Increased potency of a novel complement factor 5a receptor antagonist in a rat model of inflammatory bowel disease

Journal of Pharmacology and Experimental Therapeutics

Volumn 314, Issue 2, 2005, Pages 811-817

  Woodruff, Trent M ^a   Pollitt, Sandra ^a   Proctor, Lavinia M ^a   Stocks, Shelli Z ^a   Manthey, Helga D ^a   Williams, Hua M ^a   Mahadevan, Indumathy B ^a   Shiels, Ian A ^a   Taylor, Stephen M ^a  

^a UNIVERSITY OF QUEENSLAND   (Australia)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLPHENYLALANINE[ORNITHYLPROLYL(DEXTRO CYCLOHEXYLALANINE) TRYPTOPHANYLARGININE]; COMPLEMENT COMPONENT C5A RECEPTOR; COMPLEMENT COMPONENT FACTOR 5A ANTAGONIST; COMPLEMENT INHIBITOR; CYCLOPEPTIDE; DRUG METABOLITE; HYDROCINNAMIC ACID [ORNITHYLPROLYL(CYCLOHEXYL DEXTRO ALANINE) TRYPTOPHANYLARGININE]; TRINITROBENZENESULFONIC ACID; UNCLASSIFIED DRUG;

AMINO ACID SUBSTITUTION; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BODY WEIGHT; COLITIS; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG METABOLISM; DRUG SCREENING; DRUG STABILITY; DRUG TISSUE LEVEL; EDEMA; ENTERITIS; FEMALE; FOOD INTAKE; INTESTINE MUCOSA; MALE; MORTALITY; MULTIPLE DRUG DOSE; NONHUMAN; PRIORITY JOURNAL; RAT;

ANIMALS; BIOLOGICAL AVAILABILITY; BIOTRANSFORMATION; COMPLEMENT C5A; DIGESTIVE SYSTEM; EATING; EDEMA; FEMALE; HUMANS; INFLAMMATORY BOWEL DISEASES; INTESTINAL MUCOSA; PEPTIDES, CYCLIC; RATS; RATS, WISTAR; RECEPTORS, COMPLEMENT; TRINITROBENZENESULFONIC ACID; ULCER; WEIGHT LOSS;

EID: 22944465759     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.105.086835     Document Type: Article

References (28)

1. Abad C, Martinez C, Juarranz MG, Arranz A, Leceta J, Delgado M, and Gomariz RP (2003) Therapeutic effects of vasoactive intestinal peptide in the trinitrobenzene sulfonic acid mice model of Crohn's disease. Gastroenterology 124:961-971.
2. Allegretti M, Moriconi A, Beccari AR, Di Bitondo R, Bizzarri C, Bertini R, and Colotta F (2005) Targeting C5a: recent advances in drug discovery. Curr Med Chem 12:217-236.
3. Arumugam TV, Shiels IA, Strachan AJ, Abbenante G, Fairlie DP, and Taylor SM (2003) A small molecule C5a receptor antagonist protects kidneys from ischemia/ reperfusion injury in rats. Kidney Int 63:134-142.
4. Arumugam TV, Shiels IA, Woodruff TM, Reid RC, Fairlie DP, and Taylor SM (2002) Protective effect of a new C5a receptor antagonist against ischemia-reperfusion injury in the rat small intestine. J Surg Res 103:260-267.
5. Arumugam TV, Woodruff TM, Stocks SZ, Proctor LM, Pollitt S, Shiels IA, Reid RC, Fairlie DP, and TaylorSM(2004) Protective effect of a human C5a receptor antagonist against hepatic ischaemia-reperfusion injury in rats. J Hepatol 40:934-941.
6. Bobin-Dubigeon C, Collin X, Grimaud N, Robert JM, Le Baut G, and Petit JY (2001) Effects of tumour necrosis factor-alpha synthesis inhibitors on rat trinitrobenzene sulphonic acid-induced chronic colitis. Eur J Pharmacol 431:103-110.
7. Halstensen TS and Brandtzaeg P (1991) Local complement activation in inflammatory bowel disease. Immunol Res 10:485-492.
8. Halstensen TS, Mollnes TE, Garred P, Fausa O, and Brandtzaeg P (1990) Epithelial deposition of immunoglobulin G1 and activated complement (C3b and terminal complement complex) in ulcerative colitis. Gastroenterology 98:1264-1271.
9. Halstensen TS, Mollnes TE, Garred P, Fausa O, and Brandtzaeg P (1992) Surface epithelium related activation of complement differs in Crohn's disease and ulcerative colitis. Gut 33:902-908.
10. Harkin DW, Romaschin A, Taylor SM, Rubin BB, and Lindsay TF (2004) Complement C5a receptor antagonist attenuates multiple organ injury in a model of ruptured abdominal aortic aneurysm. J Vasc Surg 39:196-206.
11. Kitano A, Matsumoto T, Nakamura S, Obata A, Oshitani N, Okawa K, and Kobayashi K (1992) New treatment of ulcerative colitis with K-76. Dis Colon Rectum 35:560-567.
12. Kitano A, Matsumoto T, Nakamura S, Oshitani N, Obata A, Okawa K, Inoue Y, Kobayashi K, and Nakura H (1993) Multifunctional effects of anticomplementary agent K-76 on carrageenan-induced colitis in the rabbit. Clin Exp Immunol 94:348-353.
13. Kolios G, Petoumenos C, and Nakos A (1998) Mediators of inflammation: production and implication in inflammatory bowel disease. Hepatogastroenterology 45:1601-1609.
14. Lim WC and Hanauer SB (2004) Emerging biologic therapies in inflammatory bowel disease. Rev Gastroenterol Disord 4:66-85.
15. March DR, Proctor LM, Stoermer MJ, Sbaglia R, Abbenante G, Reid RC, Woodruff TM, Wadi K, Paczkowski N, Tyndall JD, et al. (2004) Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity. Mol Pharmacol 65:868-879.
16. Neurath MF, Fuss I, Kelsall BL, Stuber E, and Strober W (1995) Antibodies to interleukin 12 abrogate established experimental colitis in mice. J Exp Med 182:1281-1290.
17. Nielsen OH and Rask-Madsen J (1996) Mediators of inflammation in chronic inflammatory bowel disease. Scand J Gastroenterol Suppl 216:149-159.
18. Paczkowski NJ, Finch AM, Whitmore JB, Short AJ, Wong AK, Monk PN, Cain SA, Fairlie DP, and Taylor SM (1999) Pharmacological characterization of antagonists of the C5a receptor. Br J Pharmacol 128:1461-1466.
19. Papadakis KA and Targan SR (2000) Role of cytokines in the pathogenesis of inflammatory bowel disease. Annu Rev Med 51:289-298.
20. Rachmilewitz D, Simon PL, Schwartz LW, Griswold DE, Fondacaro JD, and Wasserman MA (1989) Inflammatory mediators of experimental colitis in rats. Gastroenterology 97:326-337.
21. Strachan AJ, Shiels IA, Reid RC, Fairlie DP, and Taylor SM (2001) Inhibition of immune-complex mediated dermal inflammation in rats following either oral or topical administration of a small molecule C5a receptor antagonist. Br J Pharmacol 134:1778-1786.
22. Strachan AJ, Woodruff TM, Haaima G, Fairlie DP, and Taylor SM (2000) A new small molecule C5a receptor antagonist inhibits the reverse-passive Arthus reaction and endotoxic shock in rats. J Immunol 164:6560-6565.
23. Taylor SM and Fairlie DP (2005) Discovery of potent cyclic antagonists of human C5a receptors type 1, in Structural Biology of the Complement System (Lambris J and Morikis D eds), Marcel Dekker, New York, in press.
24. Ueki T, Mizuno M, Uesu T, Kiso T, Nasu J, Inaba T, Kihara Y, Matsuoka Y, Okada H, Fujita T, et al. (1996) Distribution of activated complement, C3b and its degraded fragments, iC3b/C3dg, in the colonic mucosa of ulcerative colitis (UC). Clin Exp Immunol 104:286-292.
25. Woodruff TM, Arumugam TV, Shiels IA, Reid RC, Fairlie DP, and Taylor SM (2003) A potent human C5a receptor antagonist protects against disease pathology in a rat model of inflammatory bowel disease. J Immunol 171:5514-5520.
26. Woodruff TM, Arumugam TV, Shiels IA, Reid RC, Fairlie DP, and Taylor SM (2004) Protective effects of a potent C5a receptor antagonist on experimental acute limb ischemia-reperfusion in rats. J Surg Res 116:81-90.
27. Woodruff TM, Strachan AJ, Dryburgh N, Shiels IA, Reid RC, Fairlie DP, and Taylor SM (2002) Anti-arthritic activity of an orally active C5a receptor antagonist against antigen-induced monoarticular arthritis in the rat. Arth Rheum 46:2476-2485.
28. Woodruff TM, Strachan AJ, Sanderson SD, Monk PN, Wong AK, Fairlie DP, and Taylor SM (2001) Species dependence for binding of small molecule agonist and antagonists to the C5a receptor on polymorphonuclear leukocytes. Inflammation 25:171-177.