4,4'-Unsymmetrically substituted 3,3'-biphenyl alpha helical proteomimetics as potential coactivator binding inhibitors.


Journal Article

A series of unsymmetrically substituted biphenyl compounds was designed as alpha helical proteomimetics with the aim of inhibiting the binding of coactivator proteins to the nuclear hormone receptor coactivator binding domain. These compounds were synthesized in good overall yields in seven steps starting from 2-bromoanisole. The final products were evaluated using cotransfection reporter gene assays and mammalian two-hybrid competitive inhibition assays to demonstrate their effectiveness as competitive binding inhibitors. The results from this study indicate that these proteomimetics possess the ability to inhibit coactivator-receptor interactions, but via a mixed mode of inhibition.

Full Text

Duke Authors

Cited Authors

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

Published Date

  • January 15, 2014

Published In

Volume / Issue

  • 22 / 2

Start / End Page

  • 917 - 926

PubMed ID

  • 24360824

Pubmed Central ID

  • 24360824

Electronic International Standard Serial Number (EISSN)

  • 1464-3391

Digital Object Identifier (DOI)

  • 10.1016/j.bmc.2013.10.051


  • eng

Conference Location

  • England