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Gene and Protein Information ![]() |
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class A G protein-coupled receptor | ||||||
Species | TM | AA | Chromosomal Location | Gene Symbol | Gene Name | Reference |
Human | 7 | 385 | 19p13.11 | F2RL3 | F2R like thrombin or trypsin receptor 3 | |
Mouse | 7 | 396 | 8 B3.3 | F2rl3 | F2R like thrombin or trypsin receptor 3 | |
Rat | 7 | 395 | 16p14 | F2rl3 | F2R like thrombin or trypsin receptor 3 |
Database Links ![]() |
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Specialist databases | |
GPCRdb | par4_human (Hs), par4_mouse (Mm), par4_rat (Rn) |
Other databases | |
Alphafold | Q96RI0 (Hs), O88634 (Mm), Q920E0 (Rn) |
ChEMBL Target | CHEMBL4691 (Hs), CHEMBL4879420 (Mm) |
Ensembl Gene | ENSG00000127533 (Hs), ENSMUSG00000050147 (Mm), ENSRNOG00000068093 (Rn) |
Entrez Gene | 9002 (Hs), 14065 (Mm), 116498 (Rn) |
Human Protein Atlas | ENSG00000127533 (Hs) |
KEGG Gene | hsa:9002 (Hs), mmu:14065 (Mm), rno:116498 (Rn) |
OMIM | 602779 (Hs) |
Pharos | Q96RI0 (Hs) |
RefSeq Nucleotide | NM_003950 (Hs), NM_007975 (Mm), NM_053808 (Rn) |
RefSeq Protein | NP_003941 (Hs), NP_032001 (Mm), NP_446260 (Rn) |
UniProtKB | Q96RI0 (Hs), O88634 (Mm), Q920E0 (Rn) |
Wikipedia | F2RL3 (Hs) |
Natural/Endogenous Ligands ![]() |
cathepsin G {Sp: Human} , cathepsin G {Sp: Mouse} , cathepsin G {Sp: Rat} |
thrombin {Sp: Human} , thrombin {Sp: Mouse} , thrombin {Sp: Rat} |
serine proteases |
Agonist proteases (Human) |
thrombin (F2, P00734), trypsin, cathepsin G (CTSG, P08311) |
Download all structure-activity data for this target as a CSV file
Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Expression Datasets ![]() |
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Physiological Consequences of Altering Gene Expression ![]() |
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Phenotypes, Alleles and Disease Models ![]() |
Mouse data from MGI | ||||||||||||||||||||||||
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Biologically Significant Variants ![]() |
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1. Cornelissen I, Palmer D, David T, Wilsbacher L, Concengco C, Conley P, Pandey A, Coughlin SR. (2010) Roles and interactions among protease-activated receptors and P2ry12 in hemostasis and thrombosis. Proc Natl Acad Sci USA, 107 (43): 18605-10. [PMID:20930120]
2. Covic L, Misra M, Badar J, Singh C, Kuliopulos A. (2002) Pepducin-based intervention of thrombin-receptor signaling and systemic platelet activation. Nat Med, 8 (10): 1161-5. [PMID:12357249]
3. Edelstein LC, Simon LM, Lindsay CR, Kong X, Teruel-Montoya R, Tourdot BE, Chen ES, Ma L, Coughlin S, Nieman M et al.. (2014) Common variants in the human platelet PAR4 thrombin receptor alter platelet function and differ by race. Blood, 124 (23): 3450-8. [PMID:25293779]
4. Hamilton JR, Cornelissen I, Coughlin SR. (2004) Impaired hemostasis and protection against thrombosis in protease-activated receptor 4-deficient mice is due to lack of thrombin signaling in platelets. J Thromb Haemost, 2 (8): 1429-35. [PMID:15304051]
5. Lee H, Sturgeon SA, Jackson SP, Hamilton JR. (2012) The contribution of thrombin-induced platelet activation to thrombus growth is diminished under pathological blood shear conditions. Thromb Haemost, 107 (2): 328-37. [PMID:22187047]
6. Luyendyk JP, Mackman N, Sullivan BP. (2011) Role of fibrinogen and protease-activated receptors in acute xenobiotic-induced cholestatic liver injury. Toxicol Sci, 119 (1): 233-43. [PMID:20974703]
7. Mao Y, Zhang M, Tuma RF, Kunapuli SP. (2010) Deficiency of PAR4 attenuates cerebral ischemia/reperfusion injury in mice. J Cereb Blood Flow Metab, 30 (5): 1044-52. [PMID:20087365]
8. Miller MM, Banville J, Friends TJ, Gagnon M, Hangeland JJ, Lavallée JF, Martel A, O'Grady H, Rémillard R, Ruediger E et al.. (2019) Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy. J Med Chem, 62 (16): 7400-7416. [PMID:31246024]
9. Muehlschlegel JD, Perry TE, Liu KY, Fox AA, Smith SA, Lichtner P, Collard CD, Shernan SK, Hartwig JH, Body SC et al.. (2012) Polymorphism in the protease-activated receptor-4 gene region associates with platelet activation and perioperative myocardial injury. Am J Hematol, 87 (2): 161-6. [PMID:22228373]
10. Priestley ES, Banville J, Deon D, Dubé L, Gagnon M, Guy J, Lapointe P, Lavallée JF, Martel A, Plamondon S et al.. (2022) Discovery of Two Novel Antiplatelet Clinical Candidates (BMS-986120 and BMS-986141) That Antagonize Protease-Activated Receptor 4. J Med Chem, 65 (13): 8843-8854. [PMID:35729784]
11. Ramachandran R, Mihara K, Thibeault P, Vanderboor CM, Petri B, Saifeddine M, Bouvier M, Hollenberg MD. (2017) Targeting a Proteinase-Activated Receptor 4 (PAR4) Carboxyl Terminal Motif to Regulate Platelet Function. Mol Pharmacol, 91 (4): 287-295. [PMID:28126849]
12. Sambrano GR, Weiss EJ, Zheng YW, Huang W, Coughlin SR. (2001) Role of thrombin signalling in platelets in haemostasis and thrombosis. Nature, 413 (6851): 74-8. [PMID:11544528]
13. Wen W, Young SE, Duvernay MT, Schulte ML, Nance KD, Melancon BJ, Engers J, Locuson 2nd CW, Wood MR, Daniels JS et al.. (2014) Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354. Bioorg Med Chem Lett, 24 (19): 4708-13. [PMID:25176330]
14. Wong PC, Seiffert D, Bird JE, Watson CA, Bostwick JS, Giancarli M, Allegretto N, Hua J, Harden D, Guay J et al.. (2017) Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding. Sci Transl Med, 9 (371). [PMID:28053157]