Dual effect of the novel peptide antagonist K-14585 on proteinase-activated receptor-2-mediated signaling

British Journal of Pharmacology

Volumn 158, Issue 7, 2009, Pages 1695-1704

  Goh, Fui Goon ^a   Ng, Pei Yuen ^a   Nilsson, Mary ^a   Kanke, Toru ^b   Plevin, Robin ^a  

^a UNIVERSITY OF STRATHCLYDE   (United Kingdom)

^b Kowa Company Limited   (Japan)

Author keywords

G q 11 signalling; Inositol phosphate; K 14585 peptide antagonist; P38 MAP kinase; PAR 2

Indexed keywords

4 (4 FLUOROPHENYL) 2 (4 METHYLSULFINYLPHENYL) 5 (4 PYRIDYL)IMIDAZOLE; IMMUNOGLOBULIN ENHANCER BINDING PROTEIN; INHIBITORY GUANINE NUCLEOTIDE BINDING PROTEIN; INOSITOL PHOSPHATE; INTERLEUKIN 8; K 14585; MITOGEN ACTIVATED PROTEIN KINASE; MITOGEN ACTIVATED PROTEIN KINASE P38; N [1 (2,6 DICHLOROPHENYL)METHYL] 3 (1 PYRROLIDINYLMETHYL) 1H INDOL 5 YL]AMINOCARBONYL]GLYCINYLLYSINYLPHENYLALANYL N BENZHYDRYLAMIDE; PROTEIN; PROTEIN INHIBITOR; PROTEINASE ACTIVATED RECEPTOR 2; PROTEINASE ACTIVATED RECEPTOR 4; SERYLLEUCYLISOLEUCYLGLYCYLLYSYLVALINE HYDROXIDE; TRANSCRIPTION FACTOR RELA; TRITIUM; UNCLASSIFIED DRUG; YM 254890;

ARTICLE; CONTROLLED STUDY; CYTOKINE PRODUCTION; DNA BINDING; ENZYME ACTIVATION; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; HUMAN; HUMAN CELL; PRIORITY JOURNAL; PROTEIN EXPRESSION; REPORTER GENE; SIGNAL TRANSDUCTION;

CELL LINE; DOSE-RESPONSE RELATIONSHIP, DRUG; EPITHELIAL CELLS; GTP-BINDING PROTEIN ALPHA SUBUNITS, GQ-G11; HUMANS; IMIDAZOLES; OLIGOPEPTIDES; P38 MITOGEN-ACTIVATED PROTEIN KINASES; PEPTIDES, CYCLIC; PHOSPHORYLATION; PYRIDINES; RECEPTOR, PAR-2; SIGNAL TRANSDUCTION;

EID: 71249135633     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2009.00415.x     Document Type: Article

References (41)

1. Alexander SP, Mathie A, Peters JA (2008). Guide to receptors and channels (GRAC), 3rd edition. Br J Pharmacol 153 (Suppl. 2 S1 S209.
2. Andrade-Gordon P, Maryanoff BE, Derian CK, Zhang HC, Addo MF, Darrow AL et al 1999). Design, synthesis, and biological characterization of a peptide-mimetic antagonist for a tethered-ligand receptor. Proc Natl Acad Sci USA 96 : 12257 12262.
3. Azzi M, Charest PG, Angers S, Rousseau G, Kohout T, Bouvier M et al 2003). Beta-arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors. Proc Natl Acad Sci USA 100 : 11406 11411.
4. Baker JG, Hill SJ (2007). Multiple GPCR conformations and signalling pathways: Implications for antagonist affinity estimates. Trends Pharmacol Sci 28 : 374 381.
5. Cenac N, Coelho AM, Nguyen C, Compton S, Andrade-Gordon P, MacNaughton WK et al 2002). Induction of intestinal inflammation in mouse by activation of proteinase-activated receptor-2. Am J Pathol 161 : 1903 1915.
6. Cenac N, Garcia-Villar R, Ferrier L, Larauche M, Vergnolle N, Bunnett NW et al 2003). Proteinase-activated receptor-2-induced colonic inflammation in mice: Possible involvement of afferent neurons, nitric oxide, and paracellular permeability. J Immunol 170 : 4296 4300.
7. Chackalamannil S (2006). Thrombin receptor (protease activated receptor-1) antagonists as potent antithrombotic agents with strong antiplatelet effects. J Med Chem 49 : 5389 5403.
8. Charest PG, Oligny-Longpre G, Bonin H, Azzi M, Bouvier M (2007). The V2 vasopressin receptor stimulates ERK1/2 activity independently of heterotrimeric G protein signalling. Cell Signal 19 : 32 41.
9. Damiano BP, Derian CK, Maryanoff BE, Zhang HC, Gordon PA (2003). RWJ-58259: A selective antagonist of protease activated receptor-1. Cardiovasc Drug Rev 21 : 313 326.
10. Darieva Z, Lasunskaia EB, Campos MN, Kipnis TL, Da Silva WD (2004). Activation of phosphatidylinositol 3-kinase and c-Jun-N-terminal kinase cascades enhances NF-kappaB-dependent gene transcription in BCG-stimulated macrophages through promotion of p65/p300 binding. J Leukoc Biol 75 : 689 697.
11. Darmoul D, Gratio V, Devaud H, Laburthe M (2004). Protease-activated receptor 2 in colon cancer: Trypsin-induced MAPK phosphorylation and cell proliferation are mediated by epidermal growth factor receptor transactivation. J Biol Chem 279 : 20927 20934. (Pubitemid 38656491)
12. Ferrell WR, Lockhart JC, Kelso EB, Dunning L, Plevin R, Meek SE et al 2003). Essential role for proteinase-activated receptor-2 in arthritis. J Clin Invest 111 : 35 41.
13. Goon Goh F, Sloss CM, Cunningham MR, Nilsson M, Cadalbert L, Plevin R (2008). G-protein-dependent and -independent pathways regulate proteinase-activated receptor-2 mediated p65 NFkappaB serine 536 phosphorylation in human keratinocytes. Cell Signal 20 : 1267 1274.
14. Granneman JG (2001). The putative beta4-adrenergic receptor is a novel state of the beta1-adrenergic receptor. Am J Physiol Endocrinol Metab 280 : E199 E202.
15. Kanke T, Macfarlane SR, Seatter MJ, Davenport E, Paul A, McKenzie RC et al 2001). Proteinase-activated receptor-2-mediated activation of stress-activated protein kinases and inhibitory kappa B kinases in NCTC 2544 keratinocytes. J Biol Chem 276 : 31657 31666.
16. Kanke T, Takizawa T, Kabeya M, Kawabata A (2005). Physiology and pathophysiology of proteinase-activated receptors (PARs): PAR-2 as a potential therapeutic target. J Pharmacol Sci 97 : 38 42.
17. Kanke T, Kabeya M, Kubo S, Kondo S, Yasuoka K, Tagashira J et al 2009). Novel antagonists for proteinase-activated receptor 2: Inhibition of cellular and vascular responses in vitro and in vivo. Br J Pharmacol 158 : 361 371.
18. Kawabata A, Kanke T, Yonezawa D, Ishiki T, Saka M, Kabeya M et al 2004). Potent and metabolically stable agonists for protease-activated receptor-2: Evaluation of activity in multiple assay systems in vitro and in vivo. J Pharmacol Exp Ther 309 : 1098 1107.
19. Kawagoe J, Takizawa T, Matsumoto J, Tamiya M, Meek SE, Smith AJ et al 2002). Effect of protease-activated receptor-2 deficiency on allergic dermatitis in the mouse ear. Jpn J Pharmacol 88 : 77 84.
20. Kelso EB, Lockhart JC, Hembrough T, Dunning L, Plevin R, Hollenberg MD et al 2006). Therapeutic promise of proteinase-activated receptor-2 antagonism in joint inflammation. J Pharmacol Exp Ther 316 : 1017 1024.
21. Kim SJ, Hwang SG, Shin DY, Kang SS, Chun JS (2002). p38 kinase regulates nitric oxide-induced apoptosis of articular chondrocytes by accumulating p53 via NFkappa B-dependent transcription and stabilization by serine 15 phosphorylation. J Biol Chem 277 : 33501 33508.
22. Korus M, Mahon GM, Cheng L, Whitehead IP (2002). p38 MAPK-mediated activation of NF-kappaB by the RhoGEF domain of Bcr. Oncogene 21 : 4601 4612.
23. Kumar P, Lau CS, Mathur M, Wang P, DeFea KA (2007). Differential effects of beta-arrestins on the internalization, desensitization and ERK1/2 activation downstream of protease activated receptor-2. Am J Physiol Cell Physiol 293 : C346 C357.
24. Macfarlane SR, Seatter MJ, Kanke T, Hunter GD, Plevin R (2001). Proteinase-activated receptors. Pharmacol Rev 53 : 245 282.
25. Macfarlane SR, Sloss CM, Cameron P, Kanke T, McKenzie RC, Plevin R (2005). The role of intracellular Ca2+ in the regulation of proteinase-activated receptor-2 mediated nuclear factor kappa B signalling in keratinocytes. Br J Pharmacol 145 : 535 544.
26. McIntosh KA, Plevin R, Ferrell WR, Lockhart JC (2007). The therapeutic potential of proteinase-activated receptors in arthritis. Curr Opin Pharmacol 7 : 334 338.
27. Maryanoff BE, Zhang HC, Andrade-Gordon P, Derian CK (2003). 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.
28. Molenaar P (2003). The 'state' of beta-adrenoceptors. Br J Pharmacol 140 : 1 2.
29. Nystedt S, Emilsson K, Wahlestedt C, Sundelin J (1994). Molecular cloning of a potential proteinase activated receptor. Proc Natl Acad Sci USA 91 : 9208 9212.
30. Ossovskaya VS, Bunnett NW (2004). Protease-activated receptors: contribution to physiology and disease. Physiol Rev 84 : 579 621.
31. Paul A, Torrie LJ, McLaren GJ, Kennedy C, Gould GW, Plevin R (2000). P2Y receptor-mediated inhibition of tumor necrosis factor alpha -stimulated stress-activated protein kinase activity in EAhy926 endothelial cells. J Biol Chem 275 : 13243 13249.
32. Plevin R, Kellock NA, Wakelam MJ, Wadsworth R (1994). Regulation by hypoxia of endothelin-1-stimulated phospholipase D activity in sheep pulmonary artery cultured smooth muscle cells. Br J Pharmacol 112 : 311 315.
33. Ramachandran R, Sadofsky LR, Xiao Y, Botham A, Cowen M, Morice AH et al 2007). Inflammatory mediators modulate thrombin and cathepsin-G signaling in human bronchial fibroblasts by inducing expression of proteinase-activated receptor-4. Am J Physiol Lung Cell Mol Physiol 292 : L788 L798.
34. Ritchie E, Saka M, Mackenzie C, Drummond R, Wheeler-Jones C, Kanke T et al 2007). Cytokine upregulation of proteinase-activated-receptors 2 and 4 expression mediated by p38 MAP kinase and inhibitory kappa B kinase beta in human endothelial cells. Br J Pharmacol 150 : 1044 1054.
35. Schreiber E, Matthias P, Muller MM, Schaffner W (1989). Rapid detection of octamer binding proteins with 'mini-extracts' prepared from a small number of cells. Nucleic Acids Res 17 : 6419.
36. Seeliger S, Derian CK, Vergnolle N, Bunnett NW, Nawroth R, Schmelz M et al 2003). Proinflammatory role of proteinase-activated receptor-2 in humans and mice during cutaneous inflammation in vivo. FASEB J 17 : 1871 1885.
37. Steinhoff M, Vergnolle N, Young SH, Tognetto M, Amadesi S, Ennes HS et al 2000). Agonists of proteinase-activated receptor 2 induce inflammation by a neurogenic mechanism. Nat Med 6 : 151 158.
38. q/11-selective inhibitor. J Biol Chem 279 : 47438 47445.
39. Wang P, DeFea KA (2006). Protease-activated receptor-2 simultaneously directs beta-arrestin-1-dependent inhibition and Galphaq-dependent activation of phosphatidylinositol 3-kinase. Biochemistry 45 : 9374 9385.
40. Wei H, Ahn S, Shenoy SK, Karnik SS, Hunyady L, Luttrell LM et al 2003). Independent beta-arrestin 2 and G protein-mediated pathways for angiotensin II activation of extracellular signal-regulated kinases 1 and 2. Proc Natl Acad Sci USA 100 : 10782 10787.
41. Yoshida N, Katada K, Handa O, Takagi T, Kokura S, Naito Y et al 2007). Interleukin-8 production via protease-activated receptor 2 in human esophageal epithelial cells. Int J Mol Med 19 : 335 340.