Protease-activated receptors in cancer: A systematic review
- Authors:
- Na Han
- Ketao Jin
- Kuifeng He
- Jiang Cao
- Lisong Teng
-
Affiliations: Sir Run Run Shaw Institute of Clinical Medicine, Zhejiang University: Key Laboratory of Biotherapy of Zhejiang Province, and Clinical Research Center, Second Affiliated Hospital, College of Medicine, Zhejiang University, Zhejiang 310003, P.R. China, Department of Surgical Oncology, First Affiliated Hospital, College of Medicine, Zhejiang University, Hangzhou, Zhejiang 310003, P.R. China - Published online on: April 8, 2011 https://doi.org/10.3892/ol.2011.291
- Pages: 599-608
This article is mentioned in:
Abstract
Mook OR, Frederiks WM and van Noorden CJ: The role of gelatinases in colorectal cancer progression and metastasis. Biochim Biophys Acta. 1705:69–89. 2004.PubMed/NCBI | |
López-Otín C and Matrisian LM: Emerging roles of proteases in tumour suppression. Nat Rev Cancer. 7:800–808. 2007.PubMed/NCBI | |
Déry O, Corvera CU, Steinhoff M and Bunnett NW: Proteinase-activated receptors: novel mechanisms of signaling by serine proteases. Am J Physiol. 274:C1429–C1452. 1998.PubMed/NCBI | |
Macfarlane SR, Seatter MJ, Kanke T, Hunter GD and Plevin R: Proteinase-activated receptors. Pharmacol Rev. 53:245–282. 2001.PubMed/NCBI | |
Coughlin SR: Thrombin signalling and protease-activated receptors. Nature. 407:258–264. 2000. View Article : Google Scholar : PubMed/NCBI | |
Coughlin SR: How the protease thrombin talks to cells. Proc Natl Acad Sci USA. 96:11023–11027. 1999. View Article : Google Scholar : PubMed/NCBI | |
Hollenberg MD and Compton SJ: International Union of Pharmacology. XXVIII Proteinase-activated receptors. Pharmacol Rev. 54:203–217. 2002. View Article : Google Scholar : PubMed/NCBI | |
Ossovskaya VS and Bunnett NW: Protease-activated receptors: contribution to physiology and disease. Physiol Rev. 84:579–621. 2004. View Article : Google Scholar : PubMed/NCBI | |
Vu TK, Hung DT, Wheaton VI and Coughlin SR: Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation. Cell. 64:1057–1068. 1991. View Article : Google Scholar : PubMed/NCBI | |
Ishihara H, Connolly AJ, Zeng D, Kahn ML, Zheng YW, Timmons C, Tram T and Coughlin SR: Protease-activated receptor 3 is a second thrombin receptor in humans. Nature. 386:502–506. 1997. View Article : Google Scholar : PubMed/NCBI | |
Xu WF, Andersen H, Whitmore TE, Presnell SR, Yee DP, Ching A, Gilbert T, Davie EW and Foster DC: Cloning and characterization of human protease-activated receptor 4. Proc Natl Acad Sci USA. 95:6642–6646. 1998. View Article : Google Scholar : PubMed/NCBI | |
Coughlin SR and Camerer E: PARticipation in inflammation. J Clin Invest. 111:25–27. 2003. View Article : Google Scholar | |
Kondo K and Kaelin WG Jr: The von Hippel-Lindau tumor suppressor gene. Exp Cell Res. 264:117–125. 2001. View Article : Google Scholar : PubMed/NCBI | |
Ohh M, Yauch RL, Lonergan KM, Whaley JM, Stemmer-Rachamimov AO, Louis DN, Gavin BJ, Kley N, Kaelin WG Jr and Iliopoulos O: The von Hippel-Lindau tumor suppressor protein is required for proper assembly of an extracellular fibronectin matrix. Mol Cell. 1:959–968. 1998. View Article : Google Scholar : PubMed/NCBI | |
Zacharski LR, Memoli VA, Morain WD, Schlaeppi JM and Rousseau SM: Cellular localization of enzymatically active thrombin in intact human tissues by hirudin binding. Thromb Haemost. 73:793–797. 1995. | |
Rickles FR, Patierno S and Fernandez PM: Tissue factor, thrombin, and cancer. Chest. 124:S58–S68. 2003. View Article : Google Scholar | |
Maragoudakis ME, Tsopanoglou NE and Andriopoulou P: Mechanism of thrombin-induced angiogenesis. Biochem Soc Trans. 30:173–177. 2002. View Article : Google Scholar : PubMed/NCBI | |
Tsopanoglou NE, Pipili-Synetos E and Maragoudakis ME: Thrombin promotes angiogenesis by a mechanism independent of fibrin formation. Am J Physiol. 264:C1302–C1307. 1993.PubMed/NCBI | |
Haralabopoulos GC, Grant DS, Kleinman HK and Maragoudakis ME: Thrombin promotes endothelial cell alignment in Matrigel in vitro and angiogenesis in vivo. Am J Physiol. 273:C239–C245. 1997.PubMed/NCBI | |
Fujiwara M, Jin E, Ghazizadeh M and Kawanami O: Activation of PAR4 induces a distinct actin fiber formation via p38 MAPK in human lung endothelial cells. J Histochem Cytochem. 53:1121–1129. 2005. View Article : Google Scholar : PubMed/NCBI | |
Vliagoftis H: Thrombin induces mast cell adhesion to fibronectin: evidence for involvement of protease-activated receptor-1. J Immunol. 169:4551–4558. 2002. View Article : Google Scholar : PubMed/NCBI | |
Kataoka H, Hamilton JR, McKemy DD, Camerer E, Zheng YW, Cheng A, Griffin C and Coughlin SR: Protease-activated receptors 1 and 4 mediate thrombin signaling in endothelial cells. Blood. 102:3224–3231. 2003. View Article : Google Scholar : PubMed/NCBI | |
Dimitropoulou C, Malkusch W, Fait E, Maragoudakis ME and Konerding MA: The vascular architecture of the chick chorioallantoic membrane: sequential quantitative evaluation using corrosion casting. Angiogenesis. 2:255–263. 1998. View Article : Google Scholar | |
Tsopanoglou NE and Maragoudakis ME: On the mechanism of thrombin-induced angiogenesis: inhibition of attachment of endothelial cells on basement membrane components. Angiogenesis. 1:192–200. 1998. View Article : Google Scholar : PubMed/NCBI | |
Maragoudakis ME, Kraniti N, Giannopoulou E, Alexopoulos K and Matsoukas J: Modulation of angiogenesis and progelatinase a by thrombin receptor mimetics and antagonists. Endothelium. 8:195–205. 2001. View Article : Google Scholar : PubMed/NCBI | |
Brooks PC, Strömblad S, Sanders LC, von Schalscha TL, Aimes RT, Stetler-Stevenson WG, Quigley JP and Cheresh DA: Localization of matrix metalloproteinase MMP-2 to the surface of invasive cells by interaction with integrin alpha v beta 3. Cell. 85:683–693. 1996. View Article : Google Scholar : PubMed/NCBI | |
Tsopanoglou NE and Maragoudakis ME: On the mechanism of thrombin-induced angiogenesis. Potentiation of vascular endothelial growth factor activity on endothelial cells by up-regulation of its receptors. J Biol Chem. 274:23969–23976. 1999. View Article : Google Scholar | |
Liu Y and Mueller BM: Protease-activated receptor-2 regulates vascular endothelial growth factor expression in MDA-MB-231 cells via MAPK pathways. Biochem Biophys Res Commun. 344:1263–1270. 2006. View Article : Google Scholar : PubMed/NCBI | |
Marutsuka K, Hatakeyama K, Sato Y, Yamashita A, Sumiyoshi A and Asada Y: Protease-activated receptor 2 (PAR2) mediates vascular smooth muscle cell migration induced by tissue factor/factor VIIa complex. Thromb Res. 107:271–276. 2002. View Article : Google Scholar : PubMed/NCBI | |
Oikonomopoulou K, Hansen KK, Saifeddine M, Vergnolle N, Tea I, Diamandis EP and Hollenberg MD: Proteinase-mediated cell signalling: targeting proteinase-activated receptors (PARs) by kallikreins and more. Biol Chem. 387:677–685. 2006.PubMed/NCBI | |
Brooks PC, Clark RA and Cheresh DA: Requirement of vascular integrin alpha v beta 3 for angiogenesis. Science. 264:569–571. 1994. View Article : Google Scholar : PubMed/NCBI | |
Nelken NA, Soifer SJ, O'Keefe J, Vu TK, Charo IF and Coughlin SR: Thrombin receptor expression in normal and atherosclerotic human arteries. J Clin Invest. 90:1614–1621. 1992. View Article : Google Scholar : PubMed/NCBI | |
Mirza H, Yatsula V and Bahou WF: The proteinase activated receptor-2 (PAR-2) mediates mitogenic responses in human vascular endothelial cells. J Clin Invest. 97:1705–1714. 1996. View Article : Google Scholar : PubMed/NCBI | |
Schmidt VA, Nierman WC, Maglott DR, Cupit LD, Moskowitz KA, Wainer JA and Bahou WF: The human proteinase-activated receptor-3 (PAR-3) gene. Identification within a Par gene cluster and characterization in vascular endothelial cells and platelets. J Biol Chem. 273:15061–15068. 1998. View Article : Google Scholar : PubMed/NCBI | |
Camerer E, Huang W and Coughlin SR: Tissue factor- and factor X-dependent activation of protease-activated receptor 2 by factor VIIa. Proc Natl Acad Sci USA. 97:5255–5260. 2000. View Article : Google Scholar : PubMed/NCBI | |
Riewald M and Ruf W: Mechanistic coupling of protease signaling and initiation of coagulation by tissue factor. Proc Natl Acad Sci USA. 98:7742–7747. 2001. View Article : Google Scholar : PubMed/NCBI | |
Camerer E, Kataoka H, Kahn M, Lease K and Coughlin SR: Genetic evidence that protease-activated receptors mediate factor Xa signaling in endothelial cells. J Biol Chem. 277:16081–16087. 2002. View Article : Google Scholar : PubMed/NCBI | |
Garcia JG, Davis HW and Patterson CE: Regulation of endothelial cell gap formation and barrier dysfunction: role of myosin light chain phosphorylation. J Cell Physiol. 163:510–522. 1995. View Article : Google Scholar : PubMed/NCBI | |
Vouret-Craviari V, Bourcier C, Boulter E and van Obberghen-Schilling E: Distinct signals via Rho GTPases and Src drive shape changes by thrombin and sphingosine-1-phosphate in endothelial cells. J Cell Sci. 115:2475–2484. 2002.PubMed/NCBI | |
Minami T, Sugiyama A, Wu SQ, Abid R, Kodama T and Aird WC: Thrombin and phenotypic modulation of the endothelium. Arterioscler Thromb Vasc Biol. 24:41–53. 2004. View Article : Google Scholar : PubMed/NCBI | |
Carmeliet P: Angiogenesis in life, disease and medicine. Nature. 438:932–936. 2005. View Article : Google Scholar : PubMed/NCBI | |
Pinedo HM, Verheul HM, D'Amato RJ and Folkman J: Involvement of platelets in tumour angiogenesis? Lancet. 352:1775–1777. 1998. View Article : Google Scholar : PubMed/NCBI | |
Kakkar AK, Levine MN, Kadziola Z, Lemoine NR, Low V, Patel HK, Rustin G, Thomas M, Quigley M and Williamson RC: Low molecular weight heparin, therapy with dalteparin, and survival in advanced cancer: the fragmin advanced malignancy outcome study (FAMOUS). J Clin Oncol. 22:1944–1948. 2004. View Article : Google Scholar : PubMed/NCBI | |
Klerk CP, Smorenburg SM, Otten HM, Lensing AW, Prins MH, Piovella F, Prandoni P, Bos MM, Richel DJ, van Tienhoven G and Büller HR: The effect of low molecular weight heparin on survival in patients with advanced malignancy. J Clin Oncol. 23:2130–2135. 2005. View Article : Google Scholar : PubMed/NCBI | |
Browder T, Folkman J and Pirie-Shepherd S: The hemostatic system as a regulator of angiogenesis. J Biol Chem. 275:1521–1524. 2000. View Article : Google Scholar : PubMed/NCBI | |
Folkman J, Browder T and Palmblad J: Angiogenesis research: guidelines for translation to clinical application. Thromb Haemost. 86:23–33. 2001.PubMed/NCBI | |
Kisucka J, Butterfield CE, Duda DG, Eichenberger SC, Saffaripour S, Ware J, Ruggeri ZM, Jain RK, Folkman J and Wagner DD: Platelets and platelet adhesion support angiogenesis while preventing excessive hemorrhage. Proc Natl Acad Sci USA. 103:855–860. 2006. View Article : Google Scholar : PubMed/NCBI | |
Ma L, Perini R, McKnight W, Dicay M, Klein A, Hollenberg MD and Wallace JL: Proteinase-activated receptors 1 and 4 counter-regulate endostatin and VEGF release from human platelets. Proc Natl Acad Sci USA. 102:216–220. 2005. View Article : Google Scholar : PubMed/NCBI | |
Pipili-Synetos E, Papadimitriou E and Maragoudakis ME: Evidence that platelets promote tube formation by endothelial cells on matrigel. Br J Pharmacol. 125:1252–1257. 1998. View Article : Google Scholar : PubMed/NCBI | |
Italiano JE Jr, Richardson JL, Patel-Hett S, Battinelli E, Zaslavsky A, Short S, Ryeom S, Folkman J and Klement GL: Angiogenesis is regulated by a novel mechanism: pro- and anti-angiogenic proteins are organized into separate platelet alpha granules and differentially released. Blood. 111:1227–1233. 2008. View Article : Google Scholar : PubMed/NCBI | |
Möhle R, Green D, Moore MA, Nachman RL and Rafii S: Constitutive production and thrombin-induced release of vascular endothelial growth factor by human megakaryocytes and platelets. Proc Natl Acad Sci USA. 94:663–668. 1997.PubMed/NCBI | |
Wartiovaara U, Salven P, Mikkola H, Lassila R, Kaukonen J, Joukov V, Orpana A, Ristimäki A, Heikinheimo M, Joensuu H, Alitalo K and Palotie A: Peripheral blood platelets express VEGF-C and VEGF which are released during platelet activation. Thromb Haemost. 80:171–175. 1998.PubMed/NCBI | |
Kaplan DR, Chao FC, Stiles CD, Antoniades HN and Scher CD: Platelet alpha granules contain a growth factor for fibroblasts. Blood. 53:1043–1052. 1979.PubMed/NCBI | |
Ben-Ezra J, Sheibani K, Hwang DL and Lev-Ran A: Megakaryocyte synthesis is the source of epidermal growth factor in human platelets. Am J Pathol. 137:755–759. 1990.PubMed/NCBI | |
Nakamura T, Tomita Y, Hirai R, Yamaoka K, Kaji K and Ichihara A: Inhibitory effect of transforming growth factor-beta on DNA synthesis of adult rat hepatocytes in primary culture. Biochem Biophys Res Commun. 133:1042–1050. 1985. View Article : Google Scholar : PubMed/NCBI | |
Hla T: Physiological and pathological actions of sphingosine 1-phosphate. Semin Cell Dev Biol. 15:513–520. 2004. View Article : Google Scholar : PubMed/NCBI | |
Galt SW, Lindemann S, Allen L, Medd DJ, Falk JM, McIntyre TM, Prescott SM, Kraiss LW, Zimmerman GA and Weyrich AS: Outside-in signals delivered by matrix metalloproteinase-1 regulate platelet function. Circ Res. 90:1093–1099. 2002. View Article : Google Scholar : PubMed/NCBI | |
Daly ME, Makris A, Reed M and Lewis CE: Hemostatic regulators of tumor angiogenesis: a source of anti-angiogenic agents for cancer treatment? J Natl Cancer Inst. 95:1660–1673. 2003.PubMed/NCBI | |
Iruela-Arispe ML, Bornstein P and Sage H: Thrombospondin exerts an anti-angiogenic effect on cord formation by endothelial cells in vitro. Proc Natl Acad Sci USA. 88:5026–5030. 1991. View Article : Google Scholar : PubMed/NCBI | |
Maione TE, Gray GS, Petro J, Hunt AJ, Donner AL, Bauer SI, Carson HF and Sharpe RJ: Inhibition of angiogenesis by recombinant human platelet factor-4 and related peptides. Science. 247:77–79. 1990. View Article : Google Scholar : PubMed/NCBI | |
Covic L, Gresser AL and Kuliopulos A: Biphasic kinetics of activation and signaling for PAR1 and PAR4 thrombin receptors in platelets. Biochemistry. 39:5458–5467. 2000. View Article : Google Scholar : PubMed/NCBI | |
Jamieson GA: Pathophysiology of platelet thrombin receptors. Thromb Haemost. 78:242–246. 1997.PubMed/NCBI | |
Cottrell GS, Coelho AM and Bunnett NW: Protease-activated receptors: the role of cell-surface proteolysis in signalling. Essays Biochem. 38:169–183. 2002.PubMed/NCBI | |
Kahn ML, Zheng YW, Huang W, Bigornia V, Zeng D, Moff S, Farese RV Jr, Tam C and Coughlin SR: A dual thrombin receptor system for platelet activation. Nature. 394:690–694. 1998. View Article : Google Scholar : PubMed/NCBI | |
Coughlin SR: Protease-activated receptors in hemostasis, thrombosis and vascular biology. J Thromb Haemost. 3:1800–1814. 2005. View Article : Google Scholar : PubMed/NCBI | |
Brass LF: Thrombin and platelet activation. Chest. 124:S18–S25. 2003. View Article : Google Scholar | |
Vandendries ER, Hamilton JR, Coughlin SR, Furie B and Furie BC: Par4 is required for platelet thrombus propagation but not fibrin generation in a mouse model of thrombosis. Proc Natl Acad Sci USA. 104:288–292. 2007. View Article : Google Scholar : PubMed/NCBI | |
Holinstat M, Voss B, Bilodeau ML and Hamm HE: Protease-activated receptors differentially regulate human platelet activation through a phosphatidic acid-dependent pathway. Mol Pharmacol. 71:686–694. 2007. View Article : Google Scholar | |
Holinstat M, Voss B, Bilodeau ML, McLaughlin JN, Cleator J and Hamm HE: PAR4, but not PAR1, signals human platelet aggregation via Ca2+ mobilization and synergistic P2Y12 receptor activation. J Biol Chem. 281:26665–26674. 2006. View Article : Google Scholar : PubMed/NCBI | |
Kahn ML, Nakanishi-Matsui M, Shapiro MJ, Ishihara H and Coughlin SR: Protease-activated receptors 1 and 4 mediate activation of human platelets by thrombin. J Clin Invest. 103:879–887. 1999. View Article : Google Scholar : PubMed/NCBI | |
Andersen H, Greenberg DL, Fujikawa K, Xu W, Chung DW and Davie EW: Protease-activated receptor 1 is the primary mediator of thrombin-stimulated platelet procoagulant activity. Proc Natl Acad Sci USA. 96:11189–11193. 1999. View Article : Google Scholar : PubMed/NCBI | |
Wu CC, Wu SY, Liao CY, Teng CM, Wu YC and Kuo SC: The roles and mechanisms of PAR4 and P2Y12/phosphatidylinositol 3-kinase pathway in maintaining thrombin-induced platelet aggregation. Br J Pharmacol. 161:643–658. 2010. View Article : Google Scholar : PubMed/NCBI | |
Shapiro MJ, Weiss EJ, Faruqi TR and Coughlin SR: Protease-activated receptors 1 and 4 are shut off with distinct kinetics after activation by thrombin. J Biol Chem. 275:25216–25221. 2000. View Article : Google Scholar : PubMed/NCBI | |
Nierodzik ML, Plotkin A, Kajumo F and Karpatkin S: Thrombin stimulates tumor-platelet adhesion in vitro and metastasis in vivo. J Clin Invest. 87:229–236. 1991. View Article : Google Scholar : PubMed/NCBI | |
Nierodzik ML, Kajumo F and Karpatkin S: Effect of thrombin treatment of tumor cells on adhesion of tumor cells to platelets in vitro and tumor metastasis in vivo. Cancer Res. 52:3267–3272. 1992.PubMed/NCBI | |
Darmoul D, Gratio V, Devaud H, Lehy T and Laburthe M: Aberrant expression and activation of the thrombin receptor protease-activated receptor-1 induces cell proliferation and motility in human colon cancer cells. Am J Pathol. 162:1503–1513. 2003. View Article : Google Scholar : PubMed/NCBI | |
Darmoul D, Gratio V, Devaud H, Peiretti F and Laburthe M: Activation of proteinase-activated receptor 1 promotes human colon cancer cell proliferation through epidermal growth factor receptor transactivation. Mol Cancer Res. 2:514–522. 2004. | |
Chiang HS, Yang RS and Huang TF: Thrombin enhances the adhesion and migration of human colon adenocarcinoma cells via increased beta 3-integrin expression on the tumour cell surface and their inhibition by the snake venom peptide, rhodostomin. Br J Cancer. 73:902–908. 1996. View Article : Google Scholar | |
Chen HT, Tsou HK, Tsai CH, Kuo CC, Chiang YK, Chang CH, Fong YC and Tang CH: Thrombin enhanced migration and MMPs expression of human chondrosarcoma cells involves PAR receptor signaling pathway. J Cell Physiol. 223:737–745. 2010.PubMed/NCBI | |
Kaufmann R, Rahn S, Pollrich K, Hertel J, Dittmar Y, Hommann M, Henklein P, Biskup C, Westermann M, Hollenberg MD and Settmacher U: Thrombin-mediated hepatocellular carcinoma cell migration: cooperative action via proteinase-activated receptors 1 and 4. J Cell Physiol. 211:699–707. 2007. View Article : Google Scholar : PubMed/NCBI | |
Miyata S, Koshikawa N, Yasumitsu H and Miyazaki K: Trypsin stimulates integrin alpha(5)beta(1)-dependent adhesion to fibronectin and proliferation of human gastric carcinoma cells through activation of proteinase-activated receptor-2. J Biol Chem. 275:4592–4598. 2000. View Article : Google Scholar | |
Even-Ram S, Uziely B, Cohen P, Grisaru-Granovsky S, Maoz M, Ginzburg Y, Reich R, Vlodavsky I and Bar-Shavit R: Thrombin receptor overexpression in malignant and physiological invasion processes. Nat Med. 4:909–914. 1998. View Article : Google Scholar : PubMed/NCBI | |
Wojtukiewicz MZ, Tang DG, Nelson KK, Walz DA, Diglio CA and Honn KV: Thrombin enhances tumor cell adhesive and metastatic properties via increased alpha IIb beta 3 expression on the cell surface. Thromb Res. 68:233–245. 1992. View Article : Google Scholar : PubMed/NCBI | |
Wojtukiewicz MZ, Tang DG, Ciarelli JJ, Nelson KK, Walz DA, Diglio CA, Mammen EF and Honn KV: Thrombin increases the metastatic potential of tumor cells. Int J Cancer. 54:793–806. 1993. View Article : Google Scholar : PubMed/NCBI | |
Hughes PE and Pfaff M: Integrin affinity modulation. Trends Cell Biol. 8:359–364. 1998. View Article : Google Scholar | |
Hattori R, Hamilton KK, Fugate RD, McEver RP and Sims PJ: Stimulated secretion of endothelial von Willebrand factor is accompanied by rapid redistribution to the cell surface of the intracellular granule membrane protein GMP-140. J Biol Chem. 264:7768–7771. 1989.PubMed/NCBI | |
Stenberg PE, McEver RP, Shuman MA, Jacques YV and Bainton DF: A platelet alpha-granule membrane protein (GMP-140) is expressed on the plasma membrane after activation. J Cell Biol. 101:880–886. 1985. View Article : Google Scholar : PubMed/NCBI | |
Henn V, Slupsky JR, Gräfe M, Anagnostopoulos I, Förster R, Müller-Berghaus G and Kroczek RA: CD40 ligand on activated platelets triggers an inflammatory reaction of endothelial cells. Nature. 391:591–594. 1998. View Article : Google Scholar : PubMed/NCBI | |
Daniel TO, Gibbs VC, Milfay DF, Garovoy MR and Williams LT: Thrombin stimulates c-sis gene expression in microvascular endothelial cells. J Biol Chem. 261:9579–9582. 1986.PubMed/NCBI | |
Papadimitriou E, Manolopoulos VG, Hayman GT, Maragoudakis ME, Unsworth BR, Fenton JW II and Lelkes PI: Thrombin modulates vectorial secretion of extracellular matrix proteins in cultured endothelial cells. Am J Physiol. 272:C1112–C1122. 1997. | |
Wojtukiewicz MZ, Tang DG, Ben-Josef E, Renaud C, Walz DA and Honn KV: Solid tumor cells express functional 'tethered ligand' thrombin receptor. Cancer Res. 55:698–704. 1995. | |
Camerer E: Protease signaling in tumor progression. Thromb Res. 120:S75–S81. 2007. View Article : Google Scholar | |
Bohm SK, Kong W, Bromme D, Smeekens SP, Anderson DC, Connolly A, Kahn M, Nelken NA, Coughlin SR, Payan DG and Bunnett NW: Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2. Biochem J. 314:1009–1016. 1996.PubMed/NCBI | |
D'Andrea MR, Derian CK, Santulli RJ and Andrade-Gordon P: Differential expression of protease-activated receptors-1 and -2 in stromal fibroblasts of normal, benign, and malignant human tissues. Am J Pathol. 158:2031–2041. 2001. View Article : Google Scholar : PubMed/NCBI | |
Darmoul D, Marie JC, Devaud H, Gratio V and Laburthe M: Initiation of human colon cancer cell proliferation by trypsin acting at protease-activated receptor-2. Br J Cancer. 85:772–779. 2001. View Article : Google Scholar : PubMed/NCBI | |
Nierodzik ML, Bain RM, Liu LX, Shivji M, Takeshita K and Karpatkin S: Presence of the seven transmembrane thrombin receptor on human tumour cells: effect of activation on tumour adhesion to platelets and tumor tyrosine phosphorylation. Br J Haematol. 92:452–457. 1996. View Article : Google Scholar | |
Henrikson KP, Salazar SL, Fenton JW II and Pentecost BT: Role of thrombin receptor in breast cancer invasiveness. Br J Cancer. 79:401–406. 1999. View Article : Google Scholar : PubMed/NCBI | |
Nierodzik ML, Chen K, Takeshita K, Li JJ, Huang YQ, Feng XS, D'Andrea MR, Andrade-Gordon P and Karpatkin S: Protease-activated receptor 1 (PAR-1) is required and rate-limiting for thrombin-enhanced experimental pulmonary metastasis. Blood. 92:3694–3700. 1998.PubMed/NCBI | |
Gratio V, Walker F, Lehy T, Laburthe M and Darmoul D: Aberrant expression of proteinase-activated receptor 4 promotes colon cancer cell proliferation through a persistent signaling that involves Src and ErbB-2 kinase. Int J Cancer. 124:1517–1525. 2009. View Article : Google Scholar : PubMed/NCBI | |
Bergmann S, Junker K, Henklein P, Hollenberg MD, Settmacher U and Kaufmann R: PAR-type thrombin receptors in renal carcinoma cells: PAR1-mediated EGFR activation promotes cell migration. Oncol Rep. 15:889–893. 2006.PubMed/NCBI | |
Jin E, Fujiwara M, Pan X, Ghazizadeh M, Arai S, Ohaki Y, Kajiwara K, Takemura T and Kawanami O: Protease-activated receptor (PAR)-1 and PAR-2 participate in the cell growth of alveolar capillary endothelium in primary lung adenocarcinomas. Cancer. 97:703–713. 2003. View Article : Google Scholar : PubMed/NCBI | |
Fischer EG, Ruf W and Mueller BM: Tissue factor-initiated thrombin generation activates the signaling thrombin receptor on malignant melanoma cells. Cancer Res. 55:1629–1632. 1995. | |
Kaufmann R, Henklein P, Henklein P and Settmacher U: Green tea polyphenol epigallocatechin-3-gallate inhibits thrombin-induced hepatocellular carcinoma cell invasion and p42/p44-MAPKinase activation. Oncol Rep. 21:1261–1267. 2009. View Article : Google Scholar | |
Faruqi TR, Weiss EJ, Shapiro MJ, Huang W and Coughlin SR: Structure-function analysis of protease-activated receptor 4 tethered ligand peptides. Determinants of specificity and utility in assays of receptor function. J Biol Chem. 275:19728–19734. 2000. View Article : Google Scholar | |
Rickles FR, Levine M and Edwards RL: Hemostatic alterations in cancer patients. Cancer Metastasis Rev. 11:237–248. 1992. View Article : Google Scholar | |
Walz DA and Fenton JW: The role of thrombin in tumor cell metastasis. Invasion Metastasis. 14:303–308. 1994.PubMed/NCBI | |
Ruf W and Mueller BM: Tissue factor in cancer angiogenesis and metastasis. Curr Opin Hematol. 3:379–84. 1996. View Article : Google Scholar : PubMed/NCBI | |
Palumbo JS and Degen JL: Hemostatic factors in tumor biology. J Pediatr Hematol Oncol. 22:281–287. 2000. View Article : Google Scholar | |
Hejna M, Raderer M and Zielinski CC: Inhibition of metastases by anticoagulants. J Natl Cancer Inst. 91:22–36. 1999. View Article : Google Scholar : PubMed/NCBI | |
Tellez C and Bar-Eli M: Role and regulation of the thrombin receptor (PAR-1) in human melanoma. Oncogene. 22:3130–3137. 2003. View Article : Google Scholar : PubMed/NCBI | |
Shi X, Gangadharan B, Brass LF, Ruf W and Mueller BM: Protease-activated receptors (PAR1 and PAR2) contribute to tumor cell motility and metastasis. Mol Cancer Res. 2:395–402. 2004.PubMed/NCBI | |
Even-Ram SC, Maoz M, Pokroy E, Reich R, Katz BZ, Gutwein P, Altevogt P and Bar-Shavit R: Tumor cell invasion is promoted by activation of protease activated receptor-1 in cooperation with the alpha vbeta 5 integrin. J Biol Chem. 276:10952–10962. 2001. View Article : Google Scholar : PubMed/NCBI | |
Turcotte S, Desrosiers RR, Brand G and Béliveau R: von Hippel-Lindau tumor suppressor protein stimulation by thrombin involves RhoA activation. Int J Cancer. 112:777–786. 2004. View Article : Google Scholar : PubMed/NCBI | |
Chay CH, Cooper CR, Gendernalik JD, Dhanasekaran SM, Chinnaiyan AM, Rubin MA, Schmaier AH and Pienta KJ: A functional thrombin receptor (PAR1) is expressed on bone-derived prostate cancer cell lines. Urology. 60:760–765. 2002. View Article : Google Scholar : PubMed/NCBI | |
Bromberg ME, Bailly MA and Konigsberg WH: Role of protease-activated receptor 1 in tumor metastasis promoted by tissue factor. Thromb Haemost. 86:1210–1214. 2001.PubMed/NCBI | |
Fischer EG, Riewald M, Huang HY, Miyagi Y, Kubota Y, Mueller BM and Ruf W: Tumor cell adhesion and migration supported by interaction of a receptor-protease complex with its inhibitor. J Clin Invest. 104:1213–1221. 1999. View Article : Google Scholar : PubMed/NCBI | |
Karpatkin S: Does hypercoagulability awaken dormant tumor cells in the host? J Thromb Haemost. 2:2103–2106. 2004. View Article : Google Scholar : PubMed/NCBI | |
Yin YJ, Salah Z, Grisaru-Granovsky S, Cohen I, Even-Ram SC, Maoz M, Uziely B, Peretz T and Bar-Shavit R: Human protease-activated receptor 1 expression in malignant epithelia: a role in invasiveness. Arterioscler Thromb Vasc Biol. 23:940–944. 2003. View Article : Google Scholar : PubMed/NCBI | |
O'Brien PJ, Prevost N, Molino M, Hollinger MK, Woolkalis MJ, Woulfe DS and Brass LF: Thrombin responses in human endothelial cells. Contributions from receptors other than PAR1 include the transactivation of PAR2 by thrombin-cleaved PAR1. J Biol Chem. 275:13502–13509. 2000. View Article : Google Scholar : PubMed/NCBI | |
Zacharski LR and Ornstein DL: Heparin and cancer. Thromb Haemost. 80:10–23. 1998. | |
Smorenburg SM, Hettiarachchi RJ, Vink R and Büller HR: The effects of unfractionated heparin on survival in patients with malignancy – a systematic review. Thromb Haemost. 82:1600–1604. 1999. | |
Zacharski LR, Ornstein DL and Mamourian AC: Low-molecular-weight heparin and cancer. Semin Thromb Hemost. 26:69–77. 2000. View Article : Google Scholar | |
Teng LS, Jin KT, He KF, Wang HH, Cao J and Yu DC: Advances in combination of anti-angiogenic agents targeting VEGF-binding and conventional chemotherapy and radiation for cancer treatment. J Chin Med Assoc. 73:281–288. 2010. View Article : Google Scholar : PubMed/NCBI | |
Teng LS, Jin KT, He KF, Zhang J, Wang HH and Cao J: Clinical applications of VEGF-trap (aflibercept) in cancer treatment. J Chin Med Assoc. 73:449–456. 2010. View Article : Google Scholar : PubMed/NCBI | |
Jin K, Shen Y, He K, Xu Z, Li G and Teng L: Aflibercept (VEGF Trap): one more double-edged sword of anti-VEGF therapy for cancer? Clin Transl Oncol. 12:526–532. 2010. View Article : Google Scholar : PubMed/NCBI | |
Edwards RL, Klaus M, Matthews E, McCullen C, Bona RD and Rickles FR: Heparin abolishes the chemotherapy-induced increase in plasma fibrinopeptide A levels. Am J Med. 89:25–28. 1990. View Article : Google Scholar : PubMed/NCBI | |
Zangari M, Anaissie E, Barlogie B, Badros A, Desikan R, Gopal AV, Morris C, Toor A, Siegel E, Fink L and Tricot G: Increased risk of deep-vein thrombosis in patients with multiple myeloma receiving thalidomide and chemotherapy. Blood. 98:1614–1615. 2001. View Article : Google Scholar : PubMed/NCBI | |
Varki NM and Varki A: Heparin inhibition of selectin-mediated interactions during the hematogenous phase of carcinoma metastasis: rationale for clinical studies in humans. Semin Thromb Hemost. 28:53–66. 2002. View Article : Google Scholar | |
Collen A, Smorenburg SM, Peters E, Lupu F, Koolwijk P, van Noorden C and van Hinsbergh VW: Unfractionated and low molecular weight heparin affect fibrin structure and angiogenesis in vitro. Cancer Res. 60:6196–6200. 2000.PubMed/NCBI | |
Mousa SA: Anticoagulants in thrombosis and cancer: the missing link. Semin Thromb Hemost. 28:45–52. 2002. View Article : Google Scholar | |
Norrby K and Ostergaard P: Basic-fibroblast-growth-factor-mediated de novo angiogenesis is more effectively suppressed by low-molecular-weight than by high-molecular-weight heparin. Int J Microcirc Clin Exp. 16:8–15. 1996. View Article : Google Scholar : PubMed/NCBI | |
Hirsh J: Current anticoagulant therapy – unmet clinical needs. Thromb Res. 109:S1–S8. 2003. | |
Weitz JI: A novel approach to thrombin inhibition. Thromb Res. 109:S17–S22. 2003. View Article : Google Scholar : PubMed/NCBI | |
Pakala R, Liang CT and Benedict CR: Inhibition of arterial thrombosis by a peptide ligand of the thrombin receptor. Thromb Res. 100:89–96. 2000. View Article : Google Scholar : PubMed/NCBI | |
Covic L, Misra M, Badar J, Singh C and Kuliopulos A: Pepducin-based intervention of thrombin-receptor signaling and systemic platelet activation. Nat Med. 8:1161–1165. 2002. View Article : Google Scholar : PubMed/NCBI | |
Kasuda S, Sakurai Y, Shima M, Morimura Y, Kudo R, Takeda T, Ishitani A, Yoshioka A and Hatake K: Inhibition of PAR4 signaling mediates ethanol-induced attenuation of platelet function in vitro. Alcohol Clin Exp Res. 30:1608–1614. 2006. View Article : Google Scholar : PubMed/NCBI | |
Derian CK, Maryanoff BE, Zhang HC and Andrade-Gordon P: Therapeutic potential of protease-activated receptor-1 antagonists. Expert Opin Investig Drugs. 12:209–221. 2003. View Article : Google Scholar : PubMed/NCBI | |
Wu CC and Teng CM: Comparison of the effects of PAR1 anta- gonists, PAR4 antagonists, and their combinations on thrombin-induced human platelet activation. Eur J Pharmacol. 546:142–147. 2006. View Article : Google Scholar : PubMed/NCBI | |
Andrade-Gordon P, Maryanoff BE, Derian CK, et al: Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. Proc Natl Acad Sci USA. 96:12257–12262. 1999. View Article : Google Scholar : PubMed/NCBI | |
Maryanoff BE, Zhang HC, Andrade-Gordon P and Derian CK: Discovery of potent peptide-mimetic antagonists for the human thrombin receptor, protease-activated receptor-1 (PAR-1). Curr Med Chem Cardiovasc Hematol Agents. 1:13–36. 2003. View Article : Google Scholar : PubMed/NCBI | |
Zhang HC, Derian CK, Andrade-Gordon P, et al: Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates. J Med Chem. 44:1021–1024. 2001. View Article : Google Scholar | |
Derian CK, Damiano BP, Addo MF, Darrow AL, D'Andrea MR, Nedelman M, Zhang HC, Maryanoff BE and Andrade-Gordon P: Blockade of the thrombin receptor protease-activated receptor-1 with a small-molecule antagonist prevents thrombus formation and vascular occlusion in nonhuman primates. J Pharmacol Exp Ther. 304:855–861. 2003. View Article : Google Scholar | |
Chackalamannil S, Xia Y, Greenlee WJ, Clasby M, Doller D, Tsai H, Asberom T, Czarniecki M, Ahn HS, Boykow G, Foster C, Agans-Fantuzzi J, Bryant M, Lau J and Chintala M: Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents. J Med Chem. 48:5884–5887. 2005. View Article : Google Scholar : PubMed/NCBI | |
Reséndiz JC, Kroll MH and Lassila R: Protease-activated receptor-induced Akt activation – regulation and possible function. J Thromb Haemost. 5:2484–2493. 2007. | |
Mao Y, Jin J, Daniel JL and Kunapuli SP: Regulation of plasmin-induced protease-activated receptor 4 activation in platelets. Platelets. 20:191–198. 2009. View Article : Google Scholar : PubMed/NCBI | |
Seiler SM and Bernatowicz MS: Peptide-derived protease-activated receptor-1 (PAR-1) antagonists. Curr Med Chem Cardiovasc Hematol Agents. 1:1–11. 2003. View Article : Google Scholar : PubMed/NCBI | |
Strande JL, Hsu A, Su J, Fu X, Gross GJ and Baker JE: Inhibiting protease-activated receptor 4 limits myocardial ischemia/reperfusion injury in rat hearts by unmasking adenosine signaling. J Pharmacol Exp Ther. 324:1045–1054. 2008. View Article : Google Scholar | |
Hollenberg MD and Saifeddine M: Proteinase-activated receptor 4 (PAR4): activation and inhibition of rat platelet aggregation by PAR4-derived peptides. Can J Physiol Pharmacol. 79:439–442. 2001. View Article : Google Scholar : PubMed/NCBI | |
Ma L, Hollenberg MD and Wallace JL: Thrombin-induced platelet endostatin release is blocked by a proteinase activated receptor-4 (PAR4) antagonist. Br J Pharmacol. 134:701–704. 2001. View Article : Google Scholar : PubMed/NCBI | |
Kuliopulos A and Covic L: Blocking receptors on the inside: pepducin-based intervention of PAR signaling and thrombosis. Life Sci. 74:255–262. 2003. View Article : Google Scholar : PubMed/NCBI | |
Wu CC, Hwang TL, Liao CH, Kuo SC, Lee FY, Lee CY and Teng CM: Selective inhibition of protease-activated receptor 4-dependent platelet activation by YD-3. Thromb Haemost. 87:1026–1033. 2002.PubMed/NCBI | |
Sangawa T, Nogi T and Takagi J: A murine monoclonal antibody that binds N-terminal extracellular segment of human protease-activated receptor-4. Hybridoma. 27:331–335. 2008. View Article : Google Scholar : PubMed/NCBI | |
O'Brien PJ, Molino M, Kahn M and Brass LF: Protease activated receptors: theme and variations. Oncogene. 20:1570–1581. 2001. View Article : Google Scholar : PubMed/NCBI | |
Nantermet PG, Barrow JC, Lundell GF, et al: Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1). Bioorg Med Chem Lett. 12:319–323. 2002. View Article : Google Scholar : PubMed/NCBI | |
Kato Y, Kita Y, Hirasawa-Taniyama Y, Nishio M, Mihara K, Ito K, Yamanaka T, Seki J, Miyata S and Mutoh S: Inhibition of arterial thrombosis by a protease-activated receptor 1 antagonist, FR171113, in the guinea pig. Eur J Pharmacol. 473:163–169. 2003. View Article : Google Scholar : PubMed/NCBI | |
Hollenberg MD, Saifeddine M, Sandhu S, Houle S and Vergnolle N: Proteinase-activated receptor-4: evaluation of tethered ligand-derived peptides as probes for receptor function and as inflammatory agonists in vivo. Br J Pharmacol. 143:443–454. 2004. View Article : Google Scholar : PubMed/NCBI | |
Covic L, Gresser AL, Talavera J, Swift S and Kuliopulos A: Activation and inhibition of G protein-coupled receptors by cell-penetrating membrane-tethered peptides. Proc Natl Acad Sci USA. 99:643–648. 2002. View Article : Google Scholar : PubMed/NCBI |