TY - JOUR
T1 - Selective activators of thyroid hormone receptors
AU - Webb, Paul
PY - 2004/5/1
Y1 - 2004/5/1
N2 - An excess of thyroid hormone (TH) leads to a mix of deleterious (increased heart rate, muscle wasting and osteoporosis) and beneficial effects (reduced serum cholesterol and lipoprotein A and weight loss). All of these actions are mediated by nuclear thyroid hormone receptors (TRs), however, genetic evidence suggests that different TR isoforms do not contribute equally to individual TH effects. Thus, TR isoform selective activators could mimic the beneficial aspects of TH excess while avoiding the harmful effects. This article reviews new selective TR activators, their mechanism of action (they work by targeting the TR-β isoform) and their actions in animal models. It is clear that these compounds represent a promising new avenue for the treatment of lipid disorders and obesity. 2004
AB - An excess of thyroid hormone (TH) leads to a mix of deleterious (increased heart rate, muscle wasting and osteoporosis) and beneficial effects (reduced serum cholesterol and lipoprotein A and weight loss). All of these actions are mediated by nuclear thyroid hormone receptors (TRs), however, genetic evidence suggests that different TR isoforms do not contribute equally to individual TH effects. Thus, TR isoform selective activators could mimic the beneficial aspects of TH excess while avoiding the harmful effects. This article reviews new selective TR activators, their mechanism of action (they work by targeting the TR-β isoform) and their actions in animal models. It is clear that these compounds represent a promising new avenue for the treatment of lipid disorders and obesity. 2004
KW - Cholesterol
KW - Obesity
KW - Selective modulation
KW - Thyroid hormone
UR - http://www.scopus.com/inward/record.url?scp=2642588897&partnerID=8YFLogxK
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U2 - 10.1517/13543784.13.5.489
DO - 10.1517/13543784.13.5.489
M3 - Review article
C2 - 15155124
AN - SCOPUS:2642588897
SN - 1354-3784
VL - 13
SP - 489
EP - 500
JO - Expert Opinion on Investigational Drugs
JF - Expert Opinion on Investigational Drugs
IS - 5
ER -