3ILZ

Structure of TR-alfa bound to selective thyromimetic GC-1 in P212121 space group

Summary for 3ILZ

• Entry DOI: 10.2210/pdb3ilz/pdb
• Descriptor: Thyroid hormone receptor, alpha isoform 1 variant, {4-[4-hydroxy-3-(1-methylethyl)benzyl]-3,5-dimethylphenoxy}acetic acid (3 entities in total)
• Functional Keywords: nuclear receptor, signaling protein
• Biological source: Homo sapiens (human)
• Total number of polymer chains: 1
• Total formula weight: 31106.35

Authors

Aparicio, R.,Polikarpov, L.,Bleicher, L. (deposition date: 2009-08-07, release date: 2010-04-28, Last modification date: 2024-10-16)

Primary citation

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

Experimental method

X-RAY DIFFRACTION (1.85 Å)