Article
Degrading FLT3-ITD protein by proteolysis targeting chimera (PROTAC).
Bioorganic chemistry - 1 Feb 2022
Chen Yong, Yuan Xue, Tang Minghai, Shi Mingsong, Yang Tao, Liu Kongjun, Deng Dexin, Chen Lijuan
Abstract excerpt
Clinical FLT3 mutations caused poor therapeutic benefits toward the present FLT3 inhibitors, and degradation of the FLT3 mutant protein may be a promising alternative approach to protect against acute myeloid leukemia (AML). Herein, we report the discovery of small molecule FLT3 degraders based on the proteolysis targeting chimera (PROTAC). FLT3 degraders were designed, synthesized, and evaluated for FLT3...
Topics
- Animals
- Antineoplastic Agents
- Cell Line, Tumor
- Cell Proliferation
- Dose-Response Relationship, Drug
- Drug Screening Assays, Antitumor
- Female
- Humans
- Lenalidomide
- Mice
- Mice, Inbred NOD
- Mice, SCID
- Molecular Structure
- Mutation
- Neoplasms, Experimental