Prostacyclin receptor
| Prostaglandin I2 (prostacyclin) receptor (IP) | |||||||||||
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| Symbols | PTGIR ; IP; MGC102830; PRIPR | ||||||||||
| External IDs | Template:OMIM5 Template:MGI HomoloGene: 7496 | ||||||||||
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| File:PBB GE PTGIR 206187 at tn.png | |||||||||||
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| Species | Human | Mouse | |||||||||
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Prostacyclin receptor (or prostaglandin I2 receptor) is a receptor for prostacyclin.
It is a member of the G-protein coupled receptor family. Prostacyclin, the major product of cyclooxygenase in macrovascular endothelium, elicits a potent vasodilation and inhibition of platelet aggregation through binding to this receptor.[1]
Transduction
When binding a prostacyclin-molecule, the receptor changes conformation and activates Gs, with its activation of cAMP and increase in protein kinase A (PKA) activity.
In vasodilation
In vasodilation, the PKA activity causes phosphorylation of MLCK, decreasing its activity, resulting in dephosphorylation of MLC of myosin. The smooth muscle relaxation leads to vasodilation.[2]
Gene
The receptor is encoded by the human gene PTGIR.[1]
See also
References
- ↑ 1.0 1.1 "Entrez Gene: PTGIR prostaglandin I2 (prostacyclin) receptor (IP)".
- ↑ Walter F., PhD. Boron. Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 1-4160-2328-3. Page 479
Further reading
- Coleman RA, Smith WL, Narumiya S (1994). "International Union of Pharmacology classification of prostanoid receptors: properties, distribution, and structure of the receptors and their subtypes". Pharmacol. Rev. 46 (2): 205–29. PMID 7938166.
- Rauvala H, Peng HB (1997). "HB-GAM (heparin-binding growth-associated molecule) and heparin-type glycans in the development and plasticity of neuron-target contacts". Prog. Neurobiol. 52 (2): 127–44. PMID 9185236.
- Smyth EM, FitzGerald GA (2003). "Human prostacyclin receptor". Vitam. Horm. 65: 149–65. PMID 12481546.
- Boie Y, Rushmore TH, Darmon-Goodwin A; et al. (1994). "Cloning and expression of a cDNA for the human prostanoid IP receptor". J. Biol. Chem. 269 (16): 12173–8. PMID 7512962.
- Katsuyama M, Sugimoto Y, Namba T; et al. (1994). "Cloning and expression of a cDNA for the human prostacyclin receptor". FEBS Lett. 344 (1): 74–8. PMID 7514139.
- Ogawa Y, Tanaka I, Inoue M; et al. (1995). "Structural organization and chromosomal assignment of the human prostacyclin receptor gene". Genomics. 27 (1): 142–8. PMID 7665161.
- Duncan AM, Anderson LL, Funk CD; et al. (1995). "Chromosomal localization of the human prostanoid receptor gene family". Genomics. 25 (3): 740–2. PMID 7759114.
- Nakagawa O, Tanaka I, Usui T; et al. (1994). "Molecular cloning of human prostacyclin receptor cDNA and its gene expression in the cardiovascular system". Circulation. 90 (4): 1643–7. PMID 7923647.
- Bonaldo MF, Lennon G, Soares MB (1997). "Normalization and subtraction: two approaches to facilitate gene discovery". Genome Res. 6 (9): 791–806. PMID 8889548.
- Sasaki Y, Takahashi T, Tanaka I; et al. (1997). "Expression of prostacyclin receptor in human megakaryocytes". Blood. 90 (3): 1039–46. PMID 9242534.
- Fisch A, Tobusch K, Veit K; et al. (1997). "Prostacyclin receptor desensitization is a reversible phenomenon in human platelets". Circulation. 96 (3): 756–60. PMID 9264479.
- Smyth EM, Li WH, FitzGerald GA (1998). "Phosphorylation of the prostacyclin receptor during homologous desensitization. A critical role for protein kinase c.". J. Biol. Chem. 273 (36): 23258–66. PMID 9722557.
- Kömhoff M, Lesener B, Nakao K; et al. (1999). "Localization of the prostacyclin receptor in human kidney". Kidney Int. 54 (6): 1899–908. doi:10.1046/j.1523-1755.1998.00213.x. PMID 9853255.
- Hayes JS, Lawler OA, Walsh MT, Kinsella BT (1999). "The prostacyclin receptor is isoprenylated. Isoprenylation is required for efficient receptor-effector coupling". J. Biol. Chem. 274 (34): 23707–18. PMID 10446129.
- Smyth EM, Austin SC, Reilly MP, FitzGerald GA (2000). "Internalization and sequestration of the human prostacyclin receptor". J. Biol. Chem. 275 (41): 32037–45. doi:10.1074/jbc.M003873200. PMID 10889200.
- Lawler OA, Miggin SM, Kinsella BT (2001). "Protein kinase A-mediated phosphorylation of serine 357 of the mouse prostacyclin receptor regulates its coupling to G(s)-, to G(i)-, and to G(q)-coupled effector signaling". J. Biol. Chem. 276 (36): 33596–607. doi:10.1074/jbc.M104434200. PMID 11443126.
- Zhang Z, Austin SC, Smyth EM (2001). "Glycosylation of the human prostacyclin receptor: role in ligand binding and signal transduction". Mol. Pharmacol. 60 (3): 480–7. PMID 11502878.
- Fortier I, Patry C, Lora M; et al. (2001). "Immunohistochemical localization of the prostacyclin receptor (IP) human bone". Prostaglandins Leukot. Essent. Fatty Acids. 65 (2): 79–83. doi:10.1054/plef.2001.0292. PMID 11545623.
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