Document Detail

Selective PPAR agonists for the treatment of type 2 diabetes.
MedLine Citation:
PMID:  16804025     Owner:  NLM     Status:  MEDLINE    
Type 2 diabetes is a metabolic disease characterized by increased plasma glucose and insulin as well as dyslipidemia. If left untreated, chronic diseases will develop that are associated with neuropathic damage and higher mortality risk. Using a rational drug design, novel compounds have been developed that selectively activate the human PPAR receptors, leading to lessening of hyperglycemia and hyperinsulinemia as well as reduction of lipid levels in conjunction with an increase of the beneficial HDL-cholesterol. These PPAR agonists showed increased potency and efficacy compared to previously marketed insulin sensitizers. Lead compounds with desirable pharmacokinetic properties were chosen for further testing in several animal models. The in vivo activity of some synthetic ligands, capable of activating two or all three members of peroxisome proliferator-activated receptors (PPAR) family of receptors, suggested that they may have improved efficacy in type 2 diabetes therapy. Here, we briefly summarize the development of some novel PPAR agonists identified by our group in recent years.
Jan O Nehlin; John P Mogensen; Ingrid Petterson; Lone Jeppesen; Jan Fleckner; Erik M Wulff; Per Sauerberg
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Annals of the New York Academy of Sciences     Volume:  1067     ISSN:  0077-8923     ISO Abbreviation:  Ann. N. Y. Acad. Sci.     Publication Date:  2006 May 
Date Detail:
Created Date:  2006-06-28     Completed Date:  2006-07-18     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7506858     Medline TA:  Ann N Y Acad Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  448-53     Citation Subset:  IM    
Novo Nordisk A/S, Måløv, Denmark.
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MeSH Terms
Diabetes Mellitus, Type 2 / drug therapy*
Dyslipidemias / drug therapy
Hyperglycemia / drug therapy
Hypoglycemic Agents / therapeutic use
Insulin / therapeutic use
Models, Biological
Peroxisome Proliferator-Activated Receptors / agonists*,  classification,  physiology
Reg. No./Substance:
0/Hypoglycemic Agents; 0/Peroxisome Proliferator-Activated Receptors; 11061-68-0/Insulin

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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