Results 151 to 160 of about 11,642 (187)
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Important amino acids for the function of the human MT1 melatonin receptor
Biochemical Pharmacology, 2003Models of G protein-coupled melatonin receptor structure suggest that ligand recognition occurs in a binding pocket formed by transmembrane helices III, V and VII. Constitutively active mutations in G protein-coupled receptors have revealed that transmembrane helix III/intracellular loop 2 interface and transmembrane domain VI are critical regions in ...
Tarja, Kokkola +4 more
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Down-regulation of mt1 melatonin receptors in rat ovary following estrogen exposure
Life Sciences, 2001In this study, we have demonstrated that 2-[125I]-iodomelatonin binds specifically to rat ovarian granulosa cell (GC) membranes with high affinity (KD=83 pM; Bmax=3.28 fmol/mg protein). Using immunoblot analysis and an anti-mt1 melatonin receptor antibody, we have also detected mt1 melatonin receptors in rat ovary.
J W, Clemens +2 more
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Molecular Modeling of Human MT1 and MT2 Melatonin Receptors
2006Malfunction of G-protein coupled receptors (GPCR) provokes large amount of diseases. Their adequate treatment requires rational design of new high affinity and high selectivity drugs targeting these receptors. Molecular modeling represents a powerful tool to solve the problem.
A. Chugunov, P. Chavatte, R. Efremov
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Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist
Neuropharmacology, 2005Ramelteon (TAK-375) is a novel melatonin receptor agonist currently under investigation for the treatment of insomnia. This study describes the neurochemical and receptor binding characteristics of ramelteon in vitro. Ramelteon showed very high affinity for human MT1 (Mel1a) and MT2 (Mel1b) receptors (expressed in Chinese hamster ovary [CHO] cells ...
Koki, Kato +8 more
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Functional MT1 and MT2 melatonin receptors in mammals.
Endocrine, 2005Melatonin, dubbed the hormone of darkness, is known to regulate a wide variety of physiological processes in mammals. This review describes well-defined functional responses mediated through activation of high-affinity MT1 and MT2 G protein-coupled receptors viewed as potential targets for drug discovery.
Margarita L, Dubocovich +1 more
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The expression of MT1 and MT2 melatonin receptor mRNA in several rat tissues
Life Sciences, 2005The mechanisms that mediate the various effects of melatonin in mammalian tissues are not always known. Therefore, the aim of this study was to investigate whether MT(1) and MT(2) melatonin receptors are expressed in certain tissues of the rat. The expression of MT(1) and MT(2) melatonin receptor mRNA was determined using a real-time quantitative RT ...
Pirkko, Sallinen +4 more
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Chronobiological features of melatonin receptors (MT1) expression in breast cancer cells.
Journal of Clinical Oncology, 2019e12581 Background: According to WHO data, Breast Cancer is the most prevalent malignancy in women. The biological role of Melatonin in the etiology and pathogenesis of the tumour disease has already been approved by a number of research studies. The purpose of our investigation was the assessment of features of Melatonin receptor circadian expression
Alexandre Tavartkiladze +2 more
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Critical care management of chimeric antigen receptor T‐cell therapy recipients
Ca-A Cancer Journal for Clinicians, 2022Alexander Shimabukuro-Vornhagen +2 more
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