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Updated: May 17, 2026

Quantifying Agonist Activity at G Protein-coupled Receptors
Published on: December 26, 2011
[PPARs: physiological functions and pharmacological roles of agonists in human diseases. Note II]
Florina Filip-Ciubotaru1, Carmen Manciuc, Cecilia Grigore
1Disciplina de Medicina de Familie, Facultatea de Medicină, Universitatea de Medicină si Farmacie "Grigore T. Popa", Iaşi.
Abstract:
Increasing attention paid to the main family of peroxisome proliferator activated receptors--PPARs is generated, on one hand by the multiple functions of its members in numerous metabolically active tissues, and on the other hand by the therapeutic benefits expresed by some specific ligands that are used in certain metabolic diseases treatment plan. PPARalpha stimulates the beta-oxidative degradation of fatty acids and controls plasma lipid transport through the mediated action upon the triglycerides and fatty acids metabolism and by modulation of biosynthesis and catabolism of bile acids in the liver. PPARgamma promotes adipocytes differentiation and fat storage. PPARbeta/delta is involved in control and management of adipogenesis. While PPARalpha mediates the hypolipemiant actions of fibrates, PPARgamma is the receptor for thiazolidinediones (glitazones) reccomended in type 2 diabetes treatment; by binding to PPARgamma, glitazones modulates transcription of genes involved in lipid and carbohydrate metabolism.
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