA
PROVIDER: S-EPMC4383440 | biostudies-literature | 2015
REPOSITORIES: biostudies-literature
Zorn Julie A JA Wang Qi Q Fujimura Eric E Barros Tiago T Kuriyan John J
PloS one 20150402 4
More than 30% of acute myeloid leukemia (AML) patients possess activating mutations in the receptor tyrosine kinase FMS-like tyrosine kinase 3 or FLT3. A small-molecule inhibitor of FLT3 (known as quizartinib or AC220) that is currently in clinical trials appears promising for the treatment of AML. Here, we report the co-crystal structure of the kinase domain of FLT3 in complex with quizartinib. FLT3 with quizartinib bound adopts an "Abl-like" inactive conformation with the activation loop stabi ...[more]