The retinoid X receptors and their ligands.
The retinoid X receptors and their ligands.
复制标题
类维生素X受体及其配体。
DOI：
10.1016/j.bbalip.2011.09.014
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发表时间：
2012-01
期刊：
影响因子：
--
通讯作者：
Xia Z
中科院分区：
文献类型：
--
作者：
Dawson MI;Xia Z
本章概述了类视黄醇 X 受体亚型 α、β 和 γ（RXR、NR2B1-3）的结构和分子生物学、其核和细胞质功能、转录后加工以及最近报道的配体的研究现状。感兴趣的点是不同形状的激动剂诱导的配体结合口袋的不同变化，配体结合口袋与共激活剂结合表面和异二聚化界面的通讯，以及最近鉴定的天然产物配体，那些最初设计为与其他靶标相互作用的环境毒素或药物，以及那些被故意设计为RXR选择性转录的配体 激动剂、协同剂或拮抗剂。在这些合成配体中，设计的总体趋势似乎是从完全芳香族刚性结构转向含有9-顺式视黄酸柔性四烯侧链部分元素的结构。
This chapter presents an overview of the current status of studies on the structural and molecular biology of the retinoid X receptor subtypes α, β, and γ (RXRs, NR2B1–3), their nuclear and cytoplasmic functions, post-transcriptional processing, and recently reported ligands. Points of interest are the different changes in the ligand-binding pocket induced by variously shaped agonists, the communication of the ligand–bound pocket with the coactivator binding surface and the heterodimerization interface, and recently identified ligands that are natural products, those that function as environmental toxins or drugs that had been originally designed to interact with other targets, as well as those that were deliberately designed as RXR-selective transcriptional agonists, synergists, or antagonists. Of these synthetic ligands, the general trend in design appears to be away from fully aromatic rigid structures to those containing partial elements of the flexible tetraene side chain of 9-cis-retinoic acid.
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影响因子：
2.9
作者：
Borel, Franck;de Groot, Arian;Ferrer, Jean-Luc
通讯作者：
Ferrer, Jean-Luc
影响因子：
4.8
作者：
Bastien, J;Adam-Stitah, S;Rochette-Egly, C
通讯作者：
Rochette-Egly, C
影响因子：
4.4
作者：
ALMASAN, A;MANGELSDORF, DJ;EVANS, RM
通讯作者：
EVANS, RM
影响因子：
4.8
作者：
Browning, Christopher;Martin, Elyette;Billas, Isabelle M. L.
通讯作者：
Billas, Isabelle M. L.
影响因子：
2.7
作者：
Bishop-Bailey, David
通讯作者：
Bishop-Bailey, David