CRYSTAL-STRUCTURE OF THE RAR-GAMMA LIGAND-BINDING DOMAIN BOUND TO ALL-TRANS-RETINOIC ACID

被引：985

作者：

RENAUD, JP ^{[1
]}

ROCHEL, N ^{[1
]}

RUFF, M ^{[1
]}

VIVAT, V ^{[1
]}

CHAMBON, P ^{[1
]}

GRONEMEYER, H ^{[1
]}

MORAS, D ^{[1
]}

机构：

[1] UNIV STRASBOURG 1,COLL FRANCE,CNRS,INSERM,INST GENET & BIOL MOLEC & CELLULAIRE,F-67404 ILLKIRCH GRAFFENS,FRANCE

来源：

NATURE | 1995年 / 378卷 / 6558期

关键词：

D O I：

10.1038/378681a0

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

The 2.0-Angstrom crystal structure of the ligand-binding domain (LED) of the human retinoic acid receptor (RAR)-gamma bound to all-trans retinoic acid reveals the ligand-binding interactions and suggests an electrostatic guidance mechanism. The overall fold is similar to that of the human RXR-alpha apo-LBD, except for the carboxy-terminal part which folds back towards the LED core, contributing to the hydrophobic ligand pocket and 'sealing' its entry site. We propose a 'mouse trap' mechanism whereby a ligand-induced conformational transition repositions the amphipathic alpha-helix of the AF-2 activating domain and forms a transcriptionally active receptor.

引用

页码：681 / 689

页数：9

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