Selective PPAR Agonists for the Treatment of Type 2 Diabetes

:  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 dev...

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Bibliographic Details
Published in:Annals of the New York Academy of Sciences 2006-05, Vol.1067 (1), p.448-453
Main Authors: NEHLIN, JAN O., MOGENSEN, JOHN P., PETTERSON, INGRID, JEPPESEN, LONE, FLECKNER, JAN, WULFF, ERIK M., SAUERBERG, PER
Format: Article
Language:English
Subjects:
Animals
Diabetes Mellitus, Type 2 - drug therapy
diabetes type 2
dyslipidemia
Dyslipidemias - drug therapy
Humans
hyperglycemia
Hyperglycemia - drug therapy
Hypoglycemic Agents - therapeutic use
Insulin - therapeutic use
insulin sensitizers
Models, Biological
Peroxisome Proliferator-Activated Receptors - agonists
Peroxisome Proliferator-Activated Receptors - classification
Peroxisome Proliferator-Activated Receptors - physiology
PPAR
triple agonists
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Summary::  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.
ISSN:0077-8923
1749-6632
DOI:10.1196/annals.1354.064