Structural basis of GC-1 selectivity for thyroid hormone receptor isoforms

Lucas Bleicher, Ricardo Aparicio, Fabio M. Nunes, Leandro Martinez, Sandra M. Gomes Dias, Ana Carolina Migliorini Figueira, Maria Auxiliadora Morim Santos, Walter H. Venturelli, Rosangela Da Silva, Paulo Marcos Donate, Francisco A.R. Neves, Luiz A. Simeoni, John D. Baxter, Paul Webb, Munir S. Skaf, Igor Polikarpov

Research output: Contribution to journalArticle

40 Scopus citations

Abstract

Background. Thyroid receptors, TRα and TRβ, 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 TRβ isoform activation, TRα activation affects heart rates. Therefore, β-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

Original languageEnglish (US)
Article number8
JournalBMC Structural Biology
Volume8
DOIs
StatePublished - 2008

ASJC Scopus subject areas

  • Structural Biology

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