2. Academic Validation
  3. GPR120/FFAR4 Pharmacology: Focus on Agonists in Type 2 Diabetes Mellitus Drug Discovery

GPR120/FFAR4 Pharmacology: Focus on Agonists in Type 2 Diabetes Mellitus Drug Discovery

  • J Med Chem. 2021 Apr 22;64(8):4312-4332. doi: 10.1021/acs.jmedchem.0c01002.
Gabriele Carullo 1,  Sarah Mazzotta 2,  Margarita Vega-Holm 3,  Fernando Iglesias-Guerra 3,  José Manuel Vega-Pérez 3,  Francesca Aiello 4,  Antonella Brizzi 1
Affiliations

Affiliations

  • 1 Department of Biotechnology, Chemistry, and Pharmacy, DoE 2018-2022, University of Siena, Via Aldo Moro 2, 53100 Siena, Italy.
  • 2 Department of Pharmaceutical Sciences, University of Milan, Via Luigi Mangiagalli 25, 20133 Milano, Italy.
  • 3 Department of Organic and Medicinal Chemistry, Faculty of Pharmacy, University of Seville, Profesor García González 2, 41012 Seville, Spain.
  • 4 Department of Pharmacy, Health and Nutritional Sciences, DoE 2018-2022, University of Calabria, Edificio Polifunzionale, 87036 Rende, Cosenza, Italy.
PMID: 33843223 DOI: 10.1021/acs.jmedchem.0c01002
Abstract

The G-protein coupled receptors (GPCRs) activated by free fatty acids (FFAs) have emerged as new and exciting drug targets, due to their plausible translation from pharmacology to medicines. This perspective aims to report recent research about GPR120/FFAR4 and its involvement in several diseases, including Cancer, inflammatory conditions, and central nervous system disorders. The focus is to highlight the importance of GPR120 in Type 2 diabetes mellitus (T2DM). GPR120 agonists, useful in T2DM drug discovery, have been widely explored from a structure-activity relationship point of view. Since the identification of the first reported synthetic agonist TUG-891, the research has paved the way for the development of TUG-based molecules as well as new and different chemical entities. These molecules might represent the starting point for the future discovery of GPR120 agonists as antidiabetic drugs.

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