| Literature DB >> 25637122 |
Takashi Misawa1, Yosuke Demizu2, Megumi Kawamura3, Nanako Yamagata1, Masaaki Kurihara4.
Abstract
We developed several stabilized helical heptapeptides (DPI-01-10) composed of l-leucine residues, an α,α-disubstituted α-amino acid (α-aminoisobutyric acid [Aib] or hydroxymethylserine [Hms]), and a stapled side chain as inhibitors of vitamin D receptor (VDR)-coactivator interactions. The inhibitory activity of these peptides against VDR-coactivator interactions was evaluated using a receptor cofactor assay system, and DPI-08 demonstrated strong activity (IC50: 3.2μM).Entities:
Keywords: Helical structure; Protein–protein interaction; Stapled peptide; Vitamin D receptor
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Year: 2015 PMID： 25637122 DOI： 10.1016/j.bmc.2015.01.007
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641