Derivatized 2-furoyl-LIGRLO-amide, a versatile and selective probe for proteinase-activated receptor 2: Binding and visualization

Journal of Pharmacology and Experimental Therapeutics

Volumn 326, Issue 2, 2008, Pages 453-462

  Hollenberg, Morley D ^a   Renaux, Bernard ^a   Hyun, Eric ^a   Houle, Steeve ^a   Vergnolle, Nathalie ^a,b,c   Saifeddine, Mahmoud ^a   Ramachandran, Rithwik ^a  

^a UNIVERSITY OF CALGARY   (Canada)

^b INSERM   (France)

^c UNIVERSITÉ DE TOULOUSE   (France)

Author keywords

[No Author keywords available]

Indexed keywords

2 FUROYLLEUCYLISOLEUCYLGLYCYLARGINYLLEUCYLORNITHINAMIDE; ALEXA FLUOR 594; CINNAMOYLLEUCYLISOLEUCYLGYCYLARGINYLLEUCYLORNITHINAMIDE; FLUORESCENT DYE; LEUCYLARGINYLGLYCYLISOLEUCYLLEUCYLSERINAMIDE; PEPTIDE; PROPIONIC ACID DERIVATIVE; PROTEINASE ACTIVATED RECEPTOR 2; SERYLLEUCYLISOLEUCYLGLYCYLLYSYLTHREONINAMIDE; SERYLLEUCYLISOLEUCYLGLYCYLLYSYLVALINAMIDE; TRITIUM;

ANIMAL CELL; ANIMAL TISSUE; AORTA; ARTICLE; CALCIUM SIGNALING; CONTROLLED STUDY; DRUG POTENCY; DRUG RECEPTOR BINDING; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; VASODILATATION;

ANIMALS; BINDING, COMPETITIVE; CELL LINE; FLUORESCENT DYES; LIGANDS; MICROSCOPY, FLUORESCENCE; MOLECULAR PROBES; OLIGOPEPTIDES; ORGANIC CHEMICALS; PROTEIN BINDING; RADIOLIGAND ASSAY; RATS; RECEPTOR, PAR-2; REPRODUCIBILITY OF RESULTS; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSFECTION;

EID: 47949118138     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.108.136432     Document Type: Article

References (35)

1. Al-Ani B, Saifeddine M, Kawabata A, Renaux B, Mokashi S, and Hollenberg MD (1999) Proteinase-activated receptor 2 (PAR(2)): development of a ligand-binding assay correlating with activation of PAR(2) by PAR(1)- and PAR(2)-derived peptide ligands. J Pharmacol Exp Ther 290:753-760.
2. Al-Ani B, Hansen KK, and Hollenberg MD (2004) Proteinase-activated receptor-2: key role of amino-terminal dipeptide residues of the tethered ligand for receptor activation. Mol Pharmacol 65:149-156.
3. Al-Ani B, Saifeddine M, and Hollenberg MD (1995) Detection of functional receptors for the proteinase-activated-receptor-2-activating polypeptide, SLIGRL-NH2, in rat vascular and gastric smooth muscle. Can J Physiol Pharmacol 73:1203-1207.
4. Ariens EJ, Van Rossum JM, and Simonis AM (1957) Affinity, intrinsic activity and drug interactions. Pharmacol Rev 9:218-236.
5. Bernatowicz MS, Klimas CE, Hartl KS, Peluso M, Allegretto NJ, and Seiler SM (1996) Development of potent thrombin receptor antagonist peptides. J Med Chem 39:4879-4887.
6. Blackhart BD, Ruslim-Litrus L, Lu CC, Alves VL, Teng W, Scarborough RM, Reynolds EE, and Oksenberg D (2000) Extracellular mutations of protease-activated receptor-1 result in differential activation by thrombin and thrombin receptor agonist peptide. Mol Pharmacol 58:1178-1187.
7. 125I-containing acylating agent. Biochem J 133:529-539.
8. Cenac N, Coelho A, Nguyen C, Compton SJ, Andrade-Gordon P, MacNaughton WK, Wallace JL, Holleberg MD, Bunnett NW, Garcia-Villar R, et al. (2002) Induction of intestinal inflammation in mouse by activation of proteinase-activated receptor-2. Br J Pharmacol 161:1903-1915.
9. Cenac N, Andrews C, Holzhausen M, Chapman K, Andrade-Gordon P, Steinhoff M, Barbara G, Beck P, Bunnett NW, Sharkey KA, et al. (2007) Role for protease activity in visceral pain in irritable bowel syndrome. J Clin Invest 117:636-647.
10. Compton SJ, Cairns JA, Palmer KJ, Al-Ani B, Hollenberg MD, and Walls AF (2000) A polymorphic protease-activated receptor 2 (PAR2) displaying reduced sensitivity to trypsin and differential responses to PAR agonists. J Biol Chem 275:39207-39212.
11. Coughlin SR (2005) Protease-activated receptors in hemostasis, thrombosis and vascular biology. J Thromb Haemost 3:1800-1814.
12. Cuatrecasas P and Hollenberg MD (1976) Membrane receptors and hormone action. Adv Protein Chem 30:251-451.
13. DeLean A, Munson PJ, and Rodbard D (1978) Simultaneous analysis of families of sigmoidal curves: application to bioassay, radioligand assay, and physiological dose-response curves. Am J Physiol 235:E97-E102.
14. Ferrell WR, Lockhart JC, Kelso EB, Dunning L, Plevin R, Meek SE, Smith AJ, Hunter GD, McLean JS, McGarry F, et al. (2003) Essential role for proteinase-activated receptor-2 in arthritis. J Clin Invest 111:35-41.
15. Hansen KK, Oikonomopoulou K, Li Y, and Hollenberg MD (Oct 19, 2007) Proteinases, proteinase-activated receptors (PARs) and the pathophysiology of cancer and diseases of the cardiovascular, musculoskeletal, nervous and gastrointestinal systems. Naunyn Schmiedebergs Arch Pharmacol [Epub ahead of print]
16. Hansen KK, Sherman PM, Cellars L, Andrade-Gordon P, Pan Z, Baruch A, Wallace JL, Hollenberg MD, and Vergnolle N (2005) A major role for proteolytic activity and proteinase-activated receptor-2 in the pathogenesis of infectious colitis. Proc Natl Acad Sci U S A 102:8363-8368.
17. Hollenberg MD and Compton SJ (2002) International Union of Pharmacology. XXVIII. Proteinase-activated receptors. Pharmacol Rev 54:203-217.
18. Hollenberg MD and Cuatrecasas P (1976) Techniques for the study of plasma membrane receptors related to hormone action, In Methods in Cancer Research (Busch H, ed) Vol. 12, chapter VI, pp 317-366, Academic Press, New York.
19. Hollenberg MD, Saifeddine M, Al Ani B, and Kawabata A (1997) Proteinase-activated receptors: structural requirements for activity, receptor cross-reactivity, and receptor selectivity of receptor-activating peptides. Can J Physiol Pharmacol 75:832-841.
20. 3H]2-furoyl-LIGRL-NH2, to human PAR2. Br J Pharmacol 145:255-263.
21. Kawabata A, Saifeddine M, Al-Ani B, Leblond L, and Hollenberg MD (1999) Evaluation of proteinase-activated receptor-1 (PAR1) agonists and antagonists using a cultured cell receptor desensitization assay: activation of PAR2 by PAR1-targeted ligands. J Pharmacol Exp Ther 288:358-570.
22. Kawabata A, Kanke T, Yonezawa D, Ishiki T, Saka M, Kabeya M, Sekiguchi F, Kubo S, Kuroda R, Iwaki 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.
23. Kong W, McConalogue K, Khitin LM, Hollenberg MD, Payan DG, Bohm SK, and Bunnett NW (1997) Luminal trypsin may regulate enterocytes through proteinase-activated receptor 2. Proc Natl Acad Sci U S A 94:8884-8889.
24. Macfarlane SR, Seatter MJ, Kanke T, Hunter GD, and Plevin R (2001) Proteinase-activated receptors. Pharmacol Rev 53:245-282.
25. Maryanoff BE, Santulli RJ, McComsey DF, Hoekstra WJ, Hoey K, Smith CE, Addo M, Darrow AL, and Andrade-Gordon P (2001) Protease-activated receptor-2 (PAR-2): structure-function study of receptor activation by diverse peptides related to tethered-ligand epitopes. Arch Biochem Biophys 386:195-204.
26. McGuire JJ, Saifeddine M, Triggle CR, Sun K, and Hollenberg MD (2004) 2-Furoyl-LIGRLO-amide: a potent and selective proteinase-activated receptor 2 agonist. J Pharmacol Exp Ther 309:1124-1131.
27. Nguyen C, Coelho AM, Grady E, Compton SJ, Wallace JL, Hollenberg MD, Cenac N, Garcia-Villar R, Bueno L, Steinhoff M, et al. (2003) Colitis induced by proteinase-activated receptor-2 agonists is mediated by a neurogenic mechanism. Can J Physiol Pharmacol 81:920-927.
28. Ossovskaya VS and Bunnett NW (2004) Protease-activated receptors: contribution to physiology and disease. Physiol Rev 84:579-621.
29. Paton WD and Rang HP (1965) The uptake of atropine and related drugs by intestinal smooth muscle of the guinea-pig in relation to acetylcholine receptors. Proc R Soc Lond B Biol Sci 163:1-44.
30. Ramachandran R and Hollenberg MD (2008) Proteinases and signaling: pathophysiological and therapeutic implications via PARs and more. Br J Pharmacol 153:S263-S282.
31. Steinhoff M, Buddenkotte J, Shpacovitch V, Rattenholl A, Moormann C, Vergnolle N, Luger TA, and Hollenberg MD (2005) Proteinase-activated receptors: transducers of proteinase-mediated signaling in inflammation and immune response. Endocr Rev 26:1-43.
32. Stephenson RP (1956) A modification of receptor theory. Br J Pharmacol Chemother 11:379-393.
33. Vergnolle N (2004) Modulation of visceral pain and inflammation by proteaseactivated receptors. Br J Pharmacol 141:1264-1274.
34. Vergnolle N (2005) Clinical relevance of proteinase activated receptors (pars) in the gut. Gut 54:867-874.
35. Vergote D, Butler GS, Ooms M, Cox JH, Silva C, Hollenberg MD, Jhamandas JH, Overall CM, and Power C (2006) Proteolytic processing of SDF-1alpha reveals a change in receptor specificity mediating HIV-associated neurodegeneration. Proc Natl Acad Sci U S A 103:19182-19187.