The melanocortin MC 1 receptor agonist BMS-470539 inhibits leucocyte trafficking in the inflamed vasculature

British Journal of Pharmacology

Volumn 160, Issue 1, 2010, Pages 171-180

  Leoni, G ^a   Voisin, M B ^a   Carlson, K ^b   Getting, S J ^c   Nourshargh, S ^a   Perretti, M ^a  

^a QUEEN MARY UNIVERSITY OF LONDON   (United Kingdom)

^b BRISTOL MYERS SQUIBB   (United States)

^c UNIVERSITY OF WESTMINSTER   (United Kingdom)

Author keywords

Anti inflammatory GPCR; Endogenous anti inflammation; Endothelium activation; Melanocortins; Microcirculation; Neutrophil trafficking; New chemical entities; Tissue chemokines

Indexed keywords

ANTIINFLAMMATORY AGENT; BMS 470539; MELANOCORTIN 1 RECEPTOR; MELANOCORTIN RECEPTOR AGONIST; THROMBOCYTE ACTIVATING FACTOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIINFLAMMATORY ACTIVITY; ARTICLE; CELL ADHESION; CONTROLLED STUDY; DRUG SPECIFICITY; DRUG TARGETING; EXPERIMENTAL MOUSE; IMMUNOHISTOCHEMISTRY; IN VIVO STUDY; ISCHEMIA; LEUKOCYTE MIGRATION INHIBITION; MALE; MICROCIRCULATION; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; REPERFUSION INJURY; VASCULITIS; VENULE;

ANIMALS; CHEMOKINE CCL2; CHEMOKINE CXCL1; CHEMOTAXIS, LEUKOCYTE; IMIDAZOLES; MALE; MICE; MICE, INBRED C57BL; MICE, KNOCKOUT; MICROCIRCULATION; MICROVESSELS; PLATELET ACTIVATING FACTOR; RECEPTOR, MELANOCORTIN, TYPE 1; SPLANCHNIC CIRCULATION; VASCULITIS;

EID: 77950935939     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/j.1476-5381.2010.00688.x     Document Type: Article

References (39)

1. Ajuebor MN, Das AM, Virag L, Flower RJ, Szabo C, Perretti M (1999). Role of resident peritoneal macrophages and mast cells in chemokine production and neutrophil migration in acute inflammation: evidence for an inhibitory loop involving endogenous IL-10. J Immunol 162 : 1685 1691.
2. Alexander SPH, Mathie A, Peters JA (2009). Guide to Receptors and Channels, 4th edition. Br J Pharmacol 158 (Suppl. 1 S1 S253.
3. Brzoska T, Luger TA, Maaser C, Abels C, Bohm M (2008). Alpha-melanocyte-stimulating hormone and related tripeptides: biochemistry, antiinflammatory and protective effects in vitro and in vivo, and future perspectives for the treatment of immune-mediated inflammatory diseases. Endocr Rev 29 : 581 602.
4. Catania A, Airaghi L, Colombo G, Lipton JM (2000). Alpha-melanocyte- stimulating hormone in normal human physiology and disease states. Trends Endocrinol Metab 11 : 304 308.
5. Catania A, Gatti S, Colombo G, Lipton JM (2004). Targeting melanocortin receptors as a novel strategy to control inflammation. Pharmacol Rev 56 : 1 29.
6. Chatterjee BE, Yona S, Rosignoli G, Young RE, Nourshargh S, Flower RJ et al. (2005). Annexin 1-deficient neutrophils exhibit enhanced transmigration in vivo and increased responsiveness in vitro. J Leukoc Biol 78 : 639 646.
7. Cuzzocrea S, Tailor A, Zingarelli B, Salzman AL, Flower RJ, Szab C et al. (1997). Lipocortin 1 protects against splanchnic artery occlusion and reperfusion injury by affecting neutrophil migration. J Immunol 159 : 5089 5097.
8. Dangerfield J, Larbi KY, Huang MT, Dewar A, Nourshargh S (2002). PECAM-1 (CD31) homophilic interaction up-regulates alpha6beta1 on transmigrated neutrophils in vivo and plays a functional role in the ability of alpha6 integrins to mediate leukocyte migration through the perivascular basement membrane. J Exp Med 196 : 1201 1211.
9. Doi K, Hu X, Yuen PS, Leelahavanichkul A, Yasuda H, Kim SM et al. (2008). AP214, an analogue of alpha-melanocyte-stimulating hormone, ameliorates sepsis-induced acute kidney injury and mortality. Kidney Int 73 : 1266 1274.
10. Gavins FN, Chatterjee BE (2004). Intravital microscopy for the study of mouse microcirculation in anti-inflammatory drug research: focus on the mesentery and cremaster preparations. J Pharmacol Toxicol Methods 49 : 1 14.
11. Gavins FN, Kamal AM, D'Amico M, Oliani SM, Perretti M (2005). Formyl-peptide receptor is not involved in the protection afforded by annexin 1 in murine acute myocardial infarct. FASEB J 19 : 100 102.
12. Getting SJ (2006). Targeting melanocortin receptors as potential novel therapeutics. Pharmacol Ther 111 : 1 15.
13. Getting SJ, Gibbs L, Clark AJ, Flower RJ, Perretti M (1999). POMC gene-derived peptides activate melanocortin type 3 receptor on murine macrophages, suppress cytokine release, and inhibit neutrophil migration in acute experimental inflammation. J Immunol 162 : 7446 7453.
14. Getting SJ, Christian HC, Flower RJ, Perretti M (2002). Activation of melanocortin type 3 receptor as a molecular mechanism for adrenocorticotropic hormone efficacy in gouty arthritis. Arthritis Rheum 46 : 2765 2775.
15. Getting SJ, Christian HC, Lam CW, Gavins FN, Flower RJ, Schioth HB et al. (2003). Redundancy of a functional melanocortin 1 receptor in the anti-inflammatory actions of melanocortin peptides: studies in the recessive yellow (e/e) mouse suggest an important role for melanocortin 3 receptor. J Immunol 170 : 3323 3330.
16. Getting SJ, Lam CW, Leoni G, Gavins FN, Grieco P, Perretti M (2006). [d-Trp8]-gamma-melanocyte-stimulating hormone exhibits anti-inflammatory efficacy in mice bearing a nonfunctional MC1R (recessive yellow e/e mouse). Mol Pharmacol 70 : 1850 1855.
17. Gilroy DW, Lawrence T, Perretti M, Rossi AG (2004). Inflammatory resolution: new opportunities for drug discovery. Nat Rev Drug Discov 3 : 401 416.
18. Gonzalez-Rey E, Delgado M (2007). Anti-inflammatory neuropeptide receptors: new therapeutic targets for immune disorders? Trends Pharmacol Sci 28 : 482 491. (Pubitemid 47368698)
19. Gonzalez-Rey E, Chorny A, Delgado M (2007). Regulation of immune tolerance by anti-inflammatory neuropeptides. Nat Rev Immunol 7 : 52 63.
20. Grieco P, Balse PM, Weinberg D, MacNeil T, Hruby VJ (2000). d-Amino acid scan of gamma-melanocyte-stimulating hormone: importance of Trp(8) on human MC3 receptor selectivity. J Med Chem 43 : 4998 5002.
21. Herpin TF, Yu G, Carlson KE, Morton GC, Wu X, Kang L et al. (2003). Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties. J Med Chem 46 : 1123 1126.
22. Kang L, McIntyre KW, Gillooly KM, Yang Y, Haycock J, Roberts S et al. (2006). A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice. J Leukoc Biol 80 : 897 904.
23. Kubes P, Suzuki M, Granger DN (1990). Modulation of PAF-induced leukocyte adherence and increased microvascular permeability. Am J Physiol 259 : G859 G864.
24. Lam CW, Getting SJ, Perretti M (2005). In vitro and in vivo induction of heme oxygenase 1 in mouse macrophages following melanocortin receptor activation. J Immunol 174 : 2297 2304.
25. Lam CW, Perretti M, Getting SJ (2006). Melanocortin receptor signalling in RAW264.7 macrophage cell line. Peptides 27 : 404 412.
26. Leoni G, Patel HB, Sampaio AL, Gavins FN, Murray JF, Grieco P et al. (2008). Inflamed phenotype of the mesenteric microcirculation of melanocortin type 3 receptor-null mice after ischemia-reperfusion. FASEB J 22 : 4228 4238.
27. Ley K, Laudanna C, Cybulsky MI, Nourshargh S (2007). Getting to the site of inflammation: the leukocyte adhesion cascade updated. Nat Rev Immunol 7 : 678 689.
28. Lipton JM, Zhao H, Ichiyama T, Barsh GS, Catania A (1999). Mechanisms of antiinflammatory action of alpha-MSH peptides. In vivo and in vitro evidence. Ann N Y Acad Sci 885 : 173 182.
29. Luger TA, Scholzen T, Grabbe S (1997). The role of alpha-melanocyte- stimulating hormone in cutaneous biology. J Investig Dermatol Symp Proc 2 : 87 93.
30. Maaser C, Kannengiesser K, Specht C, Lugering A, Brzoska T, Luger TA et al. (2006). Crucial role of the melanocortin receptor MC1R in experimental colitis. Gut 55 : 1415 1422.
31. Robbins LS, Nadeau JH, Johnson KR, Kelly MA, Roselli-Rehfuss L, Baack E et al. (1993). Pigmentation phenotypes of variant extension locus alleles result from point mutations that alter MSH receptor function. Cell 72 : 827 834.
32. Scholzen TE, Sunderkotter C, Kalden DH, Brzoska T, Fastrich M, Fisbeck T et al. (2003). Alpha-melanocyte stimulating hormone prevents lipopolysaccharide-induced vasculitis by down regulating endothelial cells adhesion molecule expression. Endocrinology 144 : 360 370.
33. Serhan CN, Savill J (2005). Resolution of inflammation: the beginning programs the end. Nat Immunol 6 : 1191 1197.
34. Serhan CN, Brain SD, Buckley CD, Gilroy DW, Haslett C, O'Neill LA et al. (2007). Resolution of inflammation: state of the art, definitions and terms. FASEB J 21 : 325 332.
35. Tailor A, Tomlinson A, Salas A, Panés J, Granger DN, Flower RJ et al. (1999). Dexamethasone inhibition of leucocyte adhesion to rat mesenteric postcapillary venules: role of intercellular adhesion molecule 1 and KC. Gut 45 : 705 712.
36. Trevaskis JL, Gawronska-Kozak B, Sutton GM, McNeil M, Stephens JM, Smith SR et al. (2007). Role of adiponectin and inflammation in insulin resistance of Mc3r and Mc4r knockout mice. Obesity (Silver Spring) 15 : 2664 2672.
37. Voisin M-B, Pröbstl D, Nourshargh S (2010). Venular basement membranes ubiquitously express matrix protein low expression regions: characterisation in multiple tissues and remodelling during inflammation. Am J Pathol 176 : 482 495.
38. Young RE, Thompson RD, Larbi KY, La M, Roberts CE, Shapiro SD et al. (2004). Neutrophil elastase (NE)-deficient mice demonstrate a nonredundant role for NE in neutrophil migration, generation of proinflammatory mediators, and phagocytosis in response to zymosan particles in vivo. J Immunol 172 : 4493 4502.
39. Zimmerman BJ, Holt JW, Paulson JC, Anderson DC, Miyasaka M, Tamatani T et al. (1994). Molecular determinants of lipid mediator-induced leukocyte adherence and emigration in rat mesenteric venules. Am J Physiol 266 : H847 H853.