Molecular basis defining the selectivity of substituted isoquinolinones for the melatonin MT2 receptor.
Sign Up to like & getrecommendations! Published in 2020 at "Biochemical pharmacology"
DOI: 10.1016/j.bcp.2020.114020
Abstract: Melatonin MT1 and MT2 receptors represent attractive drug targets for the treatment of various disorders. However, the high conservation of the melatonin binding pocket has hindered the development of subtype-selective compounds. By leveraging on the… read more here.
Keywords: mt1 mt2; mt2; basis; receptor ... See more keywords
Neu‐P11, a novel MT1/MT2 agonist, reverses diabetes by suppressing the hypothalamic‐pituitary‐adrenal axis in rats
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DOI: 10.1016/j.ejphar.2017.07.001
Abstract: &NA; Excessive glucocorticoid (GC) in type 2 diabetes mellitus (T2DM) reduces insulin sensitivity, impairs &bgr;‐cell function, increases gluconeogenesis and glycogenolysis, impairs glucose uptake and metabolism, and reduces the insulinotropic effects of glucagon‐like peptide 1. Melatonin,… read more here.
Keywords: mt1 mt2; neu p11; p11; axis ... See more keywords
Melatonin concentration in peripheral blood and melatonin receptors (MT1 and MT2) in the testis and epididymis of male roe deer during active spermatogenesis.
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DOI: 10.1016/j.theriogenology.2020.03.025
Abstract: Melatonin regulates male reproductive function in seasonal and non-seasonal breeder mammals. The presence of melatonin membrane receptors (MT1 and MT2) in the testis and epididymis has been demonstrated in several species. Wild roe deer are… read more here.
Keywords: mt1 mt2; testis epididymis; melatonin; male roe ... See more keywords
Effect of melatonin on arsenic-induced oxidative stress and expression of MT1 and MT2 receptors in the kidney of laboratory mice
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DOI: 10.1080/09291016.2019.1566993
Abstract: ABSTRACT Arsenic is a ubiquitous element of the environment present in both inorganic and organic forms. Arsenic exposure leads to oxidative stress and tissue damages in living organisms. Kidney is one of the major target… read more here.
Keywords: mt1 mt2; stress; expression; melatonin ... See more keywords
Sleep well. Untangling the role of melatonin MT1 and MT2 receptors in sleep
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DOI: 10.1111/jpi.12544
Abstract: The pharmacological potential of targeting selectively melatonin MT1 or MT2 receptors has not yet been exploited in medicine. Research using selective MT1/MT2 receptor ligands and MT1/MT2 receptor knockout mice has indicated that the activation of… read more here.
Keywords: melatonin mt1; mt1 mt2; mt2; mt2 receptors ... See more keywords
MT1 and MT2 melatonin receptors are expressed in nonoverlapping neuronal populations
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DOI: 10.1111/jpi.12575
Abstract: Melatonin (MLT) exerts its physiological effects principally through two high‐affinity membrane receptors MT1 and MT2. Understanding the exact mechanism of MLT action necessitates the use of highly selective agonists/antagonists to stimulate/inhibit a given MLT receptor.… read more here.
Keywords: mt2 melatonin; mt1 mt2; mt2; melatonin receptors ... See more keywords
Melatonin MT1 and MT2 receptor ERK signaling is differentially dependent on Gi/o and Gq/11 proteins
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DOI: 10.1111/jpi.12641
Abstract: G protein‐coupled receptors (GPCRs) transmit extracellular signals into cells by activating G protein‐ and β‐arrestin‐dependent pathways. Extracellular signal‐regulated kinases (ERKs) play a central role in integrating these different linear inputs coming from a variety of… read more here.
Keywords: mt1 mt2; mt2; erk; melatonin mt1 ... See more keywords
Influence of agomelatine and trastuzumab on the HER2/neu(+), MT1 (+) and MT2 (+) chemo and immunoresistant breast cancer cells lines from the previously treated patients by targeted therapy with trastuzumab.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2019.37.15_suppl.e14056
Abstract: e14056 Background: Agomelatine is a melatonin receptor agonist (MT1 and MT2) and a 5-HT2C receptor antagonist. Melatonin is a lipophilic compound that is capable of binding to cell surface receptors, cytosolic sites (calmodulin), and directly… read more here.
Keywords: cells lines; mt1 mt2; trastuzumab; agomelatine trastuzumab ... See more keywords