Ontology highlight
ABSTRACT:
SUBMITTER: Gunther JR
PROVIDER: S-EPMC2427189 | biostudies-literature | 2008 May
REPOSITORIES: biostudies-literature
Gunther Jillian R JR Moore Terry W TW Collins Margaret L ML Katzenellenbogen John A JA
ACS chemical biology 20080501 5
We report here on the design, synthesis, and evaluation of small molecule inhibitors of the interaction between a steroid receptor coactivator and estrogen receptor alpha. These inhibitors are based upon an amphipathic benzene scaffold whose hydrophobic face mimics the leucine-rich alpha-helical consensus sequence on the steroid receptor coactivators that interacts with a shallow groove on estrogen receptor alpha. Several of these molecules are among the most potent inhibitors of this interactio ...[more]