3HZF

Structure of TR-alfa bound to selective thyromimetic GC-1 in C2 space group

3HZF の概要

• エントリーDOI: 10.2210/pdb3hzf/pdb
• 分子名称: Thyroid hormone receptor, alpha isoform 1 variant, {4-[4-hydroxy-3-(1-methylethyl)benzyl]-3,5-dimethylphenoxy}acetic acid (3 entities in total)
• 機能のキーワード: nuclear receptor, ligand binding domain, dna-binding, metal-binding, nucleus, receptor, transcription, transcription regulation, zinc-finger
• 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: 31334.61

構造登録者

Aparicio, R.,Bleicher, L.,Polikarpov, I. (登録日: 2009-06-23, 公開日: 2009-07-21, 最終更新日: 2024-11-20)

主引用文献

Bleicher, L.,Aparicio, R.,Nunes, F.M.,Martinez, L.,Gomes Dias, S.M.,Figueira, A.C.,Santos, M.A.,Venturelli, W.H.,da Silva, R.,Donate, P.M.,Neves, F.A.,Simeoni, L.A.,Baxter, J.D.,Webb, P.,Skaf, M.S.,Polikarpov, I.
Structural basis of GC-1 selectivity for thyroid hormone receptor isoforms.
Bmc Struct.Biol., 8:8-8, 2008

PubMed Abstract: Thyroid receptors, TRalpha and TRbeta, are involved in important physiological functions such as metabolism, cholesterol level and heart activities. Whereas metabolism increase and cholesterol level lowering could be achieved by TRbeta isoform activation, TRalpha activation affects heart rates. Therefore, beta-selective thyromimetics have been developed as promising drug-candidates for treatment of obesity and elevated cholesterol level. GC-1 [3,5-dimethyl-4-(4'-hydroxy-3'-isopropylbenzyl)-phenoxy acetic acid] has ability to lower LDL cholesterol with 600- to 1400-fold more potency and approximately two- to threefold more efficacy than atorvastatin (Lipitor(c)) in studies in rats, mice and monkeys.

PubMed: 18237438
DOI: 10.1186/1472-6807-8-8

実験手法

X-RAY DIFFRACTION (2.5 Å)