Target Information
Target General Infomation | |||||
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Target ID |
T99954
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Former ID |
TTDS00170
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Target Name |
Prostacyclin receptor
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Gene Name |
PTGIR
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Synonyms |
IP prostanoid receptor; PGI receptor; Prostaglandin I2 receptor; Prostanoid IP receptor; PTGIR
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Target Type |
Successful
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Disease | Aborting second-trimester pregnancy [ICD9: 779.6; ICD10: O04] | ||||
Asthma [ICD10: J45] | |||||
Chronic renal failure [ICD9: 585.9585.1-585.5403; ICD10: N18] | |||||
Gout [ICD9: 274.00274.1274.8274.9; ICD10: M10] | |||||
Hypertension [ICD9: 401; ICD10: I10-I16] | |||||
Medical abortion [ICD9: 779.6; ICD10: O04] | |||||
Pulmonary hypertension [ICD9: 416; ICD10: I27.0, I27.2] | |||||
Pulmonary arterial hypertension [ICD9: 416; ICD10: I27.0, I27.2] | |||||
Pulmonary arterial hypertension; Thrombosis [ICD9:416, 437.6, 453, 671.5, 671.9; ICD10: I27.0, I27.2, I80-I82] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Function |
Receptor for prostacyclin (prostaglandin I2 or PGI2).The activity of this receptor is mediated by G(s) proteins which activate adenylate cyclase.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T99954
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UniProt ID | |||||
Sequence |
MADSCRNLTYVRGSVGPATSTLMFVAGVVGNGLALGILSARRPARPSAFAVLVTGLAATD
LLGTSFLSPAVFVAYARNSSLLGLARGGPALCDAFAFAMTFFGLASMLILFAMAVERCLA LSHPYLYAQLDGPRCARLALPAIYAFCVLFCALPLLGLGQHQQYCPGSWCFLRMRWAQPG GAAFSLAYAGLVALLVAAIFLCNGSVTLSLCRMYRQQKRHQGSLGPRPRTGEDEVDHLIL LALMTVVMAVCSLPLTIRCFTQAVAPDSSSEMGDLLAFRFYAFNPILDPWVFILFRKAVF QRLKLWVCCLCLGPAHGDSQTPLSQLASGRRDPRAPSAPVGKEGSCVPLSAWGEGQVEPL PPTQQSSGSAVGTSSKAEASVACSLC |
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Drugs and Mode of Action | |||||
Drug(s) | Dinoprost Tromethamine | Drug Info | Approved | Aborting second-trimester pregnancy | [550687] |
Epoprostenol | Drug Info | Approved | Pulmonary hypertension | [536294], [539216] | |
Misoprostol | Drug Info | Approved | Medical abortion | [536361], [539235] | |
Selexipag | Drug Info | Approved | Pulmonary arterial hypertension; Thrombosis | [523009], [542553] | |
Treprostinil | Drug Info | Approved | Pulmonary arterial hypertension | [536294], [541139] | |
LAROPIPRANT | Drug Info | Phase 4 | Discovery agent | [523049], [540312] | |
esuberaprost | Drug Info | Phase 3 | Gout | [533330] | |
APD-811 | Drug Info | Phase 2 | Pulmonary hypertension | [524977] | |
Clinprost | Drug Info | Discontinued in Preregistration | Asthma | [545407] | |
Ataprost | Drug Info | Discontinued in Phase 3 | Asthma | [545086] | |
YM533 | Drug Info | Discontinued in Phase 3 | Chronic renal failure | [548502] | |
OP-2507 | Drug Info | Discontinued in Phase 2 | Hypertension | [545937] | |
AP-227 | Drug Info | Terminated | Discovery agent | [545879] | |
EPTALOPROST | Drug Info | Terminated | Solid tumours | [545433] | |
Agonist | AFP-07 | Drug Info | [534364] | ||
APD-811 | Drug Info | [544177] | |||
BMY 45778 | Drug Info | [534390] | |||
butaprost (free acid form) | Drug Info | [525673] | |||
carbacyclin | Drug Info | [525673] | |||
cicaprost | Drug Info | [534478] | |||
EP 157 | Drug Info | [533410] | |||
Epoprostenol | Drug Info | [534863], [535570], [537162] | |||
esuberaprost | Drug Info | [533330] | |||
isocarbacyclin | Drug Info | [534478] | |||
Selexipag | Drug Info | [531815] | |||
TEI-9063 | Drug Info | [534390] | |||
Treprostinil | Drug Info | [537188] | |||
U46619 | Drug Info | [525673] | |||
Inhibitor | AP-227 | Drug Info | [551275] | ||
FR-181157 | Drug Info | [528308] | |||
FR-193262 | Drug Info | [527580] | |||
LAROPIPRANT | Drug Info | [528672] | |||
Modulator | Ataprost | Drug Info | [533933] | ||
Clinprost | Drug Info | [534510] | |||
EPTALOPROST | Drug Info | [533698], [551871] | |||
OP-2507 | Drug Info | [531344] | |||
Prostacyclin analog | Drug Info | [543782] | |||
YM533 | Drug Info | [543782] | |||
Antagonist | BAY-73-1449 | Drug Info | [529584] | ||
Dinoprost Tromethamine | Drug Info | [535633], [537893] | |||
Misoprostol | Drug Info | [535633], [537850], [538121] | |||
RO1138452 | Drug Info | [527911] | |||
RO3244794 | Drug Info | [527911] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
Vascular smooth muscle contraction | |||||
Platelet activation | |||||
Pathway Interaction Database | Thromboxane A2 receptor signaling | ||||
PathWhiz Pathway | Intracellular Signalling Through Prostacyclin Receptor and Prostacyclin | ||||
Reactome | Prostanoid ligand receptors | ||||
G alpha (s) signalling events | |||||
WikiPathways | Prostaglandin Synthesis and Regulation | ||||
GPCRs, Class A Rhodopsin-like | |||||
Small Ligand GPCRs | |||||
Endothelin Pathways | |||||
Platelet homeostasis | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 523009 | ClinicalTrials.gov (NCT01106014) Selexipag (ACT-293987) in Pulmonary Arterial Hypertension, GRIPHON Trial. U.S. National Institutes of Health. | ||||
Ref 523049 | ClinicalTrials.gov (NCT01126073) Niacin/Laropiprant and Endothelial Function. U.S. National Institutes of Health. | ||||
Ref 524977 | ClinicalTrials.gov (NCT02279745) Long Term Safety and Efficacy of APD811 in Pulmonary Arterial Hypertension. U.S. National Institutes of Health. | ||||
Ref 533330 | Specific binding of the new stable epoprostenol analogue beraprost sodium to prostacyclin receptors on human and rat platelets. Arzneimittelforschung. 1989 Apr;39(4):495-9. | ||||
Ref 536294 | Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 539216 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1915). | ||||
Ref 539235 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1936). | ||||
Ref 540312 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3356). | ||||
Ref 541139 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5820). | ||||
Ref 542553 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7552). | ||||
Ref 545086 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002073) | ||||
Ref 545407 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003132) | ||||
Ref 545433 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003249) | ||||
Ref 545879 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005184) | ||||
Ref 545937 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005417) | ||||
Ref 525673 | The utilization of recombinant prostanoid receptors to determine the affinities and selectivities of prostaglandins and related analogs. Biochim Biophys Acta. 2000 Jan 17;1483(2):285-93. | ||||
Ref 527580 | Bioorg Med Chem Lett. 2005 Jul 1;15(13):3279-83.Discovery of new diphenyloxazole derivatives containing a pyrrolidine ring: orally active prostacyclin mimetics. Part 2. | ||||
Ref 527911 | RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br J Pharmacol. 2006 Feb;147(3):335-45. | ||||
Ref 528308 | Bioorg Med Chem Lett. 2006 Sep 15;16(18):4861-4. Epub 2006 Jul 11.Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6. | ||||
Ref 528672 | J Med Chem. 2007 Feb 22;50(4):794-806.Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524). | ||||
Ref 529584 | Vascular actions of the prostacyclin receptor antagonist BAY 73-1449 in the portal hypertensive rat. Eur J Pharmacol. 2008 Aug 20;590(1-3):322-6. | ||||
Ref 531344 | Effect of a prostaglandin I(2) analog on the expression of thrombomodulin in liver and spleen endothelial cells after an extensive hepatectomy. Surg Today. 2011 Feb;41(2):230-6. | ||||
Ref 531815 | Selexipag: an oral, selective prostacyclin receptor agonist for the treatment of pulmonary arterial hypertension. Eur Respir J. 2012 Oct;40(4):874-80. Epub 2012 Feb 23. | ||||
Ref 533330 | Specific binding of the new stable epoprostenol analogue beraprost sodium to prostacyclin receptors on human and rat platelets. Arzneimittelforschung. 1989 Apr;39(4):495-9. | ||||
Ref 533410 | Prostaglandin endoperoxide analogues which are both thromboxane receptor antagonists and prostacyclin mimetics. Br J Pharmacol. 1986 Mar;87(3):543-51. | ||||
Ref 533933 | Pharmacokinetics of intravenous ataprost alfadex, a new prostaglandin I2 analog in healthy volunteers. Int J Clin Pharmacol Ther Toxicol. 1993 Aug;31(8):373-5. | ||||
Ref 534364 | 7,7-Difluoroprostacyclin derivative, AFP-07, a highly selective and potent agonist for the prostacyclin receptor. Prostaglandins. 1997 Feb;53(2):83-90. | ||||
Ref 534390 | Relaxant actions of nonprostanoid prostacyclin mimetics on human pulmonary artery. J Cardiovasc Pharmacol. 1997 Apr;29(4):525-35. | ||||
Ref 534478 | Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells. Br J Pharmacol. 1997 Sep;122(2):217-24. | ||||
Ref 534510 | Protective effect of a prostaglandin I2 analog, TEI-7165, on ischemic neuronal damage in gerbils. Brain Res. 1997 Sep 26;769(2):321-8. | ||||
Ref 534863 | Expression of human hexosaminidase-A phenotype depends on genes assigned to chromosomes 5 and 15. Birth Defects Orig Artic Ser. 1976;12(7):192-6. | ||||
Ref 535570 | Signaling through Gi family members in platelets. Redundancy and specificity in the regulation of adenylyl cyclase and other effectors. J Biol Chem. 2002 Nov 29;277(48):46035-42. Epub 2002 Sep 23. | ||||
Ref 535633 | Palmitoylation of the human prostacyclin receptor. Functional implications of palmitoylation and isoprenylation. J Biol Chem. 2003 Feb 28;278(9):6947-58. Epub 2002 Dec 17. | ||||
Ref 537162 | Novel signaling pathways promote a paracrine wave of prostacyclin-induced vascular smooth muscle differentiation. J Mol Cell Cardiol. 2009 May;46(5):682-94. Epub 2009 Jan 23. | ||||
Ref 537188 | Dosing considerations in the use of intravenous prostanoids in pulmonary arterial hypertension: an experience-based review. Am Heart J. 2009 Apr;157(4):625-35. | ||||
Ref 537850 | Structural organization and chromosomal assignment of the human prostacyclin receptor gene. Genomics. 1995 May 1;27(1):142-8. | ||||
Ref 537893 | Molecular cloning of human prostacyclin receptor cDNA and its gene expression in the cardiovascular system. Circulation. 1994 Oct;90(4):1643-7. | ||||
Ref 538121 | The future potential of eicosanoids and their inhibitors in paediatric practice. Drugs. 1998 Aug;56(2):169-76. | ||||
Ref 543782 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 345). |
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