Article
Discovery of FLT3-targeting PROTACs with potent antiproliferative activity against acute myeloid leukemia cells harboring FLT3 mutations.
European journal of medicinal chemistry - 15 Mar 2024
Wang Zhijie, Lu Xun, Liu Canlin, Huang Fei, Lu Tao, Chen Yadong, Liu Lifei, Lu Shuai
Abstract excerpt
Acute myeloid leukemia (AML) patients harboring Fms-like tyrosine kinase 3 (FLT3) mutations often suffer from poor prognosis and relapse. Targeted protein degradation utilizing proteolysis targeting chimeras (PROTACs) is considered as a novel therapeutic strategy in drug discovery and may be a promising modality to target FLT3 mutations for the development of potent anti-AML drugs. Herein, a kind of...
Topics
- Humans
- fms-Like Tyrosine Kinase 3
- Proteolysis
- Leukemia, Myeloid, Acute
- Apoptosis
- Mutation
- Cell Line, Tumor
- Protein Kinase Inhibitors