Therapeutic Targets Database
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TTD Target ID: TTDS00170

Target Information
NameProstacyclin receptor    
Type of targetSuccessful target    
SynonymsIP prostanoid receptor    
PGI receptor    
Prostaglandin I2 receptor    
Prostanoid IP receptor    
DiseaseAnalgesics    [1]
Diabetes mellitus    [2]
Inflammatory pain    [1]
Drug(s)Dinoprost TromethamineApprovedAborting second-trimester pregnancy (between 12th to 18th week of gestation)[3][4]
EpoprostenolApprovedPulmonary hypertension[5][6][7]
MisoprostolApprovedMedical abortion[3][8][9]
TreprostinilApprovedPulmonary arterial hypertension[10]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
PathwayNeuroactive ligand-receptor interaction
Vascular smooth muscle contraction
UniProt IDP43119
FunctionReceptor for prostacyclin (prostaglandin i2 or pgi2). The activity of this receptor is mediated by g(s) proteins which activate adenylate cyclase.    
SequenceMADSCRNLTYVRGSVGPATSTLMFVAGVVGNGLALGILSARRPARPSAFAVLVTGLAATD LLGTSFLSPAVFVAYARNSSLLGLARGGPALCDAFAFAMTFFGLASMLILFAMAVERCLA LSHPYLYAQLDGPRCARLALPAIYAFCVLFCALPLLGLGQHQQYCPGSWCFLRMRWAQPG GAAFSLAYAGLVALLVAAIFLCNGSVTLSLCRMYRQQKRHQGSLGPRPRTGEDEVDHLIL LALMTVVMAVCSLPLTIRCFTQAVAPDSSSEMGDLLAFRFYAFNPILDPWVFILFRKAVF QRLKLWVCCLCLGPAHGDSQTPLSQLASGRRDPRAPSAPVGKEGSCVPLSAWGEGQVEPL PPTQQSSGSAVGTSSKAEASVACSLC
Related US Patent6,417,186
6,569,860
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
InhibitorAP-227[11]
DG-041[12]
FR-181157[13]
FR-193262[14]
LAROPIPRANT[15]
AgonistEpoprostenol[5][6][7]
Treprostinil[10]
AntagonistDinoprost Tromethamine[3][4]
Misoprostol[3][8][9]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The role of IP prostanoid receptors in inflammatory pain. Trends Pharmacol Sci. 1998 Apr;19(4):141-7. To Reference
Ref 2Reduced IP receptors in STZ-induced diabetic rat kidneys and high-glucose-treated mesangial cells. Am J Physiol Renal Physiol. 2004 Oct;287(4):F673-81. Epub 2004 May 25. To Reference
Ref 3Palmitoylation 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. To Reference
Ref 4Molecular cloning of human prostacyclin receptor cDNA and its gene expression in the cardiovascular system. Circulation. 1994 Oct;90(4):1643-7. To Reference
Ref 5Novel 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. To Reference
Ref 6Signaling 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. To Reference
Ref 7Expression of human hexosaminidase-A phenotype depends on genes assigned to chromosomes 5 and 15. Birth Defects Orig Artic Ser. 1976;12(7):192-6. To Reference
Ref 8The future potential of eicosanoids and their inhibitors in paediatric practice. Drugs. 1998 Aug;56(2):169-76. To Reference
Ref 9Structural organization and chromosomal assignment of the human prostacyclin receptor gene. Genomics. 1995 May 1;27(1):142-8. To Reference
Ref 10Dosing considerations in the use of intravenous prostanoids in pulmonary arterial hypertension: an experience-based review. Am Heart J. 2009 Apr;157(4):625-35. To Reference
Ref 11Bioorg. Med. Chem. Lett. 5(10):1071-1076 (1995) To Reference
Ref 12J Med Chem. 2010 Jan 14;53(1):18-36.Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor antagonist, as a novel antiplatelet agent that does not prolong bleeding. To Reference
Ref 13Bioorg 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. To Reference
Ref 14Bioorg 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. To Reference
Ref 15J 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). To Reference



 

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