Target Information

Target General Infomation
Target ID
T36483
Former ID
TTDC00071
Target Name
Thrombin receptor
Gene Name
F2R
Synonyms
Coagulation factor II receptor; PAR-1; Protease activated receptor 1; Protease-activated receptor-1; Thrombin receptor; F2R
Target Type
Successful
Disease Atherosclerosis [ICD9: 414.0, 440; ICD10: I70]
Acute coronary syndrome [ICD9: 444; ICD10: I74]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Myocardial infarction [ICD9: 410; ICD10: I21, I22]
Restenosis [ICD10: I51.89]
Thrombosis [ICD9: 437.6, 453, 671.5, 671.9; ICD10: I80-I82]
Function
High affinity receptor for activated thrombin coupled to G proteins that stimulate phosphoinositide hydrolysis. May play a role in platelets activation and in vascular development.
BioChemical Class
GPCR rhodopsin
Target Validation
T36483
UniProt ID
P25116
Sequence
MGPRRLLLVAACFSLCGPLLSARTRARRPESKATNATLDPRSFLLRNPNDKYEPFWEDEE
KNESGLTEYRLVSINKSSPLQKQLPAFISEDASGYLTSSWLTLFVPSVYTGVFVVSLPLN
IMAIVVFILKMKVKKPAVVYMLHLATADVLFVSVLPFKISYYFSGSDWQFGSELCRFVTA
AFYCNMYASILLMTVISIDRFLAVVYPMQSLSWRTLGRASFTCLAIWALAIAGVVPLLLK
EQTIQVPGLNITTCHDVLNETLLEGYYAYYFSAFSAVFFFVPLIISTVCYVSIIRCLSSS
AVANRSKKSRALFLSAAVFCIFIICFGPTNVLLIAHYSFLSHTSTTEAAYFAYLLCVCVS
SISCCIDPLIYYYASSECQRYVYSILCCKESSDPSSYNSSGQLMASKMDTCSSNLNNSIY
KKLLT
Drugs and Mode of Action
Drug(s) Vorapaxar Drug Info Approved Myocardial infarction [533123], [540647], [551871]
E5555 Drug Info Phase 2 Acute coronary syndrome [522232], [540648]
FR-171113 Drug Info Terminated Thrombosis [546808]
RWJ-58259 Drug Info Terminated Restenosis [526902]
Antagonist E5555 Drug Info [531439], [531931]
RWJ-56110 Drug Info [525623]
SCH-602539 Drug Info [543783]
Vorapaxar Drug Info [537151], [537189], [537571]
Modulator FR-171113 Drug Info [525659]
mabs targeting PAR-1 Drug Info [543783]
RWJ-58259 Drug Info [526902]
Inhibitor SCH-205831 Drug Info [528902]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Rap1 signaling pathway
Calcium signaling pathway
cAMP signaling pathway
Neuroactive ligand-receptor interaction
Endocytosis
PI3K-Akt signaling pathway
Complement and coagulation cascades
Platelet activation
Regulation of actin cytoskeleton
Pathways in cancer
NetPath Pathway TGF_beta_Receptor Signaling Pathway
TCR Signaling Pathway
PANTHER Pathway Angiogenesis
Blood coagulation
Pathway Interaction Database PAR1-mediated thrombin signaling events
Reactome Common Pathway of Fibrin Clot Formation
Peptide ligand-binding receptors
G alpha (q) signalling events
Thrombin signalling through proteinase activated receptors (PARs)
WikiPathways Complement and Coagulation Cascades
Regulation of Actin Cytoskeleton
GPCRs, Class A Rhodopsin-like
IL1 and megakaryotyces in obesity
Apoptosis-related network due to altered Notch3 in ovarian cancer
Hematopoietic Stem Cell Differentiation
Gastrin-CREB signalling pathway via PKC and MAPK
Thrombin signalling through proteinase activated receptors (PARs)
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
Ref 522232ClinicalTrials.gov (NCT00619164) A Double-Blind Study of E5555 in Japanese Patients With Acute Coronary Syndrome. U.S. National Institutes of Health.
Ref 526902RWJ-58259: a selective antagonist of protease activated receptor-1. Cardiovasc Drug Rev. 2003 Winter;21(4):313-26.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 540647(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: 4047).
Ref 540648(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: 4048).
Ref 546808Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010405)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525623Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. Proc Natl Acad Sci U S A. 1999 Oct 26;96(22):12257-62.
Ref 525659In vitro antiplatelet profile of FR171113, a novel non-peptide thrombin receptor antagonist. Eur J Pharmacol. 1999 Nov 19;384(2-3):197-202.
Ref 526902RWJ-58259: a selective antagonist of protease activated receptor-1. Cardiovasc Drug Rev. 2003 Winter;21(4):313-26.
Ref 528902Bioorg Med Chem Lett. 2007 Aug 15;17(16):4509-13. Epub 2007 Jun 15.Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring.
Ref 531439Safety and tolerability of atopaxar in the treatment of patients with acute coronary syndromes: the lessons from antagonizing the cellular effects of Thrombin-Acute Coronary Syndromes Trial. Circulation. 2011 May 3;123(17):1843-53.
Ref 531931Atopaxar and its effects on markers of platelet activation and inflammation: results from the LANCELOT CAD program. J Thromb Thrombolysis. 2012 Jul;34(1):36-43.
Ref 537151Safety and tolerability of SCH 530348 in patients undergoing non-urgent percutaneous coronary intervention: a randomised, double-blind, placebo-controlled phase II study. Lancet. 2009 Mar 14;373(9667):919-28.
Ref 537189Novel antiplatelet strategies in acute coronary syndromes. Cleve Clin J Med. 2009 Apr;76 Suppl 1:S8-15.
Ref 537571In Process Citation. Pharm Unserer Zeit. 2009;38(4):320-8.
Ref 543783(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: 347).

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