作者
Matthias Brand, Baishan Jiang, Sophie Bauer, Katherine A Donovan, Yanke Liang, Eric S Wang, Radosław P Nowak, Jingting C Yuan, Tinghu Zhang, Nicholas Kwiatkowski, André C Müller, Eric S Fischer, Nathanael S Gray, Georg E Winter
发表日期
2019/2/21
期刊
Cell chemical biology
卷号
26
期号
2
页码范围
300-306. e9
出版商
Elsevier
简介
The design of selective small molecules is often stymied by similar ligand binding pockets. Here, we report BSJ-03-123, a phthalimide-based degrader that exploits protein-interface determinants to achieve proteome-wide selectivity for the degradation of cyclin-dependent kinase 6 (CDK6). Pharmacologic CDK6 degradation targets a selective dependency of acute myeloid leukemia cells, and transcriptomics and phosphoproteomics profiling of acute degradation of CDK6 enabled dynamic mapping of its immediate role in coordinating signaling and transcription.
学术搜索中的文章
M Brand, B Jiang, S Bauer, KA Donovan, Y Liang… - Cell chemical biology, 2019