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

Publication ,  Journal Article
Weiser, PT; Chang, C-Y; McDonnell, DP; Hanson, RN
Published in: Bioorg Med Chem
January 15, 2014

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.

Duke Scholars

Published In

Bioorg Med Chem

DOI

EISSN

1464-3391

Publication Date

January 15, 2014

Volume

22

Issue

2

Start / End Page

917 / 926

Location

England

Related Subject Headings

  • Structure-Activity Relationship
  • Protein Structure, Secondary
  • Protein Binding
  • Nuclear Receptor Coactivators
  • Molecular Structure
  • Models, Molecular
  • Medicinal & Biomolecular Chemistry
  • Humans
  • Hep G2 Cells
  • Dose-Response Relationship, Drug
 

Citation

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Weiser, P. T., Chang, C.-Y., McDonnell, D. P., & Hanson, R. N. (2014). 4,4'-Unsymmetrically substituted 3,3'-biphenyl alpha helical proteomimetics as potential coactivator binding inhibitors. Bioorg Med Chem, 22(2), 917–926. https://doi.org/10.1016/j.bmc.2013.10.051
Weiser, Patrick T., Ching-Yi Chang, Donald P. McDonnell, and Robert N. Hanson. “4,4'-Unsymmetrically substituted 3,3'-biphenyl alpha helical proteomimetics as potential coactivator binding inhibitors.Bioorg Med Chem 22, no. 2 (January 15, 2014): 917–26. https://doi.org/10.1016/j.bmc.2013.10.051.
Weiser PT, Chang C-Y, McDonnell DP, Hanson RN. 4,4'-Unsymmetrically substituted 3,3'-biphenyl alpha helical proteomimetics as potential coactivator binding inhibitors. Bioorg Med Chem. 2014 Jan 15;22(2):917–26.
Weiser, Patrick T., et al. “4,4'-Unsymmetrically substituted 3,3'-biphenyl alpha helical proteomimetics as potential coactivator binding inhibitors.Bioorg Med Chem, vol. 22, no. 2, Jan. 2014, pp. 917–26. Pubmed, doi:10.1016/j.bmc.2013.10.051.
Weiser PT, Chang C-Y, McDonnell DP, Hanson RN. 4,4'-Unsymmetrically substituted 3,3'-biphenyl alpha helical proteomimetics as potential coactivator binding inhibitors. Bioorg Med Chem. 2014 Jan 15;22(2):917–926.
Journal cover image

Published In

Bioorg Med Chem

DOI

EISSN

1464-3391

Publication Date

January 15, 2014

Volume

22

Issue

2

Start / End Page

917 / 926

Location

England

Related Subject Headings

  • Structure-Activity Relationship
  • Protein Structure, Secondary
  • Protein Binding
  • Nuclear Receptor Coactivators
  • Molecular Structure
  • Models, Molecular
  • Medicinal & Biomolecular Chemistry
  • Humans
  • Hep G2 Cells
  • Dose-Response Relationship, Drug