Discovery and development of selective PPARγ modulators as safe and effective antidiabetic agents
| Autor: | Amol Dixit, Kumar V.S. Nemmani, Lalit S. Doshi, Umakant Ashok Bahirat, Manoja K. Brahma |
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| Rok vydání: | 2010 |
| Předmět: |
Pharmacology
chemistry.chemical_classification business.industry Peroxisome proliferator-activated receptor General Medicine PPAR gamma Safety profile Diabetes Mellitus Type 2 chemistry Organ Specificity Drug Discovery Adipocytes Animals Humans Hypoglycemic Agents Medicine Pharmacology (medical) Insulin Resistance business Rosiglitazone Antidiabetic agents medicine.drug |
| Zdroj: | Expert Opinion on Investigational Drugs. 19:489-512 |
| ISSN: | 1744-7658 1354-3784 |
| Popis: | PPARgamma full agonists (pioglitazone and rosiglitazone) are the mainstay drugs for the treatment of type 2 diabetes; however, mechanism-based side effects have limited their full therapeutic potential. In recent years, much progress has been achieved in the discovery and development of selective PPARgamma modulators (SPPARgammaMs) as safer alternatives to PPARgamma full agonists.This review focuses on the preclinical and clinical data of all the SPPARgammaMs discovered so far, retrieved by searching PubMed, Prous Integrity database and company news updates from 1999 to date.Here we thoroughly discuss SPPARgammaMs' mode of action, briefly examine new ways to identify superior SPPARgammaMs, and finally, compare and contrast the pharmacological and safety profile of various agents.The preclinical and clinical findings clearly suggest that selective PPARgamma modulators have the potential to become the next generation of PPARgamma agonists: effective insulin sensitizers with a superior safety profile to that of PPARgamma full agonists. |
| Databáze: | OpenAIRE |
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