Selective activation of thyroid hormone signaling pathways by GC-1: a new approach to controlling cholesterol and body weight.

Article Details

Citation

Baxter JD, Webb P, Grover G, Scanlan TS

Selective activation of thyroid hormone signaling pathways by GC-1: a new approach to controlling cholesterol and body weight.

Trends Endocrinol Metab. 2004 May-Jun;15(4):154-7.

PubMed ID
15109613 [ View in PubMed
]
Abstract

The current report describes progress in development of a selective thyroid hormone receptor modulator, GC-1. This compound binds selectively to the beta-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.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
Atorvastatin3-hydroxy-3-methylglutaryl-coenzyme A reductaseProteinHumans
Yes
Inhibitor
Details