Department of Chemistry and Chemical Biology, Northeastern University, 360 Huntington Avenue, Boston, MA 02115, USA.
Bioorg Med Chem Lett. 2012 Nov 1;22(21):6587-90. doi: 10.1016/j.bmcl.2012.09.007. Epub 2012 Sep 13.
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.
一系列双极性联苯化合物被合成，作为负责与核激素受体共激活剂结合域结合的共激活蛋白的 LXXLL 五肽基序的蛋白质模拟物类似物。这些化合物经过多种体外测定来评估它们作为竞争性结合抑制剂的有效性。这项初步研究的结果表明，这些蛋白质模拟物具有抑制这种蛋白质-蛋白质相互作用的能力。
