Article
Catalytic Degraders Effectively Address Kinase Site Mutations in EML4-ALK Oncogenic Fusions.
Journal of medicinal chemistry - 27 Apr 2023
Gao Yang, Jiang Baishan, Kim Hellen, Berberich Matthew J, Che Jianwei, Donovan Katherine A, Hatcher John M, Huerta Fidel, Kwiatkowski Nicholas P, Liu Yingpeng, Liuni Peter P, Metivier Rebecca J, Murali Vineeth K, Nowak Radosław P, Zhang Tinghu, Fischer Eric S, Gray Nathanael S, Jones Lyn H
Abstract excerpt
Heterobifunctional degraders, known as proteolysis targeting chimeras (PROTACs), theoretically possess a catalytic mode-of-action, yet few studies have either confirmed or exploited this potential advantage of event-driven pharmacology. Degraders of oncogenic EML4-ALK fusions were developed by conjugating ALK inhibitors to cereblon ligands. Simultaneous optimization of pharmacology and compound properties using...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.