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
Activation of MT2 receptor ameliorates dendritic abnormalities in Alzheimer’s disease via C/EBPα/miR‐125b pathway
Sign Up to like & getrecommendations! Published in 2019 at "Aging Cell"
DOI: 10.1111/acel.12902
Abstract: Impairments of dendritic trees and spines have been found in many neurodegenerative diseases, including Alzheimer's disease (AD), in which the deficits of melatonin signal pathway were reported. Melatonin receptor 2 (MT2) is widely expressed in… read more here.
Keywords: mt2; mir 125b; alzheimer disease; dendritic abnormalities ... See more keywords
Sleep well. Untangling the role of melatonin MT1 and MT2 receptors in sleep
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Pineal Research"
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
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Pineal Research"
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
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Pineal Research"
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
Supraspinal melatonin MT2 receptor agonism alleviates pain via a neural circuit that recruits mu opioid receptors
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Pineal Research"
DOI: 10.1111/jpi.12825
Abstract: Melatonin, through its G protein‐coupled receptor (GPCR) (MTNR1B gene) MT2, is implicated in analgesia, but the relationship between MT2 receptors and the opioid system remains elusive. In a model of rodent neuropathic pain (spared nerve… read more here.
Keywords: melatonin mt2; mt2 receptors; mt2; mor ... See more keywords
Melatonin meets diabetes
Sign Up to like & getrecommendations! Published in 2018 at "Science"
DOI: 10.1126/science.361.6405.888-p
Abstract: GPCR Signaling Some of the single-nucleotide polymorphisms associated with type 2 diabetes occur in the gene that encodes the melatonin receptor MT2, a G protein–coupled receptor (GPCR). Karamitri et al. measured the spontaneous and melatonin-stimulated… read more here.
Keywords: melatonin meets; type diabetes; meets diabetes; mt2 ... See more keywords
The Ectodomain of Matriptase-2 Plays an Important Non-Proteolytic Role in Suppressing Hepcidin Expression in Mice.
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DOI: 10.1182/blood.2020005222
Abstract: Matriptase-2 (MT2), encoded by TMPRSS6, is a membrane-anchored serine protease, which plays a key role in suppressing hepatic hepcidin expression. MT2 is synthesized as a zymogen and undergoes autocleavage for activation. Previous studies suggest that… read more here.
Keywords: mt2; role suppressing; expression; non proteolytic ... See more keywords
The Uterine Melatonergic Systems of AANAT and Melatonin Membrane Receptor 2 (MT2) Are Essential for Endometrial Receptivity and Early Implantation in Mice
Sign Up to like & getrecommendations! Published in 2023 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms24087127
Abstract: In the current study, using Aanat and Mt2 KO mice, we observed that the preservation of the melatonergic system is essential for successful early pregnancy in mice. We identified that aralkylamine N-acetyltransferase (AANAT), melatonin receptor… read more here.
Keywords: melatonergic system; aanat melatonin; mt2; aanat mt2 ... See more keywords