Ontology highlight
ABSTRACT:
SUBMITTER: Martin MP
PROVIDER: S-EPMC3846258 | biostudies-literature | 2013 Nov
REPOSITORIES: biostudies-literature
Martin Mathew P MP Olesen Sanne H SH Georg Gunda I GI Schönbrunn Ernst E
ACS chemical biology 20130910 11
Bromodomain-containing proteins are considered atypical kinases, but their potential to interact with kinase inhibitors is unknown. Dinaciclib is a potent inhibitor of cyclin-dependent kinases (CDKs), which recently advanced to Phase III clinical trials for the treatment of leukemia. We determined the crystal structure of dinaciclib in complex with CDK2 at 1.7 Å resolution, revealing an elaborate network of binding interactions in the ATP site, which explains the extraordinary potency and select ...[more]