Prostacyclin receptor

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Prostaglandin I2 (prostacyclin) receptor (IP)
Identifiers
Symbol(s) PTGIR; IP; MGC102830; PRIPR
External IDs OMIM: 600022 MGI: 99535 HomoloGene: 7496
RNA expression pattern

More reference expression data
Orthologs
Human Mouse
Entrez 5739 19222
Ensembl ENSG00000160013 ENSMUSG00000043017
Uniprot P43119 Q3U4F1
Refseq NM_000960 (mRNA)
NP_000951 (protein)		 NM_008967 (mRNA)
NP_032993 (protein)
Location Chr 19: 51.82 - 51.82 Mb Chr 7: 16.07 - 16.07 Mb
Pubmed search [1] [2]

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]

Contents

[edit] 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.

[edit] 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]

[edit] Gene

The receptor is encoded by the human gene PTGIR.[1]


[edit] See also

[edit] References

  1. ^ a b Entrez Gene: PTGIR prostaglandin I2 (prostacyclin) receptor (IP).
  2. ^ Walter F., PhD. Boron. Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 1-4160-2328-3.  Page 479

[edit] 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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v • d • e
Transmembrane receptor: G protein-coupled receptors
Class A: Rhodopsin like
Acetylcholine (M1, M2, M3, M4, M5) - Adrenergic (α1 (A, B, D), α2 (A, B, C), β1, β2, β3) - Adrenomedullin - Anaphylatoxin (C3a, C5a) - Angiotensin (1, 2) - Apelin - Bile acid - Bombesin (BRS3, GRPR, NMBR) - Bradykinin (B1, B2) - Cannabinoid (CB1, CB2) - Chemokine - Cholecystokinin (A, B) - Dopamine (D1, D2, D3, D4, D5) - Eicosanoid (CysLT (1, 2), LTB4 (1, 2), FPRL1, OXE, Prostaglandin ((DP (1, 2), EP (1, 2, 3, 4), PGF, Prostacyclin, Thromboxane) - EBI2 - Endothelin (A, B) - Estrogen - Formyl peptide (1, L1, L2) - Free fatty acid (1, 2, 3, 4) - FSH - Galanin (1, 2, 3) - Gonadotropin-releasing hormone (1, 2) - GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 79, 82, 83, 84, 85, 87, 88, 92, 101, 103, 119, 120, 132, 135, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 172, 173, 174, 176, 177, 182) - Ghrelin - Histamine (H1, H2, H3, H4) - Kisspeptin - Luteinizing hormone/choriogonadotropin - Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) - MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) - Melanocortin (1, 2, 3, 4, 5) - MCHR (1, 2) - Melatonin (1A, 1B)- Motilin - neuromedin (B, U (1, 2)) - Neuropeptide (B/W (1, 2), FF (1, 2), S, Y (1, 2, 4, 5)) - Neurotensin (1, 2) - Opioid (Delta, Kappa, Mu, Nociceptin, but not Sigma) - Olfactory - Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) - Orexin (1, 2) - Oxytocin - Oxoglutarate - PAF - Prokineticin (1, 2) - Prolactin-releasing peptide - Protease-activated (1, 2, 3, 4) - Purinergics (Adenosine (A1, A2a, A2b, A3), P2Y, (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)) - Relaxin (1, 2, 3, 4) - Somatostatin (1, 2, 3, 4, 5) - Serotonin, all but 5-HT3 (5-HT1 (A, B, D, E, F), 5-HT2 (A, B, C), 5-HT (4, 5A, 6, 7)) - SREB - Succinate - TAAR (1, 2, 3, 5, 6, 8, 9) - Tachykinin (1, 2, 3) - Thyrotropin - Thyrotropin-releasing hormone - Urotensin-II - Vasopressin (1A, 1B, 2)
Class B: Secretin like
Class C: Metabotropic
glutamate / pheromone
Calcium-sensing receptor - GABA B (1, 2) - Glutamate receptor (Metabotropic glutamate (1, 2, 3, 4, 5, 6, 7, 8)) - GPRC6A - GPR (156, 158, 179) - RAIG (1, 2, 3, 4) - Taste receptors (TAS1R (1, 2, 3) TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 38, 39, 40, 41, 43, 44, 45, 46, 47, 48, 49, 50))
Frizzled / Smoothened
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) - Smoothened