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MrgX2 Is a High Potency Cortistatin Receptor Expressed in Dorsal Root Ganglion
Open accessAbstract
MrgX2 is a recently identified orphan G-protein-coupled receptor whose ligand and physiological function were unknown. Here we describe cortistatin, a neuropeptide for which no specific receptor has been identified previously, as a high potency ligand at MrgX2. Cortistatin has several biological functions including roles in sleep regulation, locomotor activity, and cortical function. Using a "reverse pharmacology" approach, we have identified a number of additional cyclic peptide agonists for MrgX2, determined their rank order of potency, and demonstrated that this receptor has a pharmacological profile distinct from the other characterized members of the Mrg (Mas-related genes) family. In MrgX2-expressing cells, cortistatin-stimulated increases in intracellular Ca2+ but had no effect on basal or forskolin-stimulated cAMP levels, suggesting that this receptor is Gq-coupled. Immunohistochemical and quantitative PCR studies show MrgX2 to have a limited expression profile, both peripheral and within the central nervous system, with highest levels in dorsal root ganglion.
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Metadata
- Authors
- Robas, N., Mead, E., & Fidock, M.
- Venue
- Journal of Biological Chemistry
- Publisher
- Elsevier BV
- Published
- 2003-11
- Volume
- 278
- Issue
- 45
- Pages
- 44400-44404
- ISSN
- 0021-9258 (ISSN-L)
- OpenAlex
- W1986027512
- Cited by
- 249
- References
- 0
- FWCI
- 5.44
- Type
- journal article
- Language
- en
- Open access
- hybrid
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- Robas, N., Mead, E., & Fidock, M. (2003). MrgX2 Is a High Potency Cortistatin Receptor Expressed in Dorsal Root Ganglion. Journal of Biological Chemistry. https://doi.org/10.1074/jbc.m302456200
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