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 Cited by 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: 18237438DOI: 10.1186/1472-6807-8-8 PDB entries with the same primary citation |
| Experimental method | X-RAY DIFFRACTION (1.85 Å) |
Structure validation
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