Nuclear receptor antagonists designed based on the helix-folding inhibition hypothesis |
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| Authors: | Hashimoto Yuichi Miyachi Hiroyuki |
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| Institution: | Institute of Molecular & Cellular Biosciences, The University of Tokyo, 1-1-1 Yayoi, Bunkyo-ku, Tokyo 113-0032, Japan. bmcyfh@iam.u-tokyo.ac.jp |
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| Abstract: | Here we review our studies on the molecular design of nuclear receptor antagonists, including retinoic acid receptor (RAR) antagonists, retinoid X receptor (RXR) antagonists, androgen receptor (AR) antagonists, and vitamin D receptor (VDR) antagonists, based on inhibition of folding of helix 12, which contains a co-activator binding site. Recent progress in structural development studies of peroxisome proliferator-activated receptor (PPAR) ligands is also reviewed. |
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