Melatonin Receptor Type 1A (human recombinant)

Melatonin receptor type 1A (MT₁) (human recombinant) contains amino acids corresponding to the full length, wild-type human MT₁ receptor, as well as N-terminal histidine and streptavidin tags with a TEV protease cleavage site. The MT₁ receptor is encoded by the MTNR1A gene and is a G protein-coupled receptor expressed on post-synaptic terminals in the suprachiasmic nucleus (SCN) and hypothalamus.¹ It is activated by melatonin and signals through G_i and G_q proteins. Based on MT₁ and MT₂ receptor knockout mouse studies, the MT₁ receptor is involved in decreasing neuronal firing in the SCN and inhibits prolactin secretion in the pituitary gland. MT₁ receptor activation inhibits proliferation of hormone-refractory 22Rv1 prostate cancer cells in vitro.² Polymorphisms in the MTNR1A gene are associated with a higher risk of oral cancer and hepatocellular carcinoma and of developing distant metastases^3,4

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1. Dubocovich, M.L., Rivera-Bermudez, M.A., Gerdin, M.J., et al. Molecular pharmacology, regulation and function of mammalian melatonin receptors. Front. Biosci. 8, d1093-d1108 (2003).

2. Tam, C.W., Mo, C.W., Yao, K.M., et al. Signaling mechanisms of melatonin in antiproliferation of hormone-refractory 22Rv1 human prostate cancer cells: implications for prostate cancer chemoprevention. J. Pineal. Res. 42(2), 191-202 (2007).

3. Lin, F.Y., Lin, C.W., Yang, S.F., et al. Interactions between environmental factors and melatonin receptor type 1A polymorphism in relation to oral cancer susceptibility and clinicopathologic development. PLoS One 10(3), e0121677 (2015).

4. Su, S.C., Ho, Y.C., Liu, Y.F., et al. Association of melatonin membrane receptor 1A/1B gene polymorphisms with the occurrence and metastasis of hepatocellular carcinoma. Oncotarget 8(49), 85655-85669 (2017).