Ontology highlight
ABSTRACT:
SUBMITTER: Zhou H
PROVIDER: S-EPMC5658359 | biostudies-literature | 2017 Oct
REPOSITORIES: biostudies-literature
Nature communications 20171027 1
The Cullin-RING E3 ubiquitin ligases (CRLs) regulate homeostasis of ~20% of cellular proteins and their activation require neddylation of their cullin subunit. Cullin neddylation is modulated by a scaffolding DCN protein through interactions with both the cullin protein and an E2 enzyme such as UBC12. Here we report the development of DI-591 as a high-affinity, cell-permeable small-molecule inhibitor of the DCN1-UBC12 interaction. DI-591 binds to purified recombinant human DCN1 and DCN2 proteins ...[more]