Selective activation of thyroid hormone signaling pathways by GC-1

A new approach to controlling cholesterol and body weight

John D. Baxter, Paul Webb, Gary Grover, Thomas (Tom) Scanlan

Research output: Contribution to journalArticle

90 Citations (Scopus)

Abstract

The current report describes progress in development of a selective thyroid hormone receptor modulator, GC-1. This compound binds selectively to the β-isoform of the thyroid hormone receptor, and its uptake into the heart is relatively low. Studies in rats, mice and monkeys show that GC-1 lowers cholesterol with 600- to 1400-fold more potency and approximately two- to threefold more efficacy than atorvastatin, a compound that blocks HMG-CoA reductase. GC-1 also decreases plasma levels of triglyceride and lipoprotein (a), and induces loss of fat. These effects can be observed under conditions where there is either no or minimal effect on heart rate, and no detectable loss of muscle. Although more study is required, compounds of this class deserve further investigation for treating lipid disorders and obesity.

Original languageEnglish (US)
Pages (from-to)154-157
Number of pages4
JournalTrends in Endocrinology and Metabolism
Volume15
Issue number4
DOIs
StatePublished - May 2004
Externally publishedYes

Fingerprint

Thyroid Hormones
Thyroid Hormone Receptors
Cholesterol
Body Weight
Hydroxymethylglutaryl CoA Reductases
Lipoprotein(a)
Haplorhini
Protein Isoforms
Triglycerides
Obesity
Heart Rate
Fats
Lipids
Muscles
GC 1 compound

ASJC Scopus subject areas

  • Endocrinology
  • Endocrinology, Diabetes and Metabolism

Cite this

Selective activation of thyroid hormone signaling pathways by GC-1 : A new approach to controlling cholesterol and body weight. / Baxter, John D.; Webb, Paul; Grover, Gary; Scanlan, Thomas (Tom).

In: Trends in Endocrinology and Metabolism, Vol. 15, No. 4, 05.2004, p. 154-157.

Research output: Contribution to journalArticle

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