Development of stapled short helical peptides capable of inhibiting vitamin D receptor (VDR)-coactivator interactions

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• 作者：Yosuke Demizu ; Saori Nagoya ; Manami Shirakawa ; Megumi Kawamura ; Nanako Yamagata ; Yukiko Sato ; Mitsunobu Doi ; Masaaki Kurihara
• 关键词：Vitamin D receptor ; VDR&ndash ; coactivator interaction inhibitor ; Stapled helical peptide ; Protein&ndash ; protein interaction
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：1 August, 2013
• 年：2013
• 卷：23
• 期：15
• 页码：4292-4296
• 全文大小：741 K

文摘

We synthesized stapled helical leucine-based peptides (DPI-01-07) containing 2-aminoisobutyric acid and a covalent cross-linked unit as inhibitors of vitamin D receptor (VDR)-coactivator interactions. The effects of these peptides on the human VDR were examined in an inhibition assay based on the receptor cofactor assay system, and one of them, DPI-07, exhibited potent inhibitory activity (IC₅₀: 3.2 ¦ÌM).