Results 141 to 150 of about 11,642 (187)

Functionality of Melatonin Receptors: Recruitment of β-Arrestin at MT1

2022
The main process of downregulation of G protein-coupled receptors is desensitization by which the receptor is extruded from the plasma membrane and directed to the endosomal compartment for recycling. Typically, the first step of this phenomenon consists in the recruitment of the protein β-arrestin induced by the agonist.
Clémence, Dupré, Céline, Legros, Jean A, Boutin   +2 more
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Homology modeling of MT1 and MT2 receptors

European Journal of Medicinal Chemistry, 2008
Melatonin is a neurohormone synthesized and secreted mainly during the dark period of the circadian cycle by the pineal gland. It has already been proved to be involved in a number of chronobiological processes, most of them being mediated by its membranar receptors MT1 and MT2.
Farce, Amaury, Chugunov, Anton O., Logé, Cédric, Sabaouni, Ahmed, Yous, Said, Dilly, Sébastien, Renault, Nicolas, Vergoten, Gérard, Efremov, Roman G., Lesieur, Daniel, Chavatte, Philippe   +10 more
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Characterization of an Antibody to the Human Melatonin mt1 Receptor

Journal of Neuroendocrinology, 2001
AbstractMelatonin acts via high affinity, G‐protein coupled, seven transmembrane domain receptors. To precisely localize these receptors, antibodies were raised in chickens against a 15 amino acid fragment at the intracellular C‐terminal region of the human melatonin receptor subtype mt1 (DSSNDVADRVKWKPS, mt1338−352).
L M, Williams, J E, Drew, N W, Bunnett, E, Grady, P, Barrett, D R, Abramovich, A, Morris, D, Slater   +7 more
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Cerebrovascular melatonin MT1-receptor alterations in patients with Alzheimer's disease

Neuroscience Letters, 2001
The pineal hormone melatonin has two major functions: as a transducer of the circadian day-night signal across the seasons, and as a vasoactive substance regulating cerebral circulation. The vasoconstrictive effects of melatonin have been postulated to be mediated by the melatonin 1a-receptor (MT1).
E, Savaskan, G, Olivieri, L, Brydon, R, Jockers, K, Kräuchi, A, Wirz-Justice, F, Müller-Spahn   +6 more
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Involvement of the mt1 melatonin receptor in human breast cancer

Cancer Letters, 2002
Two putative melatonin receptors have been described including the cell surface G-protein-linked receptors, mt1 and MT2, and the nuclear retinoic orphan receptor alpha (RORalpha). The mt1 receptor, but not the MT2 receptor, is expressed in human breast tumor cell lines, and melatonin-induced growth suppression can be mimicked by the mt1 and MT2 agonist,
P T, Ram, J, Dai, L, Yuan, C, Dong, T L, Kiefer, L, Lai, S M, Hill   +6 more
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Molecular pharmacology of the ovine melatonin receptor: comparison with recombinant human MT1 and MT2 receptors

Biochemical Pharmacology, 2004
The variations of the pharmacological properties of melatonin receptors between different mammalian species in transfected cell lines have been poorly investigated. In the present study, melatonin analogues have been used to characterize the pharmacology of the recombinant ovine melatonin receptor (oMT1) expressed in CHO cell lines and the native oMT1 ...
Mailliet, F., Audinot, V., Malpaux, Benoit, Bonnaud, Anthony, Delagrange, P., Migaud, Martine, Barrett, P., Viaud-Massuard, M.C., Lesieur, D., Lefoulon, F., Renard, P., Boutin, Jany   +11 more
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A new melatonin receptor ligand with mt1‐agonist and MT2‐antagonist properties

Journal of Pineal Research, 2000
It has been difficult, so far, to obtain melatonin analogs possessing high selectivity for the respective melatonin receptors, mt1 and MT2. In the present work, we report the synthesis and pharmacological characterization of a new compound N‐{2‐[5‐(2‐hydroxyethoxy)‐1H‐indol‐3‐yl)] ethyl} acetamide or 5‐hydroxyethoxy‐N‐acetyltryptamine (5‐HEAT).
NONNO R, LUCINI V, SPADONI, GILBERTO, PANNACCI M, CROCE A, ESPOSTI D, BALSAMINI, CESARINO, TARZIA, GIORGIO, FRASCHINI F, STANKOV BM   +9 more
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Molecular cloning and pharmacological characterization of rat melatonin MT1 and MT2 receptors

Biochemical Pharmacology, 2008
In order to interpret the effects of melatonin ligands in rats, we need to determine their activity at the receptor subtype level in the corresponding species. Thus, the rat melatonin rMT(1) receptor was cloned using DNA fragments for exon 1 and 2 amplified from rat genomic DNA followed by screening of a rat genomic library for the full length exon ...
Valérie, Audinot, Anne, Bonnaud, Line, Grandcolas, Marianne, Rodriguez, Nadine, Nagel, Jean-Pierre, Galizzi, Ales, Balik, Sophie, Messager, David G, Hazlerigg, Perry, Barrett, Philippe, Delagrange, Jean A, Boutin   +11 more
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Molecular pharmacology of the mouse melatonin receptors MT1 and MT2

European Journal of Pharmacology, 2012
The main melatonin receptors are two G-protein coupled receptors named MT(1) and MT(2). Having described the molecular pharmacology of the human versions of these receptors, we turned to two of the three species most useful in studying melatonin physiology: rat and sheep (a diurnal species used to understand the relationship between circadian rhythm ...
Devavry, Séverine, Legros, Celine, Brasseur, Chantal, Cohen, William, Guénin, Sophie-Pénélope, Delagrange, Philippe, Malpaux, Benoit, Ouvry, Christine, Cogé, Francis, Nosjean, Olivier, Boutin, Jany   +10 more
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The melatonin-MT1 receptor axis modulates tumor growth in PTEN-mutated gliomas

Biochemical and Biophysical Research Communications, 2018
More than 40% of glioma patients have tumors that harbor PTEN (phosphatase and tensin homologue deleted on chromosome ten) mutations; this disease is associated with poor therapeutic resistance and outcome. Such mutations are linked to increased cell survival and growth, decreased apoptosis, and drug resistance; thus, new therapeutic strategies ...
Huihui Ma, Zhen Wang, Lei Hu, Shangrong Zhang, Chenggang Zhao, Haoran Yang, Hongzhi Wang, Zhiyou Fang, Lijun Wu, Xueran Chen   +9 more
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