Structure–activity relationship of benzodiazepine derivatives as LXXLL peptide mimetics that inhibit the interaction of vitamin D receptor with coactivators

…, T Noguchi-Yachide, Y Hashimoto, M Ishikawa

Index: Mita, Yusuke; Dodo, Kosuke; Noguchi-Yachide, Tomomi; Hashimoto, Yuichi; Ishikawa, Minoru Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 4 p. 993 - 1005

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Citation Number: 13

Abstract

Suppression of vitamin D receptor (VDR)-mediated transcription is expected to be of therapeutic value in Paget's disease of bone. It is known that interaction between VDR and coactivators is necessary for VDR transactivation, and the interaction occurs when VDR recognizes an LXXLL peptide motif of coactivators. We previously reported that benzodiazepine derivatives designed as LXXLL peptide mimetics inhibited the interaction ...