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G-Protein Coupled Receptors Involved in the Resolution of Inflammation: Ligands and Therapeutic Perspectives

Author(s):

Margherita Mastromarino, Enza Lacivita*, Nicola A. Colabufo and Marcello Leopoldo   Pages 1 - 14 ( 14 )

Abstract:


Dysregulated inflammation is a central pathological process in diverse disease states, including neurodegenerative disorders. The recent concept of “resolution of inflammation” is offering a conceptual change for the diagnosis and the development of new therapeutic approaches for chronic inflammatory diseases. Resolution of inflammation terminates the inflammatory response promoting return to tissue homeostasis through the action of several classes of mediators, termed specialized pro-resolving lipid mediators (SPMs), that include lipoxins, resolvins, protectins, and maresins. SPMs provide “stop signals” that reduce the number of immune cells at the site of insult and increase clearance of apoptotic cells through phagocytosis. SPMs elicit their effects through the interaction with specific G-protein coupled receptors (GPCRs). The elucidation of the pathways downstream the GPCRs involved in the resolution of chronic inflammation is opening novel opportunities to generate novel anti-inflammatory agents. This review focuses on the SPMs and the receptors through which their effects are mediated. The medicinal chemistry of the modulators of the GPCRs involved in the resolution of inflammation will be illustrated, by highlighting the potential for developing new anti-inflammatory drugs.

Keywords:

Resolution of inflammation, pro-resolving specialized mediators, GPCRs, FPR2, GPR32, ChemR23, GPR18.

Affiliation:

Dipartimento di Farmacia - Scienze del Farmaco, Università degli Studi di Bari Aldo Moro, via Orabona, 4, 70125 Bari, Dipartimento di Farmacia - Scienze del Farmaco, Università degli Studi di Bari Aldo Moro, via Orabona, 4, 70125 Bari, Dipartimento di Farmacia - Scienze del Farmaco, Università degli Studi di Bari Aldo Moro, via Orabona, 4, 70125 Bari, Dipartimento di Farmacia - Scienze del Farmaco, Università degli Studi di Bari Aldo Moro, via Orabona, 4, 70125 Bari



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