Proteinase-activated receptor 4

GWB-C3B8FE

Receptor for activated thrombin or trypsin coupled to G proteins that stimulate phosphoinositide hydrolysis. May play a role in platelets activation.

Widely expressed with highest levels in lung pancreas thyroid testis and small intestine. Not expressed in brain kidney spinal cord and peripheral blood leukocytes. Also detected in platelets.

Belongs to the G-protein coupled receptor 1 family [view classification]. Summary: Coagulation factor II (thrombin) receptor-like 3 (F2RL3) is a member of the large family of 7-transmembrane-region receptors that couple to guanosine-nucleotide-binding proteins. F2RL3 is also a member of the protease-activated receptor family. F2RL3 is activated by proteolytic cleavage of its extracellular amino terminus. The new amino terminus functions as a tethered ligand and activates the receptor. F2RL3 is activated by thrombin and trypsin. [1] Lova P. Campus F. Lombardi R. Cattaneo M. Sinigaglia F. Balduini C. and Torti M. Contribution of protease-activated receptors 1 and 4 and glycoprotein Ib-IX-V in the G(i)-independent activation of platelet Rap1B by thrombin[2] Soslau G. Goldenberg S. J. Class R. and Jameson B. et al. Differential activation and inhibition of human platelet thrombin receptors by structurally distinct alpha- beta- and gamma-thrombin[3] Quinton T. M. Kim S. Derian C. K. Jin J. and Kunapuli S. P. et al. Plasmin-mediated activation of platelets occurs by cleavage of protease-activated receptor 4[4] Dubois C. Steiner B. and Meyer Reigner S. C. et al. Contribution of PAR-1 PAR-4 and GPIbalpha in intracellular signaling leading to the cleavage of the beta3 cytoplasmic domain during thrombin-induced platelet aggregation[5] Jacques S. L. and Kuliopulos A. et al. Protease-activated receptor-4 uses dual prolines and an anionic retention motif for thrombin recognition and cleavage[6] Kahn M. L. Hammes S. R. Botka C. Coughlin S. R. Gene and locus structure and chromosomal localization of the protease-activated receptor gene family. [7] Kahn M. L. Zheng Y. -W. Huang W. Bigornia V. Zeng D. Moff S. Farese R. V. Jr. Tam C. Coughlin S. R. A dual thrombin receptor system for platelet activation. [8] Xu W. -F. Andersen H. Whitmore T. E. Presnell S. R. Yee D. P. Ching A. Gilbert T. Davie E. W. Foster D. C. Cloning and characterization of human protease-activated receptor 4. [9] King M. M. Aronstam R. S. Sharma S. V. cDNA clones of human proteins involved in signal transduction sequenced by the Guthrie cDNA resource center (www. cdna. org). [10] Rieder M. J. Carrington D. P. Chung M. -W. Lee K. L. Poel C. L. Yi Q. Nickerson D. A. SeattleSNPs. NHLBI HL66682 program for genomic applications UW-FHCRC Seattle WA (URL: http://pga. gs. washington. edu).