Do peroxisome proliferation receptor-γ antagonists have clinical potential as combined antiobesity and antidiabetic drugs?

Doggrell S. (2003) Do peroxisome proliferation receptor-γ antagonists have clinical potential as combined antiobesity and antidiabetic drugs?. Expert Opinion on Investigational Drugs, 12 4: 713-716. doi:10.1517/eoid.12.4.713.23746


Author Doggrell S.
Title Do peroxisome proliferation receptor-γ antagonists have clinical potential as combined antiobesity and antidiabetic drugs?
Journal name Expert Opinion on Investigational Drugs   Check publisher's open access policy
ISSN 1354-3784
Publication date 2003-04-01
Sub-type Critical review of research, literature review, critical commentary
DOI 10.1517/eoid.12.4.713.23746
Volume 12
Issue 4
Start page 713
End page 716
Total pages 4
Language eng
Subject 3004 Pharmacology
Abstract There is genetic evidence that reducing the activity of peroxisome proliferation receptor-γ (PPAR-γ) may increase insulin sensitivity. SR-202 is a selective antagonist at PPAR-γ, which inhibits the adipocyte differentiation normally seen with the PPAR-γ agonist rosiglitazone. SR-202 also reduces the ability of young mice to put on weight and accumulate fat. The levels of circulating TNF-α correlates with body fat stores and/or hyperinsulinaemia. SR-202-treated wild-type mice have reduced TNF-α levels. When wild-type mice are fed a high-fat diet, the plasma levels of TNF-α are raised, and SR-202 treatment protects against this rise. Feeding mice with a high-fat diet induced insulin resistance measured as increased plasma levels of glucose, insulin and free fatty acids, and SR-202 protected against these changes. The ob/ob mouse is diabetic at 8 weeks and plasma glucose and insulin levels continue to rise over the next 3 weeks, and treatment with SR-202 prevents these increases. The development of PPAR-γ antagonists should continue as the results to date suggest that they have clinical potential for the treatment of diabetes Type 2 and obesity.
Keyword Diabetes
Mouse models
Obesity
SR-202
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Critical review of research, literature review, critical commentary
Collection: Scopus Import
 
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Created: Tue, 28 Jun 2016, 18:09:25 EST by System User