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Expression cloning of a high-affinity melatonin receptor from Xenopus dermal melanophores.
Open accessAbstract
Using an expression cloning strategy, a high-affinity melatonin receptor cDNA has been isolated from Xenopus laevis dermal melanophores. Transient expression of the cDNA in COS-7 cells resulted in high-affinity 2-[125I]-iodomelatonin binding (Kd = 6.3 +/- 0.3 x 10(-11) M). In addition, six ligands exhibited a rank order of inhibition of specific 2-[125I]iodomelatonin binding that was identical to that reported for endogenous high-affinity receptors. Functional studies of CHO cells stably expressing the receptor cDNA showed that melatonin acting through the cloned receptor inhibited forskolin-stimulated cAMP accumulation in a dose-dependent manner. Northern blot analysis showed that melatonin receptor transcripts are moderately expressed in Xenopus dermal melanophores. The cDNA encodes a protein of 420 amino acids, which contains seven hydrophobic segments. Structural analysis revealed that the receptor protein is a newly discovered member of the guanine nucleotide binding protein-coupled receptor family.
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Cited by
Brzezinski, A. (1997) · New England Journal of Medicine · doi:10.1056/nejm199701163360306 · Cited by 1,549
Reppert, S. M., Weaver, D. R., & Ebisawa, T. (1994) · Neuron · doi:10.1016/0896-6273(94)90055-8 · Cited by 1,096
Self-citationMolecular pharmacology regulation and function of mammalian melatonin receptors
Dubocovich, M. L. (2003) · Frontiers in Bioscience · doi:10.2741/1089 · Cited by 451
Rapid color change in fish and amphibians – function, regulation, and emerging applications
Nilsson Sköld, H., Aspengren, S., & Wallin, M. (2013) · Pigment Cell & Melanoma Research · doi:10.1111/pcmr.12040 · Cited by 329
Melatonin receptors, heterodimerization, signal transduction and binding sites: what's new?
Jockers, R., Maurice, P., Boutin, J. A., & Delagrange, P. (2008) · British Journal of Pharmacology · doi:10.1038/bjp.2008.184 · Cited by 293
Metadata
- Authors
- Ebisawa, T., Karne, S., Lerner, M. R., & Reppert, S. M.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 1994-06-21
- Volume
- 91
- Issue
- 13
- Pages
- 6133-6137
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2002226670
- Cited by
- 432
- References
- 0
- FWCI
- 17.66
- Type
- journal article
- Language
- en
- Open access
- green
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- Ebisawa, T., Karne, S., Lerner, M. R., & Reppert, S. M. (1994). Expression cloning of a high-affinity melatonin receptor from Xenopus dermal melanophores. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.91.13.6133
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