Design and characterization of a thyroid hormone receptor alpha (TRalpha)-specific agonist.

Cory A. Ocasio, Thomas (Tom) Scanlan

Research output: Contribution to journalArticle

36 Citations (Scopus)

Abstract

Thyroid hormone is a classical endocrine signaling molecule that regulates a diverse array of physiological processes ranging from energy metabolism to cardiac performance. The active form of thyroid hormone, 3,5,3'-triiodo- l -thyronine or T 3 , exerts many of its actions through its receptor, the thyroid hormone receptor (TR), of which there are two subtypes for two isoforms: TRalpha 1 , TRalpha 2 , TRbeta 1 , and TRbeta 2 . Although TR isoforms, with the exception of TRbeta 2 , are expressed in all tissues, they display different patterns of expression in different tissues, giving rise to tissue-specific isoform actions. Currently, several TRbeta-selective agonists have been developed; however, TRalpha-selective agonists have remained elusive. Herein, we report the synthesis and biological evaluation of CO23, the first potent thyromimetic with TRalpha-specific effects in vitro and in vivo .

Original languageEnglish (US)
Pages (from-to)585-593
Number of pages9
JournalACS Chemical Biology
Volume1
Issue number9
DOIs
StatePublished - Oct 24 2006
Externally publishedYes

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Thyroid Hormone Receptors alpha
Thyroid Hormone Receptors
Protein Isoforms
Tissue
Thyroid Hormones
Thyronines
Physiological Phenomena
Energy Metabolism
Molecules

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine

Cite this

Design and characterization of a thyroid hormone receptor alpha (TRalpha)-specific agonist. / Ocasio, Cory A.; Scanlan, Thomas (Tom).

In: ACS Chemical Biology, Vol. 1, No. 9, 24.10.2006, p. 585-593.

Research output: Contribution to journalArticle

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