Are G protein‐coupled receptor heterodimers of physiological relevance?—Focus on melatonin receptors

A Levoye, R Jockers, MA Ayoub… - Chronobiology …, 2006 - Taylor & Francis
In mammals, the circadian hormone melatonin targets two seven‐transmembrane–spanning
receptors, MT1 and MT2, of the G protein‐coupled receptor (GPCR) super‐family. Evidence …

[HTML][HTML] Recombinant human melatonin receptor MT1 isolated in mixed detergents shows pharmacology similar to that in mammalian cell membranes

C Logez, S Berger, C Legros, JL Baneres, W Cohen… - PLoS …, 2014 - journals.plos.org
The human melatonin MT1 receptor—belonging to the large family of G protein-coupled
receptors (GPCRs)—plays a key role in circadian rhythm regulation and is notably involved …

The orphan GPR50 receptor specifically inhibits MT1 melatonin receptor function through heterodimerization

A Levoye, J Dam, MA Ayoub, JL Guillaume… - The EMBO …, 2006 - embopress.org
One‐third of the∼ 400 nonodorant G protein‐coupled receptors (GPCRs) are still orphans.
Although a considerable number of these receptors are likely to transduce cellular signals in …

Preferential formation of MT1/MT2 melatonin receptor heterodimers with distinct ligand interaction properties compared with MT2 homodimers

MA Ayoub, A Levoye, P Delagrange, R Jockers - Molecular pharmacology, 2004 - ASPET
Heterodimerization has been documented for several members of the G protein-coupled
receptor (GPCR) superfamily, including the closely related MT1 and MT2 melatonin …

Detection of recombinant and endogenous mouse melatonin receptors by monoclonal antibodies targeting the C‐terminal domain

E Cecon, A Ivanova, M Luka, F Gbahou… - Journal of pineal …, 2019 - Wiley Online Library
Melatonin receptors play important roles in the regulation of circadian and seasonal
rhythms, sleep, retinal functions, the immune system, depression, and type 2 diabetes …

Heteromeric MT1/MT2 Melatonin Receptors Modulate Photoreceptor Function

K Baba, A Benleulmi-Chaachoua, AS Journé… - Science …, 2013 - science.org
The formation of G protein (heterotrimeric guanine nucleotide–binding protein)–coupled
receptor (GPCR) heteromers enables signaling diversification and holds great promise for …

Melatonin receptor signaling: impact of receptor oligomerization on receptor function

A Oishi, E Cecon, R Jockers - International Review of Cell and Molecular …, 2018 - Elsevier
The melatonin receptor subfamily is composed of three members, MT 1 and MT 2, which are
binding to melatonin, and GPR50, which shows high sequence homology to MT 1 and MT 2 …

Melatonin receptors, heterodimerization, signal transduction and binding sites: what's new?

R Jockers, P Maurice, JA Boutin… - British journal of …, 2008 - Wiley Online Library
Melatonin is a neurohormone that has been claimed to be involved in a wide range of
physiological functions. Nevertheless, for most of its effects, the mechanism of action is not …

Description of the constitutive activity of cloned human melatonin receptors hMT1 and hMT2 and discovery of inverse agonists

S Devavry, C Legros, C Brasseur… - Journal of pineal …, 2012 - Wiley Online Library
Melatonin receptors have been described to activate different G protein–dependent
signaling pathways, both in laboratory, heterologous, cellular models and in physiological …

Melatonin MT1 and MT2 receptors display different molecular pharmacologies only in the G‐protein coupled state

C Legros, S Devavry, S Caignard… - British journal of …, 2014 - Wiley Online Library
Background and Purpose Melatonin receptors have been extensively characterized
regarding their affinity and pharmacology, mostly using 2‐[125I]‐melatonin as a radioligand …