"ThrR" redirects here. For other uses, see THRR (disambiguation).
There are three known thrombin receptors (ThrR[1]), termed PAR1, PAR3 and PAR4 (PAR for protease-activated receptor).[2]
Activation of PARs
G-protein-coupled receptors that are responsible for the coagulation effects and responses of thrombin on cells are known as protease-activated receptors, or PARs. These receptors are members of the 7-transmembrane g protein-coupled family of receptors, however, their method of activation is unique. Unlike most G-protein-coupled receptors, PARs are irreversibly activated by proteolytic mechanism and therefore, are strictly regulated.
Thrombin is an allosteric serine protease that is an essential effector of coagulation that is produced at sites of vascular injury and plays a critical role in cellular response to blood-related diseases.[3] It binds to and cleaves the extracellular N-terminal domain of the receptor. A tethered ligand corresponding to the new N-terminus, SFLLRN, is then unmasked, binding to the second extracellular loop of the receptor and activating it.
^Darrow AL, Fung-Leung WP, Ye RD, Santulli RJ, Cheung WM, Derian CK, et al. (December 1996). "Biological consequences of thrombin receptor deficiency in mice". Thrombosis and Haemostasis. 76 (6): 860–866. doi:10.1055/s-0038-1650676. PMID 8972001. S2CID 13524388.
^Cirino G, Severino B (July 2010). "Thrombin receptors and their antagonists: an update on the patent literature". Expert Opinion on Therapeutic Patents. 20 (7): 875–884. doi:10.1517/13543776.2010.487864. PMID 20450349. S2CID 6409635.
^Heuberger DM, Schuepbach RA (December 2019). "Protease-activated receptors (PARs): mechanisms of action and potential therapeutic modulators in PAR-driven inflammatory diseases". Thrombosis Journal. 17 (1): 4. doi:10.1186/s12959-019-0194-8. PMC 6440139. PMID 30976204.
are three known thrombinreceptors (ThrR), termed PAR1, PAR3 and PAR4 (PAR for protease-activated receptor). G-protein-coupled receptors that are responsible...
forming a platelet plug. These platelets have thrombinreceptors on their surfaces that bind serum thrombin molecules, which in turn convert soluble fibrinogen...
Protease activated receptor 3 (PAR-3) also known as coagulation factor II receptor-like 2 (F2RL2) and thrombinreceptor-like 2, is a protein that in humans...
possibly influence vascular function, with some upregulation of the thrombinreceptor observed with etonogestrel in vascular smooth muscle cells in vitro...
name Zontivity, formerly known as SCH 530348) is a thrombinreceptor (protease-activated receptor, PAR-1) antagonist based on the natural product himbacine...
Protease-activated receptor 4 (PAR-4), also known as coagulation factor II (thrombin) receptor-like 3, is a protein that in humans is encoded by the F2RL3...
failed but an analog, vorapaxar, has been approved by the FDA as a thrombinreceptor antagonist. Chackalamannil S, Davies RJ, Wang Y, et al. (March 1999)...
or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It works by stopping...
(July 1987). "Structure and expression of human thrombomodulin, a thrombinreceptor on endothelium acting as a cofactor for protein C activation". The...
glucocorticoid activity of MPA may also result in an upregulation of the thrombinreceptor in blood vessel walls, which may contribute to procoagulant effects...
factor X, thrombin and fibrin. The main role of the tissue factor (TF) pathway is to generate a "thrombin burst", a process by which thrombin, the most...
fibrinolysis. Excess circulating thrombin results from the excess activation of the coagulation cascade. The excess thrombin cleaves fibrinogen, which ultimately...
THRR or variation, may refer to: Training heart rate range (THRR) Thrombinreceptor (ThrR) Thrr, Dog of Thunder (Marvel Comics), an anthropomorphic dog...
or a synthetic progestogen, and hence is an agonist of the progesterone receptor, the biological target of progestogens like progesterone. It has weak androgenic...
animals. Nonetheless, progesterone has been found to upregulate the thrombinreceptor in vascular smooth muscle cells in vitro, a glucocorticoid effect...
"G proteins of the G12 family are activated via thromboxane A2 and thrombinreceptors in human platelets". Proc. Natl. Acad. Sci. U.S.A. 91 (2): 504–8....
to increase thrombin production. Thrombin is a potent platelet activator, acting through Gq and G12. These are G protein-coupled receptors and they turn...
Hepatocyte growth factor receptor (HGF receptor) is a protein that in humans is encoded by the MET gene. The protein possesses tyrosine kinase activity...
melanoma progression and modulates expression of the thrombinreceptor protease activated receptor 1". Cancer Res. 64 (20): 7361–9. doi:10.1158/0008-5472...
inhibitors and ADP receptor inhibitors, while anticoagulants include vitamin K antagonists, direct oral anticoagulants (DOACs) and indirect thrombin inhibitors...
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