Ontology highlight
ABSTRACT:
SUBMITTER: Brand M
PROVIDER: S-EPMC6444916 | biostudies-literature | 2019 Feb
REPOSITORIES: biostudies-literature
Cell chemical biology 20181227 2
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 immed ...[more]