3,3'-Disubstituted bipolar biphenyls as inhibitors of nuclear receptor coactivator binding.

Journal Article (Journal Article)

A series of bipolar biphenyl compounds was synthesized as proteomimetic analogs of the LXXLL penta-peptide motif responsible for the binding of coactivator proteins to the nuclear hormone receptor coactivator binding domain. These compounds were subjected to multiple in vitro assays to evaluate their effectiveness as competitive binding inhibitors. The results from this initial study indicate that these proteomimetics possess the ability to inhibit this protein-protein interaction.

Full Text

Duke Authors

Cited Authors

  • Weiser, PT; Williams, AB; Chang, C-Y; McDonnell, DP; Hanson, RN

Published Date

  • November 1, 2012

Published In

Volume / Issue

  • 22 / 21

Start / End Page

  • 6587 - 6590

PubMed ID

  • 23017882

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2012.09.007


  • eng

Conference Location

  • England