2LBD

LIGAND-BINDING DOMAIN OF THE HUMAN RETINOIC ACID RECEPTOR GAMMA BOUND TO ALL-TRANS RETINOIC ACID

2LBD の概要

• エントリーDOI: 10.2210/pdb2lbd/pdb
• 分子名称: RETINOIC ACID RECEPTOR GAMMA, RETINOIC ACID (3 entities in total)
• 機能のキーワード: nuclear receptor, retinoic acid receptor, all-trans retinoic acid, ligand-binding domain, complex, holo form, transcription regulation, ligand-dependent, active conformation, structural proteomics in europe, spine, structural genomics
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 30493.49

構造登録者

Renaud, J.-P.,Rochel, N.,Ruff, M.,Moras, D.,Structural Proteomics in Europe (SPINE) (登録日: 1997-08-19, 公開日: 1997-11-12, 最終更新日: 2024-02-21)

主引用文献

Renaud, J.P.,Rochel, N.,Ruff, M.,Vivat, V.,Chambon, P.,Gronemeyer, H.,Moras, D.
Crystal structure of the RAR-gamma ligand-binding domain bound to all-trans retinoic acid.
Nature, 378:681-689, 1995

PubMed Abstract: The 2.0-A crystal structure of the ligand-binding domain (LBD) 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 LBD 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.

PubMed: 7501014
DOI: 10.1038/378681a0

実験手法

X-RAY DIFFRACTION (2.06 Å)