Literature DB >> 27314810

Update on melatonin receptors: IUPHAR Review 20.

Ralf Jockers1,2,3, Philippe Delagrange4, Margarita L Dubocovich5, Regina P Markus6, Nicolas Renault7, Gianluca Tosini8, Erika Cecon1,2,3, Darius P Zlotos9.   

Abstract

Melatonin receptors are seven transmembrane-spanning proteins belonging to the GPCR superfamily. In mammals, two melatonin receptor subtypes exist - MT1 and MT2 - encoded by the MTNR1A and MTNR1B genes respectively. The current review provides an update on melatonin receptors by the corresponding subcommittee of the International Union of Basic and Clinical Pharmacology. We will highlight recent developments of melatonin receptor ligands, including radioligands, and give an update on the latest phenotyping results of melatonin receptor knockout mice. The current status and perspectives of the structure of melatonin receptor will be summarized. The physiological importance of melatonin receptor dimers and biologically important and type 2 diabetes-associated genetic variants of melatonin receptors will be discussed. The role of melatonin receptors in physiology and disease will be further exemplified by their functions in the immune system and the CNS. Finally, antioxidant and free radical scavenger properties of melatonin and its relation to melatonin receptors will be critically addressed.
© 2016 The British Pharmacological Society.

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Year:  2016        PMID: 27314810      PMCID: PMC4995287          DOI: 10.1111/bph.13536

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  204 in total

1.  A single blind, placebo controlled, across groups dose escalation study of the safety, tolerability, pharmacokinetics and pharmacodynamics of the melatonin analog beta-methyl-6-chloromelatonin.

Authors:  J J Mulchahey; D R Goldwater; F P Zemlan
Journal:  Life Sci       Date:  2004-08-27       Impact factor: 5.037

2.  Effect of exogenous melatonin on sleep and motor dysfunction in Parkinson's disease. A randomized, double blind, placebo-controlled study.

Authors:  Camila Andrade Mendes Medeiros; Pedro Felipe Carvalhedo de Bruin; Lívia Ariane Lopes; Maria Cecília Magalhães; Maria de Lourdes Seabra; Veralice Meireles Sales de Bruin
Journal:  J Neurol       Date:  2007-04-03       Impact factor: 4.849

3.  Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs.

Authors:  Ron O Dror; Hillary F Green; Celine Valant; David W Borhani; James R Valcourt; Albert C Pan; Daniel H Arlow; Meritxell Canals; J Robert Lane; Raphaël Rahmani; Jonathan B Baell; Patrick M Sexton; Arthur Christopoulos; David E Shaw
Journal:  Nature       Date:  2013-10-13       Impact factor: 49.962

Review 4.  MT1 and MT2 Melatonin Receptors: A Therapeutic Perspective.

Authors:  Jiabei Liu; Shannon J Clough; Anthony J Hutchinson; Ekue B Adamah-Biassi; Marina Popovska-Gorevski; Margarita L Dubocovich
Journal:  Annu Rev Pharmacol Toxicol       Date:  2015-10-23       Impact factor: 13.820

Review 5.  Beyond standard molecular dynamics: investigating the molecular mechanisms of G protein-coupled receptors with enhanced molecular dynamics methods.

Authors:  Jennifer M Johnston; Marta Filizola
Journal:  Adv Exp Med Biol       Date:  2014       Impact factor: 2.622

6.  Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor.

Authors:  M L Dubocovich; M I Masana; S Iacob; D M Sauri
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1997-03       Impact factor: 3.000

7.  Monitoring of ligand-independent dimerization and ligand-induced conformational changes of melatonin receptors in living cells by bioluminescence resonance energy transfer.

Authors:  Mohammed A Ayoub; Cyril Couturier; Estelle Lucas-Meunier; Stephane Angers; Philippe Fossier; Michel Bouvier; Ralf Jockers
Journal:  J Biol Chem       Date:  2002-04-08       Impact factor: 5.157

8.  Genetic deletion of MT(1) and MT(2) melatonin receptors differentially abrogates the development and expression of methamphetamine-induced locomotor sensitization during the day and the night in C3H/HeN mice.

Authors:  Anthony J Hutchinson; Randall L Hudson; Margarita L Dubocovich
Journal:  J Pineal Res       Date:  2012-06-07       Impact factor: 13.007

9.  Melatonin from cerebrospinal fluid but not from blood reaches sheep cerebral tissues under physiological conditions.

Authors:  C Legros; D Chesneau; J A Boutin; C Barc; B Malpaux
Journal:  J Neuroendocrinol       Date:  2014-03       Impact factor: 3.627

10.  Melatonin agonist tasimelteon (VEC-162) for transient insomnia after sleep-time shift: two randomised controlled multicentre trials.

Authors:  Shantha Mw Rajaratnam; Mihael H Polymeropoulos; Dennis M Fisher; Thomas Roth; Christin Scott; Gunther Birznieks; Elizabeth B Klerman
Journal:  Lancet       Date:  2008-12-04       Impact factor: 79.321

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  109 in total

Review 1.  Melatonin receptors: molecular pharmacology and signalling in the context of system bias.

Authors:  Erika Cecon; Atsuro Oishi; Ralf Jockers
Journal:  Br J Pharmacol       Date:  2017-08-17       Impact factor: 8.739

Review 2.  Melatonin, clock genes and mitochondria in sepsis.

Authors:  Darío Acuña-Castroviejo; Ibtissem Rahim; Carlos Acuña-Fernández; Marisol Fernández-Ortiz; Jorge Solera-Marín; Ramy K A Sayed; María E Díaz-Casado; Iryna Rusanova; Luis C López; Germaine Escames
Journal:  Cell Mol Life Sci       Date:  2017-08-07       Impact factor: 9.261

Review 3.  Pleiotropic genetic effects influencing sleep and neurological disorders.

Authors:  Olivia J Veatch; Brendan T Keenan; Philip R Gehrman; Beth A Malow; Allan I Pack
Journal:  Lancet Neurol       Date:  2017-02       Impact factor: 44.182

Review 4.  Effects of melatonin on cardiovascular risk factors and metabolic syndrome: a comprehensive review.

Authors:  Mohsen Imenshahidi; Golamreza Karimi; Hossein Hosseinzadeh
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2020-01-30       Impact factor: 3.000

5.  Fluorine substituted methoxyphenylalkyl amides as potent melatonin receptor agonists.

Authors:  Andrew Tsotinis; Rodanthi Kompogennitaki; Ioannis Papanastasiou; Peter J Garratt; Alina Bocianowska; David Sugden
Journal:  Medchemcomm       Date:  2019-02-11       Impact factor: 3.597

6.  Design and validation of the first cell-impermeant melatonin receptor agonist.

Authors:  Florence Gbahou; Erika Cecon; Guillaume Viault; Romain Gerbier; Frederic Jean-Alphonse; Angeliki Karamitri; Gérald Guillaumet; Philippe Delagrange; Robert M Friedlander; Jean-Pierre Vilardaga; Franck Suzenet; Ralf Jockers
Journal:  Br J Pharmacol       Date:  2017-06-11       Impact factor: 8.739

7.  Melatonin promotes sleep by activating the BK channel in C. elegans.

Authors:  Longgang Niu; Yan Li; Pengyu Zong; Ping Liu; Yuan Shui; Bojun Chen; Zhao-Wen Wang
Journal:  Proc Natl Acad Sci U S A       Date:  2020-09-21       Impact factor: 11.205

8.  Cryo-EM structure of the human MT1-Gi signaling complex.

Authors:  Hiroyuki H Okamoto; Hirotake Miyauchi; Asuka Inoue; Francesco Raimondi; Hirokazu Tsujimoto; Tsukasa Kusakizako; Wataru Shihoya; Keitaro Yamashita; Ryoji Suno; Norimichi Nomura; Takuya Kobayashi; So Iwata; Tomohiro Nishizawa; Osamu Nureki
Journal:  Nat Struct Mol Biol       Date:  2021-08-05       Impact factor: 15.369

9.  Melatonin protects INS-1 pancreatic β-cells from apoptosis and senescence induced by glucotoxicity and glucolipotoxicity.

Authors:  Yu Hee Lee; Hye Sook Jung; Min Jeong Kwon; Jung Eun Jang; Tae Nyun Kim; Soon Hee Lee; Mi-Kyung Kim; Jeong Hyun Park
Journal:  Islets       Date:  2020-07-16       Impact factor: 2.694

Review 10.  Melatonin, an ubiquitous metabolic regulator: functions, mechanisms and effects on circadian disruption and degenerative diseases.

Authors:  Andreea Iulia Socaciu; Răzvan Ionuţ; Mihai Adrian Socaciu; Andreea Petra Ungur; Maria Bârsan; Angelica Chiorean; Carmen Socaciu; Armand Gabriel Râjnoveanu
Journal:  Rev Endocr Metab Disord       Date:  2020-12       Impact factor: 6.514

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