title: 3,3'-Disubstituted bipolar biphenyls as inhibitors of nuclear receptor coactivator binding.
abstract: 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.
authors.affiliation: Department of Chemistry and Chemical Biology, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA.
authors.forename: Patrick T
authors.initials: PT
authors.lastname: Weiser
authors.forename: Anna B
authors.initials: AB
authors.lastname: Williams
authors.forename: Ching-Yi
authors.initials: CY
authors.lastname: Chang
authors.forename: Donald P
authors.initials: DP
authors.lastname: McDonnell
authors.forename: Robert N
authors.initials: RN
authors.lastname: Hanson
mesh_terms: D001665:Binding Sites; D001667:Binding, Competitive; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D047628:Estrogen Receptor alpha / Q000378:metabolism; D005260:Female; D006801:Humans; D015394:Molecular Structure; D051958:Nuclear Receptor Coactivator 2 / Q000378:metabolism; D056918:Nuclear Receptor Coactivators / Q000037:antagonists & inhibitors*; D011485:Protein Binding / Q000187:drug effects
chemical_list: D001713:Biphenyl Compounds; D047628:Estrogen Receptor alpha; D051958:Nuclear Receptor Coactivator 2; D056918:Nuclear Receptor Coactivators