Ontology highlight
ABSTRACT:
SUBMITTER: Butler KV
PROVIDER: S-EPMC5148670 | biostudies-literature | 2016 Nov
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20161102 21
Selective inhibitors of protein lysine methyltransferases, including SET domain-containing protein 8 (SETD8), are highly desired, as only a fraction of these enzymes are associated with high-quality inhibitors. From our previously discovered SETD8 inhibitor, we developed a more potent analog and solved a cocrystal structure, which is the first crystal structure of SETD8 in complex with a small-molecule inhibitor. This cocrystal structure allowed the design of a covalent inhibitor of SETD8 (MS453 ...[more]