3FC6

hRXRalpha & mLXRalpha with an indole Pharmacophore, SB786875

3FC6 の概要

• エントリーDOI: 10.2210/pdb3fc6/pdb
• 分子名称: Retinoic acid receptor RXR-alpha, Nr1h3 protein, RETINOIC ACID, ... (5 entities in total)
• 機能のキーワード: liver x receptor, nuclear hormone receptors, agonists, epoxycholesterol, dna-binding, host-virus interaction, metal-binding, nucleus, polymorphism, receptor, transcription, transcription regulation, ubl conjugation, zinc, zinc-finger
• 由来する生物種: Homo sapiens (human); 詳細
• 細胞内の位置: Nucleus: P19793
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 117308.05

構造登録者

Washburn, D.G.,Hoang, T.H.,Campobasso, N.,Smallwood, A.,Parks, D.J.,Webb, C.L.,Frank, K.,Nord, M.,Duraiswami, C.,Evans, C.,Jaye, M.,Thompson, S.K. (登録日: 2008-11-21, 公開日: 2009-02-10, 最終更新日: 2023-12-27)

主引用文献

Washburn, D.G.,Hoang, T.H.,Campobasso, N.,Smallwood, A.,Parks, D.J.,Webb, C.L.,Frank, K.A.,Nord, M.,Duraiswami, C.,Evans, C.,Jaye, M.,Thompson, S.K.
Synthesis and SAR of potent LXR agonists containing an indole pharmacophore.
Bioorg.Med.Chem.Lett., 19:1097-1100, 2009

PubMed Abstract: A novel series of 1H-indol-1-yl tertiary amine LXR agonists has been designed. Compounds from this series were potent agonists with good rat pharmacokinetic parameters. In addition, the crystal structure of an LXR agonist bound to LXRalpha will be disclosed.

PubMed: 19167885
DOI: 10.1016/j.bmcl.2009.01.004

実験手法

X-RAY DIFFRACTION (2.063 Å)