Prostacyclin receptor

Prostacyclin receptor

Prostacyclin receptor (or prostaglandin I2 receptor) is a receptor for prostacyclin.

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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.cite web | title = Entrez Gene: PTGIR prostaglandin I2 (prostacyclin) receptor (IP)| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=5739| accessdate = ]

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. cite book |author=Walter F., PhD. Boron |title=Medical Physiology: A Cellular And Molecular Approaoch |publisher=Elsevier/Saunders |location= |year= |pages= |isbn=1-4160-2328-3 |oclc= |doi= Page 479 ]

Gene

The receptor is encoded by the human gene PTGIR.cite web | title = Entrez Gene: PTGIR prostaglandin I2 (prostacyclin) receptor (IP)| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=5739| accessdate = ]

ee also

* Eicosanoid receptor

References

Further reading

PBB_Further_reading
citations =
*cite journal | author=Coleman RA, Smith WL, Narumiya S |title=International Union of Pharmacology classification of prostanoid receptors: properties, distribution, and structure of the receptors and their subtypes. |journal=Pharmacol. Rev. |volume=46 |issue= 2 |pages= 205–29 |year= 1994 |pmid= 7938166 |doi=
*cite journal | author=Rauvala H, Peng HB |title=HB-GAM (heparin-binding growth-associated molecule) and heparin-type glycans in the development and plasticity of neuron-target contacts. |journal=Prog. Neurobiol. |volume=52 |issue= 2 |pages= 127–44 |year= 1997 |pmid= 9185236 |doi=
*cite journal | author=Smyth EM, FitzGerald GA |title=Human prostacyclin receptor. |journal=Vitam. Horm. |volume=65 |issue= |pages= 149–65 |year= 2003 |pmid= 12481546 |doi=
*cite journal | author=Boie Y, Rushmore TH, Darmon-Goodwin A, "et al." |title=Cloning and expression of a cDNA for the human prostanoid IP receptor. |journal=J. Biol. Chem. |volume=269 |issue= 16 |pages= 12173–8 |year= 1994 |pmid= 7512962 |doi=
*cite journal | author=Katsuyama M, Sugimoto Y, Namba T, "et al." |title=Cloning and expression of a cDNA for the human prostacyclin receptor. |journal=FEBS Lett. |volume=344 |issue= 1 |pages= 74–8 |year= 1994 |pmid= 7514139 |doi=
*cite journal | author=Ogawa Y, Tanaka I, Inoue M, "et al." |title=Structural organization and chromosomal assignment of the human prostacyclin receptor gene. |journal=Genomics |volume=27 |issue= 1 |pages= 142–8 |year= 1995 |pmid= 7665161 |doi=
*cite journal | author=Duncan AM, Anderson LL, Funk CD, "et al." |title=Chromosomal localization of the human prostanoid receptor gene family. |journal=Genomics |volume=25 |issue= 3 |pages= 740–2 |year= 1995 |pmid= 7759114 |doi=
*cite journal | author=Nakagawa O, Tanaka I, Usui T, "et al." |title=Molecular cloning of human prostacyclin receptor cDNA and its gene expression in the cardiovascular system. |journal=Circulation |volume=90 |issue= 4 |pages= 1643–7 |year= 1994 |pmid= 7923647 |doi=
*cite journal | author=Bonaldo MF, Lennon G, Soares MB |title=Normalization and subtraction: two approaches to facilitate gene discovery. |journal=Genome Res. |volume=6 |issue= 9 |pages= 791–806 |year= 1997 |pmid= 8889548 |doi=
*cite journal | author=Sasaki Y, Takahashi T, Tanaka I, "et al." |title=Expression of prostacyclin receptor in human megakaryocytes. |journal=Blood |volume=90 |issue= 3 |pages= 1039–46 |year= 1997 |pmid= 9242534 |doi=
*cite journal | author=Fisch A, Tobusch K, Veit K, "et al." |title=Prostacyclin receptor desensitization is a reversible phenomenon in human platelets. |journal=Circulation |volume=96 |issue= 3 |pages= 756–60 |year= 1997 |pmid= 9264479 |doi=
*cite journal | author=Smyth EM, Li WH, FitzGerald GA |title=Phosphorylation of the prostacyclin receptor during homologous desensitization. A critical role for protein kinase c. |journal=J. Biol. Chem. |volume=273 |issue= 36 |pages= 23258–66 |year= 1998 |pmid= 9722557 |doi=
*cite journal | author=Kömhoff M, Lesener B, Nakao K, "et al." |title=Localization of the prostacyclin receptor in human kidney. |journal=Kidney Int. |volume=54 |issue= 6 |pages= 1899–908 |year= 1999 |pmid= 9853255 |doi= 10.1046/j.1523-1755.1998.00213.x
*cite journal | author=Hayes JS, Lawler OA, Walsh MT, Kinsella BT |title=The prostacyclin receptor is isoprenylated. Isoprenylation is required for efficient receptor-effector coupling. |journal=J. Biol. Chem. |volume=274 |issue= 34 |pages= 23707–18 |year= 1999 |pmid= 10446129 |doi=
*cite journal | author=Smyth EM, Austin SC, Reilly MP, FitzGerald GA |title=Internalization and sequestration of the human prostacyclin receptor. |journal=J. Biol. Chem. |volume=275 |issue= 41 |pages= 32037–45 |year= 2000 |pmid= 10889200 |doi= 10.1074/jbc.M003873200
*cite journal | author=Lawler OA, Miggin SM, Kinsella BT |title=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. |journal=J. Biol. Chem. |volume=276 |issue= 36 |pages= 33596–607 |year= 2001 |pmid= 11443126 |doi= 10.1074/jbc.M104434200
*cite journal | author=Zhang Z, Austin SC, Smyth EM |title=Glycosylation of the human prostacyclin receptor: role in ligand binding and signal transduction. |journal=Mol. Pharmacol. |volume=60 |issue= 3 |pages= 480–7 |year= 2001 |pmid= 11502878 |doi=
*cite journal | author=Fortier I, Patry C, Lora M, "et al." |title=Immunohistochemical localization of the prostacyclin receptor (IP) human bone. |journal=Prostaglandins Leukot. Essent. Fatty Acids |volume=65 |issue= 2 |pages= 79–83 |year= 2001 |pmid= 11545623 |doi= 10.1054/plef.2001.0292

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