Molecular Characterization and Pharmacology of Melatonin Receptors in Animals

Author:

Cecon Erika1ORCID,Boutin Jean A.2ORCID,Jockers Ralf1

Affiliation:

1. Institut Cochin, Université Paris Cité, INSERM, CNRS, 75014 Paris, France

2. Laboratory of Neuronal and Neuroendocrine Differentiation and Communication, University of Normandy, INSERM U1239, 76000 Rouen, France

Abstract

Melatonin, the hormone of darkness, is secreted in minute amounts during the night and is virtually undetectable during the day. Melatonin mainly acts on high-affinity G protein-coupled receptors. The present review will trace the path of the discovery of melatonin receptors from their cloning, expression and purification to the development of recent radioactive and fluorescent tracers. We will then report on the state-of-the-art of melatonin receptor functional properties, including ligand bias and system bias due to receptor-associated proteins and receptor heteromers. Currently available antibodies raised against melatonin receptors will be critically reviewed here for the first time. The review will close with future perspectives in terms of the discovery of allosteric ligands and the in vivo validation of a range of melatonin receptor-associated signaling complexes to improve future drug development.

Funder

Agence Nationale de la Recherche

ANR: Appel RA-Covid-19 projet MELATOVID

Fondation pour la recherche Médicale

La Ligue Contre le Cancer

Institut National de la Santé et de la Recherche Médicale (INSERM), Centre National de la Recherche Scientifique

Publisher

MDPI AG

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