322
Views
10
CrossRef citations to date
0
Altmetric
Review

Recent developments in C5/C5a inhibitors

, &
Pages 445-458 | Published online: 24 Mar 2006

Bibliography

  • ABBAS AK, POBER JS: The complement system. In: Cellular and Molecular Immunology. WB Sauders Company, Philadelphia (1997):315-338.
  • BITTER-SUERMANN D: The anaphylatoxins. In: The Complement System. Springer-Verlag, Berlin (1988):367-384.
  • ZUIDERWEG ER, NETTESHEIM DG, MOLLISON KW, CARTER GW: Tertiary structure of human complement component C5a in solution from nuclear magnetic resonance data. Biochemistry (1989) 28(1):172-185.
  • ZHANG X, BOYAR W, TOTH MJ, WENNOGLE L, GONNELLA NC: Structural definition of the C5a C terminus by two-dimensional nuclear magnetic resonance spectroscopy. Proteins Structure Function Genetics (1997) 28:261-267.
  • EMBER JA, JAGELS MA, HUGLI TE: Characterization of complement anaphylatoxins and their biological responses. In: The Human Complement System in Health and Disease. Jevamm F (Ed.) Marcel Dekker, New York (1998):241-284.
  • HARTMANN K, HENZ BM, KRUGER-KRASAGAKES S et al.: C3a and C5a stimulate chemotaxis of human mast cells. Blood (1997) 89(8):2863-2870.
  • SOZZANI S, SALLUSTO F, LUINI W et al.: Migration of dendritic cells in response to formyl peptides, C5a, and a distinct set of chemokines. J. Immunol. (1995) 155(7):3292-3295.
  • MORELLI A, LARREGINA A, CHULUYAN I, KOLKOWSKI E, FAINBOIM L: Expression and modulation of C5a receptor (CD88) on skin dendritic cells. Chemotactic effect of C5a on skin migratory dendritic cells. Immunology (1996) 89(1):126-134.
  • JAGELS MA, CHAMBERS JD, ARFORS KE, HUGLI TE: C5a- and tumor necrosis factor-α-induced leukocytosis occurs independently of β2 integrins and L-selectin: differential effects on neutrophil adhesion molecule expression in vivo. Blood (1995) 85(10):2900-2909.
  • FOREMAN KE, VAPORCIYAN AA, BONISH BK et al.: C5a-induced expression of P-selectin in endothelial cells. J. Clin. Invest. (1994) 94(3):1147-1155.
  • FOREMAN KE, GLOVSKY MM, WARNER RL, HORVATH SJ, WARD PA: Comparative effect of C3a and C5a on adhesion molecule expression on neutrophils and endothelial cells. Inflammation (1996) 20(1):1-9.
  • DISCIPIO RG, DAFFERN PJ, JAGELS MA, BROIDE DH, SRIRAMARAO P: A comparison of C3a and C5a-mediated stable adhesion of rolling eosinophils in postcapillary venules and transendothelial migration in vitro and in vivo. J. Immunol. (1999) 162(2):1127-1136.
  • JAGELS MA, DAFFERN PJ, HUGLI TE: C3a and C5a enhance granulocyte adhesion to endothelial and epithelial cell monolayers: epithelial and endothelial priming is required for C3a-induced eosinophil adhesion. Immunopharmacology (2000) 46(3):209-222.
  • MCCARTHY K, HENSON PM: Induction of lysosomal enzyme secretion by alveolar macrophages in response to the purified complement fragments C5a and C5a des-arg. J. Immunol. (1979) 123(6):2511-2517.
  • OKUSAWA S, DINARELLO CA, YANCEY KB et al.: C5a induction of human interleukin 1. Synergistic effect with endotoxin or interferon-γ. J. Immunol. (1987) 139(8):2635-2640.
  • OKUSAWA S, YANCEY KB, VAN DER MEER JW et al.: C5a stimulates secretion of tumor necrosis factor from human mononuclear cells in vitro. Comparison with secretion of interleukin 1β and interleukin 1α. J. Exp. Med. (1988) 168(1):443-448.
  • EMBER JA, SANDERSON SD, HUGLI TE, MORGAN EL: Induction of interleukin-8 synthesis from monocytes by human C5a anaphylatoxin. Am. J. Pathol. (1994) 144(2):393-403.
  • MORGAN EL, SANDERSON S, SCHOLZ W et al.: Identification and characterization of the effector region within human C5a responsible for stimulation of IL-6 synthesis. J. Immunol. (1992) 148(12):3937-3942.
  • SMEDEGARD G, CUI LX, HUGLI TE: Endotoxin-induced shock in the rat. A role for C5a. Am. J. Pathol. (1989) 135(3):489-497.
  • SHORT A, WONG AK, FINCH AM et al.: Effects of a new C5a receptor antagonist on C5a- and endotoxin-induced neutropenia in the rat. Br. J. Pharmacol. (1999) 126(3):551-554.
  • STRACHAN AJ, WOODRUFF TM, HAAIMA G, FAIRLIE DP, TAYLOR SM: A new small molecule C5a receptor antagonist inhibits the reverse-passive Arthus reaction and endotoxic shock in rats. J. Immunol. (2000) 164(12):6560-6565.
  • WETSEL RA: Structure, function and cellular expression of complement anaphylatoxin receptors. Curr. Opin. Immunol. (1995) 7(1):48-53.
  • BARNUM SR: Complement in central nervous system inflammation. Immunol. Res. (2002) 26(1-3):7-13.
  • ZWIRNER J, GOTZE O, BEGEMANN G et al.: Evaluation of C3a receptor expression on human leucocytes by the use of novel monoclonal antibodies. Immunology (1999) 97(1):166-172.
  • GERARD NP, BAO L, XIAO-PING H et al.: Human chemotaxis receptor genes cluster at 19q13.3-13.4. Characterization of the human C5a receptor gene. Biochemistry (1993) 32(5):1243-1250.
  • SICILIANO SJ, ROLLINS TE, DEMARTINO J et al.: Two-site binding of C5a by its receptor: an alternative binding paradigm for G-protein-coupled receptors. Proc. Natl. Acad. Sci. USA (1994) 91(4):1214-1218.
  • MOLLISON KW, FEY TA, KRAUSE RA et al.: C5a structural requirements for neutrophil receptor interaction. Agents Actions Suppl. (1991) 35(17):17-21.
  • MERY L, BOULAY F: Evidence that the extracellular N-terminal domain of C5aR contains amino-acid residues crucial for C5a binding. Eur. J. Haematol. (1993) 51(5):282-287.
  • BUBECK P, GROTZINGER J, WINKLER M et al.: Site-specific mutagenesis of residues in the human C5a anaphylatoxin which are involved in possible interaction with the C5a receptor. Eur. J. Biochem. (1994) 219(3):897-904.
  • VLATTAS I, SYTWU II, DELLUREFICIO J et al.: Identification of a receptor-binding region in the core segment of the human anaphylatoxin C5a. J. Med. Chem. (1994) 37(17):2783-2790.
  • CHEN Z, ZHANG X, GONNELLA NC et al.: Residues 21-30 within the extracellular N-terminal region of the C5a receptor represent a binding domain for the C5a anaphylatoxin. J. Biol. Chem. (1998) 273(17):10411-10419.
  • CHENOWETH DE, HUGLI TE: Human C5a and C5a analogs as probes of the neutrophil C5a receptor. Mol. Immunol. (1980) 17(2):151-161.
  • DEMARTINO JA, VAN RIPER G, SICILIANO SJ et al.: The amino terminus of the human C5a receptor is required for high affinity C5a binding and for receptor activation by C5a but not C5a analogs. J. Biol. Chem. (1994) 269(20):14446-14450.
  • GROTZINGER J, ENGELS M, JACOBY E, WOLLMER A, STRASSBURGER W: A model for the C5a receptor and for its interaction with the ligand. Protein Eng. (1991) 4(7):767-771.
  • MONK PN, PEASE JE, MARLAND G, BARKER MD: Mutation of aspartate 82 of the human C5a receptor abolishes the secretory response to human C5a in transfected rat basophilic leukemia cells. Eur. J. Immunol. (1994) 24(11):2922-2925.
  • MONK PN, BARKER MD, PARTRIDGE LJ, PEASE JE: Mutation of glutamate 199 of the human C5a receptor defines a binding site for ligand distinct from the receptor N terminus. J. Biol. Chem. (1995) 270(28):16625-16629.
  • DEMARTINO JA, KONTEATIS ZD, SICILIANO SJ et al.: Arginine 206 of the C5a receptor is critical for ligand recognition and receptor activation by C-terminal hexapeptide analogs. J. Biol. Chem. (1995) 270(27):15966-15969.
  • CRASS T, AMES RS, SARAU HM et al.: Chimeric receptors of the human C3a receptor and C5a receptor (CD88). J. Biol. Chem. (1999) 274(13):8367-8370.
  • CAIN SA, COUGHLAN T, MONK PN: Mapping the ligand-binding site on the C5a receptor: arginine74 of C5a contacts aspartate282 of the C5a receptor. Biochemistry (2001) 40(46):14047-14052.
  • RAFFETSEDER U, ROPER D, MERY L et al.: Site-directed mutagenesis of conserved charged residues in the helical region of the human C5a receptor. Arg2O6 determines high-affinity binding sites of C5a receptor. Eur. J. Biochem. (1996) 235(1-2):82-90.
  • GERBER BO, MENG EC, DOTSCH V, BARANSKI TJ, BOURNE HR: An activation switch in the ligand binding pocket of the C5a receptor. J. Biol. Chem. (2001) 276(5):3394-3400.
  • HUBER-LANG MS, SARMA JV, MCGUIRE SR et al.: Structure–function relationships of human C5a and C5aR. J. Immunol. (2003) 170(12):6115-6124.
  • CAIN SA, MONK PN: The orphan receptor C5L2 has high affinity binding sites for complement fragments C5a and C5a des-Arg(74). J. Biol. Chem. (2002) 277(9):7165-7169.
  • KALANT D, CAIN SA, MASLOWSKA M et al.: The chemoattractant receptor-like protein C5L2 binds the C3a des-Arg77/acylation-stimulating protein. J. Biol. Chem. (2003) 278(13):11123-11129.
  • OKINAGA S, SLATTERY D, HUMBLES A et al.: C5L2, a nonsignaling C5A binding protein. Biochemistry (2003) 42(31):9406-9415.
  • OHNO M, HIRATA T, ENOMOTO M et al.: A putative chemoattractant receptor, C5L2, is expressed in granulocyte and immature dendritic cells, but not in mature dendritic cells. Mol. Immunol. (2000) 37(8):407-412.
  • LEE DK, GEORGE SR, CHENG R et al.: Identification of four novel human G protein-coupled receptors expressed in the brain. Brain Res. Mol. Brain Res. (2001) 86(1-2):13-22.
  • OTTO M, HAWLISCH H, MONK PN et al.: C5a mutants are potent antagonists of the C5a receptor (CD88) and of C5L2: position 69 is the locus that determines agonism or antagonism. J. Biol. Chem. (2004) 279(1):142-151.
  • RATAJCZAK MZ, RECA R, WYSOCZYNSKI M et al.: Transplantation studies in C3-deficient animals reveal a novel role of the third complement component (C3) in engraftment of bone marrow cells. Leukemia (2004) 18(9):1482-1490.
  • KALANT D, MACLAREN R, CUI W et al.: C5L2 Is a functional receptor for acylation-stimulating protein. J. Biol. Chem. (2005) 280(25):23936-23944.
  • GAO H, NEFF TA, GUO RF et al.: Evidence for a functional role of the second C5a receptor C5L2. Faseb J. (2005) 19(8):1003-1005.
  • WOODRUFF TM, STRACHAN AJ, DRYBURGH N et al.: Antiarthritic activity of an orally active C5a receptor antagonist against antigen-induced monarticular arthritis in the rat. Arthritis Rheum. (2002) 46(9):2476-2485.
  • WOODRUFF TM, ARUMUGAM TV, SHIELS IA et al.: A potent human C5a receptor antagonist protects against disease pathology in a rat model of inflammatory bowel disease. J. Immunol. (2003) 171(10):5514-5520.
  • ARUMUGAM TV, SHIELS IA, WOODRUFF TM et al.: Protective effect of a new C5a receptor antagonist against ischemia-reperfusion injury in the rat small intestine. J. Surg. Res. (2002) 103(2):260-267.
  • ARUMUGAM TV, SHIELS IA, STRACHAN AJ et al.: A small molecule C5a receptor antagonist protects kidneys from ischemia/reperfusion injury in rats. Kidney Int. (2003) 63(1):134-142.
  • ARUMUGAM TV: WOODRUFF TM, STOCKS SZ et al.: Protective effect of a human C5a receptor antagonist against hepatic ischaemia-reperfusion injury in rats. J. Hepatol. (2004) 40(6):934-941.
  • WOODRUFF TM, ARUMUGAM TV, SHIELS IA et al.: Protective effects of a potent C5a receptor antagonist on experimental acute limb ischemia–reperfusion in rats. J. Surg. Res. (2004) 116(1):81-90.
  • HUBER-LANG MS, RIEDEMAN NC, SARMA JV et al.: Protection of innate immunity by C5aR antagonist in septic mice. FASEB J. (2002) 16(12):1567-1574.
  • SEWELL DL, NACEWICZ B, LIU F et al.: Complement C3 and C5 play critical roles in traumatic brain cryoinjury: blocking effects on neutrophil extravasation by C5a receptor antagonist. J. Neuroimmunol. (2004) 155(1-2):55-63.
  • GIRARDI G, BERMAN J, REDECHA P et al.: Complement C5a receptors and neutrophils mediate fetal injury in the antiphospholipid syndrome. J. Clin. Invest. (2003) 112(11):1644-1654.
  • KOHL J: Anaphylatoxins and infectious and non-infectious inflammatory diseases. Mol. Immunol. (2001) 38(2-3):175-187.
  • BHOLE D, STAHL GL: Therapeutic potential of targeting the complement cascade in critical care medicine. Crit. Care Med. (2003) 31(1 Suppl.):S97-104.
  • HOLLAND MC, MORIKIS D, LAMBRIS JD: Synthetic small-molecule complement inhibitors. Curr. Opin. Investig. Drugs (2004) 5(11):1164-1173.
  • GUO RF, WARD PA: Role of C5a in inflammatory responses. Ann. Rev. Immunol. (2005) 23:821-852.
  • TAYLOR SM, FAIRLIE DP: Regulators of the anaphylatoxin C5a. Expert Opin. Ther. Patents (2000) 10(4):449-458.
  • MIZUNO M, NISHIKAWA K, MORGAN BP, MATSUO S: Comparison of the suppressive effects of soluble CR1 and C5a receptor antagonist in acute arthritis induced in rats by blocking of CD59. Clin. Exp. Immunol. (2000) 119(2):368-375.
  • FINCH AM, WONG AK, PACZKOWSKI NJ et al.: Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. J. Med. Chem. (1999) 42(11):1965-1974.
  • KAWAI M, QUINCY DA, LANE B et al.: Identification and synthesis of a receptor binding site of human anaphylatoxin C5a. J. Med. Chem. (1991) 34(7):2068-2071.
  • SANDERSON SD, KIRNARSKY L, SHERMAN SA et al.: Decapeptide agonists of human C5a: the relationship between conformation and spasmogenic and platelet aggregatory activities. J. Med. Chem. (1994) 37(19):3171-3180.
  • SANDERSON SD, KIRNARSKY L, SHERMAN SA et al.: Decapeptide agonists of human C5a: the relationship between conformation and neutrophil response. J. Med. Chem. (1995) 38(18):3669-3675.
  • FINCH AM, VOGEN SM, SHERMAN SA et al.: Biologically active conformer of the effector region of human C5a and modulatory effects of N-terminal receptor binding determinants on activity. J. Med. Chem. (1997) 40(6):877-884.
  • FORTIN JP, BOUTHILLIER J, ST-PIERRE SA, MARCEAU F: Contractile effect of anaphylatoxin C5a and of a mimetic peptide on the human umbilical artery: further evidence for leukocyte-dependent vasomotion. J. Cardiovasc. Pharmacol. (2002) 40(6):815-821.
  • BACHVAROV DR, HOULE S, BACHVAROVA M et al.: Cloning and preliminary pharmacological characterization of the anaphylatoxin C5a receptor in the rabbit. Br. J. Pharmacol. (1999) 128(2):321-326.
  • SHORT AJ, PACZKOWSKI NJ, VOGEN SM, SANDERSON SD, TAYLOR SM: Response-selective C5a agonists: differential effects on neutropenia and hypotension in the rat. Br. J. Pharmacol. (1999) 128(3):511-514.
  • PROCTOR LM, WOODRUFF TM, PAZCKOWSKI NP, MONK PN, TAYLOR SM: Dual C3a/C5a receptor agonism by a C5a C-terminal analogue decapeptide XXth International Complement Workshop. Honolulu, Hawaii, USA (2004).
  • KONTEATIS ZD, SICILIANO SJ, VAN RG et al.: Development of C5a receptor antagonists. Differential loss of functional responses. J. Immunol. (1994) 153(9):4200-4205.
  • MIZUNO M, NISHIKAWA K, OKADA N et al.: Inhibition of a membrane complement regulatory protein by a monoclonal antibody induces acute lethal shock in rats primed with lipopolysaccharide. J. Immunol. (1999) 162(9):5477-5482.
  • KONDO C, MIZUNO M, NISHIKAWA K et al.: The role of C5a in the development of thrombotic glomerulonephritis in rats. Clin. Exp. Immunol. (2001) 124(2):323-329.
  • WONG AK, FINCH AM, PIERENS GK et al.: Small molecular probes for G-protein-coupled C5a receptors: conformationally constrained antagonists derived from the C terminus of the human plasma protein C5a. J. Med. Chem. (1998) 41(18):3417-3425.
  • MARCH DR, PROCTOR LM, STOERMER MJ et al.: Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity. Mol. Pharmacol. (2004) 65(4):868-879.
  • PACZKOWSKI NJ, FINCH AM, WHITMORE JB et al.: Pharmacological characterization of antagonists of the C5a receptor. Br. J. Pharmacol. (1999) 128(7):1461-1466.
  • HAYNES DR, HARKIN DG, BIGNOLD LP et al.: Inhibition of C5a-induced neutrophil chemotaxis and macrophage cytokine production in vitro by a new C5a receptor antagonist. Biochem. Pharmacol. (2000) 60(5):729-33.
  • HARKIN DW, ROMASCHIN A, TAYLOR SM, RUBIN BB, LINDSAY TF: Complement C5a receptor antagonist attenuates multiple organ injury in a model of ruptured abdominal aortic aneurysm. J. Vasc. Surg. (2004) 39(1):196-206.
  • WOODRUFF TM, POLLITT S, PROCTOR LM et al.: Increased potency of a novel C5a receptor antagonist in a rat model of inflammatory bowel disease. J. Pharmacol. Exp. Ther. (2005) 314(2):811-817.
  • BUCK E, BOURNE H, WELLS JA: Site-specific disulfide capture of agonist and antagonist peptides on the C5a receptor. J. Biol. Chem. (2005) 280(6):4009-4012.
  • BUCK E, WELLS JA: Disulfide trapping to localize small-molecule agonists and antagonists for a G protein-coupled receptor. Proc. Natl. Acad. Sci. USA (2005) 102(8):2719-2724.
  • SUMICHIKA H, SAKATA K, SATO N et al.: Identification of a potent and orally active non-peptide C5a receptor antagonist. J. Biol. Chem. (2002) 277(51):49403-49407.
  • SAKATA K, SUMICHIKA H, GOTO K et al.: A potent and orally active C5a receptor antagonist, W-54011, ameliorates established collagen-induced arthritis in cynomolgus monkeys. 12th International Congress of Immunology and 4th Annual Conference of FOCIS. Montreal, Canada (2004).
  • ANZENBACHER P, ANZENBACHEROVA E: Cytochromes P450 and metabolism of xenobiotics. Cell Mol. Life Sci. (2001) 58(5-6):737-747.
  • BERTINI R, ALLEGRETTI M, BIZZARRI C et al.: Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: prevention of reperfusion injury. Proc. Natl. Acad. Sci. USA (2004) 101(32):11791-11796.
  • ALLEGRETTI M, MORICONI A, BECCARI AR et al.: Targeting C5a: recent advances in drug discovery. Curr. Med. Chem. (2005) 12(2):217-236.
  • DE HAAS CJ, VELDKAMP KE, PESCHEL A et al.: Chemotaxis inhibitory protein of Staphylococcus aureus, a bacterial antiinflammatory agent. J. Exp. Med. (2004) 199(5):687-695.
  • POSTMA B, POPPELIER MJ, VAN GALEN JC et al.: Chemotaxis inhibitory protein of Staphylococcus aureus binds specifically to the C5a and formylated peptide receptor. J. Immunol. (2004) 172(11):6994-7001.
  • POSTMA B, KLEIBEUKER W, POPPELIER MJ et al.: Residues 10-18 within the C5a receptor N terminus compose a binding domain for chemotaxis inhibitory protein of Staphylococcus aureus. J. Biol. Chem. (2005) 280(3):2020-2027.
  • HAAS PJ, DE HAAS CJ, POPPELIER MJ et al.: The structure of the C5a receptor-blocking domain of chemotaxis inhibitory protein of Staphylococcus aureus is related to a group of immune evasive molecules. J. Mol. Biol. (2005) 353(4):859-872.
  • Annual Report. Alligator Bioscience AB, Scheelevägen 19 A, SE-223 70 Lund, Sweden (2004).
  • HELLER T, HENNECKE M, BAUMANN U et al.: Selection of a C5a receptor antagonist from phage libraries attenuating the inflammatory response in immune complex disease and ischemia/reperfusion injury. J. Immunol. (1999) 163(2):985-994.
  • LAUDES IJ, CHU JC, SIKRANTH S et al.: Anti-c5a ameliorates coagulation/fibrinolytic protein changes in a rat model of sepsis. Am. J. Pathol. (2002) 160(5):1867-1875.
  • CZERMAK BJ, SARMA V, PIERSON CL et al.: Protective effects of C5a blockade in sepsis. Nat. Med. (1999) 5(7):788-792.
  • HUBER-LANG M, SARMA VJ, LU KT et al.: Role of C5a in multiorgan failure during sepsis. J. Immunol. (2001) 166(2):1193-1199.
  • CZERMAK BJ, BRECKWOLDT M, RAVAGE ZB et al.: Mechanisms of enhanced lung injury during sepsis. Am. J. Pathol. (1999) 154(4):1057-1065.
  • FUNG M, LU M, FURE H et al.: Pre-neutralization of C5a-mediated affects by the monoclonal antibody 137-26 reacting with the C5a moiety of native C5 without preventing C5 cleavage. Clin. Exp. Immunol. (2003) 133(2):160-169.
  • WANG Y, HU Q, MADRI JA et al.: Amelioration of lupus-like autoimmune disease in NZB/WF1 mice after treatment with a blocking monoclonal antibody specific for complement component C5. Proc. Natl. Acad. Sci. USA (1996) 93(16):8563-8568.
  • WANG Y, ROLLINS SA, MADRI JA, MATIS LA: Anti-C5 monoclonal antibody therapy prevents collagen-induced arthritis and ameliorates established disease. Proc. Natl. Acad. Sci. USA (1995) 92(19):8955-8959.
  • TUERK C, GOLD L: Systematic evolution of ligands by exponential enrichment: RNA ligands to bacteriophage T4 DNA polymerase. Science (1990) 249(4968):505-510.
  • KURZ JC, ROTTMAN JB, MCCAULEY TM, BENEDICT C, EPSTEIN D: In vitro and in vivo studies of a synthetic anti-C5 aptamer. 3rd Workshop on Complement Associated Diseases, Animal Models, and Therapeutics. Rodos, Greece (2005).

Patents

Websites

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.