Nuclear receptor antagonists designed based on the helix-folding inhibition hypothesis

Nuclear receptor antagonists designed based on the helix-folding inhibition hypothesis
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DOI:
10.1016/j.bmc.2005.03.027
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发表时间:
2005-09-01
影响因子:
3.5
通讯作者:
Miyachi, H
Miyachi, H
中科院分区:
医学3区
文献类型:
--
作者:
Hashimoto, Y;Miyachi, H

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在这里,我们回顾了我们的研究,包括视黄酸受体(RAR)拮抗剂,维甲酸X受体(RXR)拮抗剂,雄激素受体(AR)拮抗剂,维生素D受体(VDR)拮抗剂的分子设计的基础上,抑制折叠的螺旋12,其中包含一个辅激活剂结合位点。对过氧化物酶体增殖物激活受体(PPAR)配体的结构研究进展进行了综述。(c)2005爱思唯尔有限公司保留所有权利。
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.