Inverse agonist exposure enhances ligand binding and G protein activation of the human MT1 melatonin receptor, but leads to receptor down‐regulation
T Kokkola, M Vaittinen, JT Laitinen - Journal of pineal research, 2007 - Wiley Online Library
Melatonin binds and activates G protein‐coupled melatonin receptors. The density and
affinity of the endogenous melatonin receptors change throughout the 24‐hr day, and the …
affinity of the endogenous melatonin receptors change throughout the 24‐hr day, and the …
Melatonin-mediated regulation of human MT1 melatonin receptors expressed in mammalian cells
MJ Gerdin, MI Masana, ML Dubocovich - Biochemical pharmacology, 2004 - Elsevier
In mammals, the pineal hormone melatonin activates G protein-coupled MT1 and MT2
melatonin receptors. Acute exposure of recombinant MT1 and MT2 melatonin receptors to …
melatonin receptors. Acute exposure of recombinant MT1 and MT2 melatonin receptors to …
Mutagenesis studies of the human MT2 melatonin receptor
MJ Gerdin, F Mseeh, ML Dubocovich - Biochemical pharmacology, 2003 - Elsevier
Melatonin mediates its physiological effects through activation of high affinity G protein-
coupled receptors. The vertebrate MT1, MT2 and Mel1c melatonin receptors are molecularly …
coupled receptors. The vertebrate MT1, MT2 and Mel1c melatonin receptors are molecularly …
Identification of cysteines involved in ligand binding to the human melatonin MT2 receptor
F Mseeh, MJ Gerdin, ML Dubocovich - European journal of pharmacology, 2002 - Elsevier
In mammals, melatonin activates melatonin MT1 and MT2 receptors. Using site-directed
mutagenesis and chemical modification, we investigated the role of conserved cysteines in …
mutagenesis and chemical modification, we investigated the role of conserved cysteines in …
C‐terminal domains within human MT1 and MT2 melatonin receptors are involved in internalization processes
S Sethi, W Adams, J Pollock… - Journal of pineal …, 2008 - Wiley Online Library
Melatonin, a molecule implicated in a variety of diseases, including cancer, often exerts its
effects through G‐protein‐coupled melatonin receptors, MT1 and MT2. In this study, we …
effects through G‐protein‐coupled melatonin receptors, MT1 and MT2. In this study, we …
Chimeric melatonin mt1 and melatonin-related receptors: Identification of domains and residues participating in ligand binding and receptor activation of the melatonin …
S Conway, JE Drew, ES Mowat, P Barrett… - Journal of Biological …, 2000 - ASBMB
Melatonin receptors bind and become activated by melatonin. The melatonin-related
receptor, despite sharing considerable amino acid sequence identity with melatonin …
receptor, despite sharing considerable amino acid sequence identity with melatonin …
The functional role of cysteines adjacent to the NRY motif of the human MT1 melatonin receptor
All G protein‐coupled melatonin receptors have two conserved cysteines in the interphase
between transmembrane helix III and the second intracellular loop, in the region assumed …
between transmembrane helix III and the second intracellular loop, in the region assumed …
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 …
signaling pathways, both in laboratory, heterologous, cellular models and in physiological …
17β-estradiol modulates hMT1 melatonin receptor function
MI Masana, JM Soares Jr, ML Dubocovich - Neuroendocrinology, 2005 - karger.com
Estrogen modulates expression and function of G-protein-coupled receptors. The goal of this
study was to assess the effect of 17β-estradiol (10 nM) exposure for 1 (E1) or 6 (E6) days on …
study was to assess the effect of 17β-estradiol (10 nM) exposure for 1 (E1) or 6 (E6) days on …
In vitro comparison of duration of action of melatonin agonists on melatonin MT1 receptor: Possible link between duration of action and dissociation rate from receptor
K Nishiyama, K Hirai - European Journal of Pharmacology, 2015 - Elsevier
Melatonin MT 1 and MT 2 receptors are Gi protein-coupled receptors and promising
therapeutic targets for a number of diseases. A proportion of G protein-coupled receptor …
therapeutic targets for a number of diseases. A proportion of G protein-coupled receptor …
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