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 language | English (US) |
|---|---|
| Pages (from-to) | 154-157 |
| Number of pages | 4 |
| Journal | Trends in Endocrinology and Metabolism |
| Volume | 15 |
| Issue number | 4 |
| DOIs | |
| State | Published - May 2004 |
| Externally published | Yes |
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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 journal › Article
}
TY - JOUR
T1 - Selective activation of thyroid hormone signaling pathways by GC-1
T2 - A new approach to controlling cholesterol and body weight
AU - Baxter, John D.
AU - Webb, Paul
AU - Grover, Gary
AU - Scanlan, Thomas (Tom)
PY - 2004/5
Y1 - 2004/5
N2 - 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.
AB - 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.
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UR - http://www.scopus.com/inward/citedby.url?scp=1942453725&partnerID=8YFLogxK
U2 - 10.1016/j.tem.2004.03.008
DO - 10.1016/j.tem.2004.03.008
M3 - Article
C2 - 15109613
AN - SCOPUS:1942453725
VL - 15
SP - 154
EP - 157
JO - Trends in Endocrinology and Metabolism
JF - Trends in Endocrinology and Metabolism
SN - 1043-2760
IS - 4
ER -