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

Publication ,  Journal Article
Weiser, PT; Williams, AB; Chang, C-Y; McDonnell, DP; Hanson, RN
Published in: Bioorg Med Chem Lett
November 1, 2012

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.

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Published In

Bioorg Med Chem Lett

DOI

EISSN

1464-3405

Publication Date

November 1, 2012

Volume

22

Issue

21

Start / End Page

6587 / 6590

Location

England

Related Subject Headings

  • Protein Binding
  • Nuclear Receptor Coactivators
  • Nuclear Receptor Coactivator 2
  • Molecular Structure
  • Medicinal & Biomolecular Chemistry
  • Humans
  • Female
  • Estrogen Receptor alpha
  • Cell Line, Tumor
  • Biphenyl Compounds
 

Citation

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Weiser, P. T., Williams, A. B., Chang, C.-Y., McDonnell, D. P., & Hanson, R. N. (2012). 3,3'-Disubstituted bipolar biphenyls as inhibitors of nuclear receptor coactivator binding. Bioorg Med Chem Lett, 22(21), 6587–6590. https://doi.org/10.1016/j.bmcl.2012.09.007
Weiser, Patrick T., Anna B. Williams, Ching-Yi Chang, Donald P. McDonnell, and Robert N. Hanson. “3,3'-Disubstituted bipolar biphenyls as inhibitors of nuclear receptor coactivator binding.Bioorg Med Chem Lett 22, no. 21 (November 1, 2012): 6587–90. https://doi.org/10.1016/j.bmcl.2012.09.007.
Weiser PT, Williams AB, Chang C-Y, McDonnell DP, Hanson RN. 3,3'-Disubstituted bipolar biphenyls as inhibitors of nuclear receptor coactivator binding. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6587–90.
Weiser, Patrick T., et al. “3,3'-Disubstituted bipolar biphenyls as inhibitors of nuclear receptor coactivator binding.Bioorg Med Chem Lett, vol. 22, no. 21, Nov. 2012, pp. 6587–90. Pubmed, doi:10.1016/j.bmcl.2012.09.007.
Weiser PT, Williams AB, Chang C-Y, McDonnell DP, Hanson RN. 3,3'-Disubstituted bipolar biphenyls as inhibitors of nuclear receptor coactivator binding. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6587–6590.
Journal cover image

Published In

Bioorg Med Chem Lett

DOI

EISSN

1464-3405

Publication Date

November 1, 2012

Volume

22

Issue

21

Start / End Page

6587 / 6590

Location

England

Related Subject Headings

  • Protein Binding
  • Nuclear Receptor Coactivators
  • Nuclear Receptor Coactivator 2
  • Molecular Structure
  • Medicinal & Biomolecular Chemistry
  • Humans
  • Female
  • Estrogen Receptor alpha
  • Cell Line, Tumor
  • Biphenyl Compounds