Nuclear receptor antagonists designed based on the helix-folding inhibition hypothesis
Nuclear receptor antagonists designed based on the helix-folding inhibition hypothesis
复制标题
DOI:
10.1016/j.bmc.2005.03.027
复制
发表时间:
2005-09-01
影响因子:
3.5
通讯作者:
Miyachi, H
中科院分区:
文献类型:
--
作者:
Hashimoto, Y;Miyachi, H
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. (c) 2005 Elsevier Ltd. All rights reserved.