Related Experiment Video
Updated: Aug 17, 2026

Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
Published on: May 24, 2024
[PPAR receptors: recent data]
1INSERM U449/INRA U1235, Faculté de Médecine Laënnec, Université Claude-Bernard, F-69372 Lyon Cedex 08, France. vidal@laennec.univ-lyon1.fr
Abstract:
The nuclear receptors PPAR (Peroxisome Proliferator-Activated Receptors) are transcription factors which form with the retinoid receptor RXR, a PPAR/RXR heterodimer, the functional transcription factor within cells. PPAR receptors are activated by their ligands, either naturals or synthetics, and modulate target gene transcription. There are three PPAR subtypes (PPARalpha, PPARbeta/delta et PPARgamma) coded by different genes, and two isoforms of PPARgamma proteins have been detected in humans (PPARgamma1 and PPARgamma2). PPAR are mainly modulators of lipid metabolism, but each receptor subtype is pharmacologically distinct, and development of synthetic PPAR agonists has shown their role in cellular (mainly adipocyte) differentiation and in glucose homeostasis. This review summarise the main data, currently available, on expression, biological functions, natural and synthetic (activators) ligands for the PPAR receptor subtypes. PPAR receptors key-role in lipid and glucose métabolisms, has lead to a large clinical use of pharmacological agents acting as PPAR ligands: fibrates, PPARalpha agonists as hypolipidaemic treatment, thiazolidinediones (glitazones), PPARalpha agonists as antidiabetics. Lipid metabolism is impaired in insulin resistant skeletal muscles, fatty acids role in the pathophysiology of insulin resistance generates several hypothesis we briefly describe. Finally, we present and discuss experimental data, suggesting the activation of PPARbeta/delta in skeletal muscle to be a potential new approach in the treatment of insulin resistance and metabolic syndrome.
Related Concept Videos
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Transducer Mechanism: Nuclear Receptors
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
G Protein-coupled Receptors
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs Regulate Adenylyl Cylase Activity
Two...
Transducer Mechanism: G Protein–Coupled Receptors
GPCRs are also called heptahelical, 7TM, or...
Spare Receptors
