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Research Article

A review on the Strategies for the Development and Application of New Anti-arthritic Agents

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Pages 607-663 | Published online: 27 Sep 2008

References

  • Harris ED, Jr. Rheumatoid arthritis. Pathophysiology and implication for therapy. N Eng J Med 1990; 322: 1277–1289
  • Gay S, Gay RE, Koopman WJ. Molecular and cellular mechanisms of joint destruction in rheumatoid arthritis: two cellular mechanisms explain joint destruction. Ann Rheum Dis 1993; 52: S39–S47
  • Brooks PM. Clinical management of rheumatoid arthritis. Lancet 1993; 341: 286–290
  • Felson DT, Anderson JT, Meehan RF. The comparative efficacy and toxicity of second-line drugs in rheumatoid arthritis. Arth Rheum 1990; 33: 1449–1461
  • Panayi GS, Lanchburg JS, Kingsley GH. The importance of the T cell in initiating and maintaining the chronic synovitis of rheumatoid arthritis. Arth Rheum 1992; 35: 729–735
  • Malmberg AB, Yaksh TL. Hyperalgesia mediated by spinal glutamate or substance P receptor blocked by spinal cyclooxygenase inhibition. Science 1992; 257: 1276–1279
  • Goodwin JS. Are prostaglandins proinflammatory, antiinflammatory, both or neither?. J Rheumatol 1991; 18(Supl 28)26–29
  • Belch J JF. Eicosanoids and rheumatology: inflammatory and vascular aspects. Prostaglandins, Leukotrienes and Essential Fatty Acids 1989; 36: 219–234
  • Williams KI, Higgs GA. Eicosanoids and inflammation. J Pathology 1988; 156: 101–110
  • Henderson B, Pettipher ER, Higgs GA. Mediators of rheumatoid arthritis. Br Med Bull 1987; 43: 415–428
  • Higgs GA, Moncada S, Vane JR. Eicosanoids in inflammation. Ann Clin Res 1984; 16: 287–299
  • Robinson DW. Eicosanoids in human inflammation. Trends in RA-Research, P Hedqvist, JR Kalden, R Muller-Peddinghaus, DR Robinson. EULAR, Basel 1991; 195–198
  • Rothwell NJ. Eicosanoids, thermogenesis and thermoregulation. Prostaglandins, Leukotrienes and Essential Fatty Acids 1992; 46: 1–7
  • Vane JR. Inhibition of prostaglandin synthesis as a mechanism of action of aspirin-like drugs. Nature (New Biol) 1971; 231: 232–235
  • Brooks PM, Day RO. Nonsteroidal antiinflammatory drugs-differences and similarities. New Engl J Med 1991; 324: 1716–1725
  • Abramson SB, Weissmann G. The mechanisms of action of nonsteroidal antiinflammatory drugs. Arth Rheum 1989; 32: 1–9
  • Bray MA. Prostaglandins and leukotrienes: fine tuning the immune response. ISI Atlas of Science: Pharmacology 1987; 1: 101–106
  • Alvarellos A, Lipsky PE, Jasin HE. Prostaglandin E2 modulation of rheumatoid factor synthesis. Arth Rheum 1988; 31: 1473–1480
  • Chouaib S, Bertoglio JH. Prostaglandin E as modulators of the immune response. Lymphokine Res 1988; 7: 237–245
  • Phipps RP, Stein SH, Roper RL. A new view of prostaglandin E regulation of the immune response. Immunology Today 1991; 12: 349–352
  • Form D, Auerbach R. PGE2 and angiogenesis. Proc Soc Exp Biol Med 1983; 172: 214–218
  • Colville-Nash PR, Scott DL. Angiogenesis and rheumatoid arthritis: pathogenic and therapeutic implications. Ann Rheum Dis 1992; 51: 919–925
  • Prostaglandins in bone resorption, W Harvey, A Bennett. CRC Press, Boca Raton 1988
  • Dingle JT, Sheild MJ. The interactions of cytokines, NSAIDs and prostaglandins in cartilage destruction and repair. Adv Prostaglandin, Thrombox Leukotriene Res 1990; 21: 955–966
  • Schenkier S, Golbus J. Treatment of rheumatoid arthritis. Postgrad Med 1992; 91: 285–292
  • Borda IT. The spectrum of adverse gastrointestinal effects associated with nonsteroidal anti-inflammatory drugs. NSAIDs-A Profile of Adverse Effects, IT Borda, RS Koff. Hanley & Belfus, Philadelphia 1992; 25–81
  • Allison MC. Gastrointestinal damage associated with the use of nonsteroidal antiinflammatory drugs. New Engl J Med 1992; 327: 749–754
  • Wilson TW, Carruthers SG. Renal and cardiovascular adverse effects of nonsteroidal anti-inflammatory drugs. NSAIDs-A Profile of Adverse Effects, IT Borda, RS Koff. Hanley & Belfus, Philadelphia 1992; 81–112
  • Savage RL, Moller PW, Ballantyne CL, Wells JE. Variation in the risk of peptic ulcer complications with nonsteroidal antiinflammatory drug therapy. Arth Rheum 1993; 36: 84–90
  • Balfour JA, Buckley M M-T. Etodolac. A reappraisal of its pharmacology and therapeutic use in rheumatic and pain states. Drugs 1991; 42: 274–299
  • Friedel HA, Langtry HD, Buckley MM. Nabumetone. A reappraisal of its pharmacology and therapeutic use in rheumatic diseases. Drugs 1993; 45: 131–156
  • Miller LG. Oxaprozin: A once daily nonsteroidal anti-inflammatory drug. Clin Pharm 1992; 11: 591–603
  • Taha AS, et al. Effect on gastric and duodenal mucosal prostaglandins of repeated intake of therapeutic doese of naproxen and etodolac in rheumatoid arthritis. Ann Rheum Dis 1990; 49: 354–358
  • Leese P. Comparison of the effects of etodolac SR and naproxen on gastro-intestinal blood loss. Cur Med Res Opin 1992; 13: 13–20
  • Dvornik D, Lee D KH. Possible mechanisms for the gastric safety of etodolac. J Musculoskel Med 1991; S47–S53, April Supplement
  • Xie W, Robertson DL, Simmons DL. Mitogen-inducible prostaglandin G/H synthase: a new target for nonsteroidal antiinflammatory drugs. Drug Develop Res 1992; 25: 249–265
  • Hla T, Neilson K. Human cyclooxygenase-2 cDNA. Proc Natl Acad Sci USA 1992; 89: 7384–7388
  • O'Sullivan MG, Huggins EM, Meade EA, DeWitt DL, McCall CE. Lipopolysaccharide induces prostaglandin H synthase-2 in alveolar macrophages. Biochem Biophys Res Commun 1992; 187: 1123–1127
  • Lyons-Giordano B, Pratta MA, Galbraith W, Davis GL, Arner EC. Interleukin-1 differentially modulates chondrocyte expression of cyclooxygenase-2 and phospholipase A2-. Exp Cell Biol 1993; 206: 58–62
  • Masferrer JL, Seibert K, Zweifel B, Needleman P. Endogenous glucocorticoids regulate an inducible cyclooxygenase enzyme. Proc Natl Acad Sci USA 1992; 89: 3917–3921
  • Sano H, Hla T, Maier JA, Crofford LJ, Case JP, Maclag T, Wilder RL. In vivo cyclooxygenase expression in synovial tissues of patients with rheumatoid arthritis and osteoarthritis and rats with adjuvant and streptococcal wall arthritis. J Clin Invest 1992; 89: 97–108
  • Meade EA, Smith WL, DeWitt DL. Differential inhibition of prostaglandin endoperoxide synthase (cyclooxygenase) isozymes by aspirin and other non-steroidal antiinflammatory drugs. J Biol Chem 1993; 268: 6610–6614
  • Chen L-S K. Transcriptional modulation: A new approach to drug discovery. Med Chem Res 1992; 2: 397–409
  • Wang L-H, Hajibeigi A, Xu X-M, Loose-Mitchell D, Wu KK. Characterization of the promoter of human prostaglandin H synthase-1 gene. Biochem Biophys Res Commun 1993; 190: 406–411
  • Vane JS. Evidence for the proinflammatory effects of prostaglandins. 8th International Conference on Prostaglandins and Related Compounds, Montreal, Quebec, July, 26–311992, abstract 161
  • Twomey BM, Dale MM. Cyclooxygenase-independent effects of non-steroidal antiinflammatory drugs on the respiratory burst. Biochem Pharmacol 1992; 43: 413–418
  • Gardiner PJ. Classification of prostanoid receptors. Adv Prostaglandin, Thromboxane and Leukotriene Res 1990; 20: 110–118
  • O'Brien WM. Radiologic evaluation of erosions: a quantitative method for assessing long-term remittive therapy in rheumatoid arthritis. Br J Clin Pharmacol 1986; 22: 173S–182S
  • Musser JH, Kreft AF. 5-Lipoxygenase: Properties, pharmacology, and the quinoline(bridged) class of inhibitors. J Med Chem 1992; 35: 2501–2524
  • Batt DG. 5-Lipoxygenase inhibitors and their anti-inflammatory activities. Prog Med Chem 1992; 29: 1–63
  • Meghji S, Sandy JR, Scutt AM, Harvey W, Harris M. Stimulation of bone resorption by lipoxygenase metabolites of arachidonic acid. Prostaglandins 1988; 36: 139–149
  • Kanayasu T, et al. Leukotriene C4 stimulates angiogenesis in bovine carotid artery endothelial cells in vitro. Biochem Biophys Res Commun 1989; 159: 572–578
  • Hwang D. Essential fatty acids and the immune response. FASEB J 1989; 3: 2052–2061
  • Schrieber L. Effect of leukotriene B4 and PGE2 on the adhesion of lymphocytes to endothelial cells. Clin Exp Immunol 1990; 81: 160–165, To SST
  • Caccese RG, Cummons TA, Chang JY, Adams LM. Effect of the 5-lipoxygenase (5-LO) inhibitor WY-50,295 tromethamine and indomethacin on lipopolysaccharide (LPS)-challenged collagen-induced arthritis (CIA) in mice. FASEB J 1991; 5: A511
  • Kreisle RA, Parker CW, Griffin GL, Senior RM, Stenson WF. Studies of leukotriene B4-specific binding and function in rat polymorphonuclear leukocytes: Absence of a chemotactic response. J Immunol 1985; 134: 3356–3363
  • Weinblatt M, Kremer J, Coblyn J, Helfgott S, Maier A, Petrillo G, Henson B, Rubin P, Sperling R. Zileuton, a 5-lipoxygenase inhibitor in rheumatoid arthritis. J Rheumatol 1992; 19: 1537–1541
  • Ojingwa JC, Braeckman RA, Hui J, Hansen RG, Rubin PD. Pharmacokinetics and pharmacodynamics of the second generation 5-lipoxygenase inhibitor A-78773 after single oral dosing in healthy volunteers. Pharmaceut Res 1992; 9: S304
  • McMillan RM, Spruce KE, Crawley GC, Walker E RH, Foster SJ. Pre-clinical pharmacology of ICI D2138, a potent orally-active non-redox inhibitor of 5-lipoxygenase. Br J Pharmacol 1992; 107: 1042–1047
  • Sperling RI, Benincaso AI, Anderson RJ, Coblyn JS, Austen KF, Weinblatt ME. Acute and chronic suppression of leukotriene B4 synthesis ex vivo in neutrophils from patients with rheumatoid arthritis beginning treatment with methotrexate. Arth Rheum 1992; 35: 376–384
  • Leroux JL, Damon M, Chavis C, De Paulet AC, Blotman F. Effects of a single dose of methotrexate on 5- and 12-lipoxygenase products in patients with rheumatoid arthritis. J Rheumatol 1992; 19: 863–866
  • Yuan W, Munoz B, Wong C-H, Haeggstrom JZ, Wetterholm A, Samuelsson B. Development of selective tight-binding inhibitors of leukotriene A4 hydrolase. J Med Chem 1993; 36: 211–220
  • Djuric SW, Fretland DJ, Penning TD. Leukotriene B4 receptor antagonists-a most discriminating class of antiinflammatory agent?. Drugs Fut 1992; 17: 819–830
  • Garst M. Phospholipase A2 inhibitors. Curr Opin Thera Patents 1992; 2: 400–408
  • Mayer RJ, Marshall LA. New insights on mammalian phospholipase A2(s); comparison of arachidonoyl-selective and non-selective enzymes. FASEB J 1993; 7: 339–348
  • Glaser KB, Mobilio D, Chang JY, Senko N. Phospholipase A2 enzymes: regulation and inhibition. Trends Pharmacol 1993; 14: 92–98
  • Pruzanski W, Vadas P. Phospholipase A2 -a mediator between proximal and distal effectors of inflammation. Immunol Today 1991; 12: 143–146
  • Asoka Y, Yoshida K, Sasaki Y, Nishizuka Y, Murakami M, Kudo I, Inoue K. Possible role of mammalian secretory group II phospholipase A2 in T-lymphocyte activation: Implications in propagation of inflammatory reaction. Proc Natl Acad Sci USA 1993; 90: 716–719
  • Sessions RB, Dauber-Osguthorpe P, Campbell MM, Osguthorpe DJ. Modeling of substrate and inhibitor binding to phospholipase A2. Proteins 1992; 14: 45–64
  • Bennion C, Connolly S, Gensmantel NP, Hallam C, Jackson CG, Primrose WU, Roberts G CK, Robinson DH, Slaich PK. Design and synthesis of some substrate analogue inhibitors of phospholipase A2 and investigation by NMR and molecular modeling into binding interactions in the enzyme-inhibitor complex. J Med Chem 1992; 35: 2939–2951
  • Jones ST, Ahlstrom P, Berendsen H JC, Pickersgill RW. Molecular dynamics simulation of a phospholipase A2-substrate complex. Biochem Biophys Acta 1993; 1162: 135–142
  • Wery J-P, Schevitz RW, Clawson DK, Bobbitt JL, Dow ER, Gamboa G, Goodson T, Herman RB, Kramer RM, McClure DB, Mihelich ED, Putnam JE, Sharp JD, Stark DH, Teater C, Warrick MW, Jones ND. Structure of recombinant human rheumatoid arthritic synovial fluid phospholipase A2 at 2.2A resolution. Nature 1991; 352: 79–82
  • Scott DL, White SP, Browning JL, Rosa JJ, Gelb MH, Sigler PB. Structures of free and inhibited human secretory phospholipase A2 from inflammatory exudate. Science 1991; 254: 1007–1010
  • Peters AR, Dekker N, van den Berg L, Boelens R, Kaptein R, Slotboom AJ, de Haas GH. Conformational changes in phospholipase A2 upon binding to micellar interfaces in the absence and presence of competitive inhibitors. A H1 and 15N NMR study. Biochemistry 1992; 31: 10024–10030
  • Bayburt T, Yu B-Z, Lin H-K, Browning J, Jain MK, Gelb MH. Human nonpancreatic secreted phospholipase A2: Interfacial parameters, substrate specificities, and competitive inhibitors. Biochemistry 1993; 32: 573–582
  • Jain MK, Ghomashchi F, Yu B-Z, Bayburt T, Murphy D, Houch D, Brownell J, Reid JC, Solowiej JE, Wong S-M, Mocek U, Jarrell R, Sasser M, Gelb MH. Fatly acid amides: scooting mode-based discovery of tight-binding competitive inhibitors of secreted phospholipase A2. J Med Chem 1992; 35: 3584–3586
  • Slaich PK, Primrose WU, Robinson DH, Wharton CW, White AJ, Drabble K, Roberts G CK. The binding of amide substrate analogues to phospholipase A2. Biochem J 1992; 288: 167–173
  • Yu L, Dennis EA. Defining the dimensions of the catalytic site of phospholipase A2 using amide substrate analogues. J Am Chem Soc 1992; 114: 8757–8763
  • Potts B CM, Faulkner DJ. Phospholipase A2 inhibitors from marine organisms. J Natural Prod 1992; 55: 1701–1717
  • Potts B CM, Faulkner DJ, de Carvalho MS, Jacobs RS. Chemical mechanism of inactivation of bee venom phospholipase A2 by the marine natural products manoalide, luffariellolide, and scalaradial. J Am Chem Soc 1992; 114: 5093–5100
  • Caufield CE, Rinker JM, von Burg G, Glaser K, Marshall L, Sung A, Lock T, Bauer J, Carlson R, Chang JY, Weichman B. Development of a series of potent selective PLA2 inhibitors with in vivo activity. 205th American Chemical Society National Meeting, Denver, Colorado, March 28-April 2, 1993, MEDI 106
  • Tanaka K, Matsutani S, Matsumoto K, Yoshida T. A novel type of PLA2 inhibitor, thielocin A1β, mechanism of action. J Antibiotics 1992; 45: 1071–1078
  • Miyake A, Yamamoto H, Takebayashi Y, Imai H, Honda K. The novel natural product YM-25567–1 [(+) trans-4-(3-dodecanoyl-2,4,6-trihydroxyphenyl)-7-hydroxy-2-(4-hydroxyphenyl) chroman]: A competitive inhibitor of group II phospholipase A2. J Pharmacol Exp Ther 1992; 263: 1302–1307
  • Tobetto K, Yasui T, Ando T, Hayaishi M, Motohashi N, Shinogi M, Mori I. Inhibitory effects of hyaluronan on [14CJ arachidonic acid release from labeled human synovial fibroblasts. Japan J Pharmacol 1992; 60: 79–84
  • Duval D, Freyss-Begiun M. Glucocorticoids and prostaglandin synthesis: We cannot see the wood for the trees. Prostaglandins, Leukotrienes Essential Fatty Acids 1992; 45: 85–112
  • Goulding N, Guyre PM. Glucocorticoids, lipocortins and the immune response. Cur Opin Immunol 1993; 5: 108–113
  • Sautebin L, Carnuccio R, Lalenti A, Di Rosa M. Lipocortin and vasocortin: Two species of anti-inflammatory proteins mimicking the effects of glucocorticoids. Pharmacol Respondent 1992; 25: 1–12
  • Morand EF, Jefferiss CM, Goulding NJ, Maddison PJ. Induction of lipocortin 1 by glucocorticoids is impaired in rheumatoid arthritis (RA). Arthritis Rheum 1991; 34: S155, (Sup)
  • Duncan GS, Peers SH, Carey F, Forder RA, Flower RJ. The local anti-inflammatory action of dexamethasone in the rat carrageenan edema model is reversed by an antiserum to lipocortin-1 in the rat. Br J Pharmacol 1993; 108: 62–65
  • Podgorski MR, Goulding NJ, Hall ND, Flower RJ, Maddison. Autoantibodies to lipocortin 1 are associated with impaired glucocorticoid responsiveness in rheumatoid arthritis. J Rheumatol 1992; 19: 1668–1671
  • Sierra-Honigmann MR, Murphy PA. Suppression of interleukin-1 action by phospholipase A2 inhibitors in helper T lymphocytes. Peptide Res 1992; 5: 258–261
  • Cabre F, Moreno JJ, Carabaza A, Ortega E, Mauleon D, Carganico G. Antiflammins, anti-inflammatory activity and effect on human phospholipase A2. Biochem Pharmacol 1992; 44: 519–525
  • Cirino G, Cicala C, Sorrentino L, Ciliberto G, Arpaia G, Perretti M, Flower RJ. Anti-inflammatory actions of an N-terminal peptide from human lipocortin-1. Br J Pharmacol 1993; 108: 573–574
  • Perretti M, Flower RJ, Goulding NJ. The ability of murine leukocytes to bind lipocortin 1 is lost during acute inflammation. Biochem Biophy Res Commun 1993; 192: 345–350
  • Tramposch KM, Steiner SA, Stanley P, Nettleton DO, Franson RC, Lewin AH, Carroll FI. Novel inhibitor of phospholipase A2 with topical anti-inflammatory activity. Biochem Biophys Res Commun 1992; 189: 272–279
  • Kreft A, Failli A, Nelson J, Musser J, Kubrak D, Banker A, Shah U, Steffan R, Schiehser G, Sturm R, Holloway D, Sung M-L, Bauer J, Marshall L, Glaser K. Structure-activity relationships leading to WAY-121,520, a tris-aryl indomethacin-based PLA2/leukotriene biosynthesis inhibitor. Agents Actions
  • Raghupathi R, Franson RC. Inhibition of phospholipase A2 by cis-unsaturated fatty acids: evidence for the binding of fatty acid to enzyme. Biochim Biophys Acta 1992; 1126: 206–214
  • Glaser K, Carlson R, Sung A, Bauer J, Lock Y-W, Holloway D, Sturm R, Hartman D, Berkenkopf J, Woeppel S, Howell R, Gray W, Grimes D, Kubrak D, Banker A, Kreft A, Weichman B. Pharmacological characterization of WAY-121,520: a potent anti-inflammatory indomethacin-based inhibitor of 5-lipoxygenase (5-LO) and phospholipase A2 (PLA2). Agents Actions
  • Kohler T, Heinisch M, Kirchner M, Peinhardt G, Hirschelmann R, Nuhn P. Phospholipase A2 inhibition by alkylbenzoylacrylic acids. Biochem Pharmacol 1992; 44: 805–813
  • Wilkerson W, DeLucca I, Galbraith W, Harris R, Kerr J. Anti-inflammatory β-benzene ethanamines III. Bioorg Med Chem Lett 1993; 3: 711–716
  • Zupan LA, Weiss RH, Hazen SL, Parnas BL, Aston KW, Lennon PJ, Getman DP, Gross RW. Structural determinants of haloenol lactone-mediated suicide inhibition of canine myocardial calcium-independent phospholipase A2. J Med Chem 1993; 36: 95–100
  • Barbour SG, Dennis EA. Antisense inhibition of group II phospholipase A2 blocks the production of PGE2 by P388D1 cells. FASEB J 1993; 7: A1265
  • Hardingham TE, Venn G, Bayliss MT. Chondrocyte responses in cartilage and in experimental osteoarthritis. Br J Rheumatol 1991; 30(Sup 1)32–37
  • Schwartz MA, Van Wart HE. Synthetic inhibitors of bacterial mammalian interstitial collagenases. Prog Med Chem 1992; 29: 271–334
  • Murphy G, Hembry RM. Proteinases in rheumatoid arthritis. J Rheumatol 1992; 19(Sup 32)61–64
  • Murphy G, Docherty A JP. The matrix metalloproteinases and their inhibitors. Am J Respir Cell Mol Biol 1992; 7: 120–125
  • Goodacre JA, Pearson JP. Human cartilage proteoglycan as T cell autoantigen. Ann Rheum Dis 1992; 51: 1094–1097
  • Mignatti P, Rifkin DB. Biology and biochemistry of proteinases in tumor invasion. Physiolog Rev 1993; 73: 161–195
  • Sorsa T, Konttinen YT, Lindy O, Ritchlin C, Saari H, Suomalainen K, Eklund KK, Santavirta S. Collagenase in synovitis of rheumatoid arthritis. Sem Arth Rheum 1992; 22: 44–53
  • Brtnckerhoff CE. Regulation of metalloproteinase gene expression: Implications for osteoarthritis. Crit Rev Eukaryotic Gene Expression 1992; 2: 145–164
  • Ye Q-Z, Johnson LL, Hupe DJ, Baragi V. Purification and characterization of human stromelysin catalytic domain expressed in Escherichia coli. Biochemistry 1992; 31: 11231–11235
  • Johnson WH. Collagenase inhibitors Drug News Perspec 1990; 3: 453–458
  • Henderson B, Docherty A JP, Beeley N RA. Design of inhibitors of articular cartilage destruction. Drugs Fut 1990; 15: 495–508
  • Drummond AH. Synthetic inhibitors of matrix-degrading metalloproteinases. 2nd 1BC Symposium on Advances in Understanding and Treating Rheumatoid Arthritis, New Orleans, LA, November, 9–101992
  • Harris GH, Hoogsteen K, Silverman KC, Raghoobar SL, Bills GF, Lingham RB, Smith JL, Dougherty HW, Cascales C, Pelaez F. Isolation and structure determination of pycnidione, a novel bistropolone stromelysin inhibitor from a Phoma sp. Tetrahedron 1993; 49: 2139–2144
  • Niedzwiecki L, Teahan J, Harrison RK, Stein RL. Substrate specificity of the human matrix metalloproteinase stromelysin and the development of continuous fluorometric assays. Biochemistry 1992; 31: 12618–12623
  • Greenwald RA. Tetracycline derivatives as potential inhibitors of connective tissue degradation. Drug News Perspec 1990; 3: 161–166
  • Bols M, Binderup L, Hansen J, Rasmussen P. Inhibition of collagenase by aranciamycin and aranciamycin derivatives. J Med Chem 1992; 35: 2768–2771
  • Lewis AJ, Glaser KB, Sturm RJ, Molnar-Kimber KL, Bansbach CC. Strategies for the development of new antiarthritic agents. Int J Immunopharmacol 1992; 14: 497–504
  • Woessner JF. Matrix metalloproteinases and their inhibitors in connective tissue remodeling. FASEB J 1991; 5: 2145–2154
  • Mainardi CL, Pourmotabbed TF, Hasty KA. Inflammatory phagocytes and connective tissue degrading metalloproteinases. Am J Med Sci 1991; 302: 171–175
  • Clark IM, Powell LK, Ramsey S, Hazleman BL, Cawston TE. The measurement of collagenase, tissue inhibitor of metalloproteinases (TIMP) and collagenase - TIMP complex in synovial fluids from patients with osteoarthritis and rheumatoid arthritis. Arth Rheum 1993; 36: 372–379
  • Dean D. Proteinase-mediated cartilage degradation in osteoarthritis. Sem Arth Rheum 1991; 20(Suppl 2)2–11
  • Murphy G, Docherty A JP, Hembrey RM, Reynolds JJ. Metalloproteinases and tissue damage. Br J Rheumatol 1991; 30(Suppl 1)25–31
  • Lohmander LS, Hoerrner LA, Lark MW. Metalloproteinases, tissue inhibitors, and proteoglycan fragments in knee synovial fluid in human osteoarthritis. Arth Rheum 1993; 36: 181–189
  • Andrews HJ, Plumpton TA, Harper GP, Cawston TE. A synthetic peptide metalloproteinase inhibitor, but not Timp, prevents the breakdown of proteoglycan within articular cartilage in vitro. Agents Actions 1992; 37: 147–154
  • Cronstein BN, Weissman G. The adhesion molecules of inflammation. Arth Rheum 1993; 36: 147–157
  • Bevilacqua MP, Nelson RM. Selectins. J Clin Invest 1993; 91: 379–387
  • Johnson BA, Haines GK, Harlow LA, Koch AE. Adhesion molecule expression in human synovial tissue. Arth Rheum 1993; 36: 137–146
  • Mason JC, Kapahi P, Haskard DO. Detection of increased levels of circulating intracellular adhesion molecule 1 in some patients with rheumatoid arthritis but not in patients with systemic lupus erythematosus. Arth Rheum 1993; 36: 519–527
  • Wilkinson LS, Edwards, Poston RN, Haskard DO. Expression of vascular cell adhesion molecule-1 in normal and inflamed synovium. Lab Invest 1993; 68: 82–88
  • Makgoba MW, Bernard A, Sanders ME. Cell adhesion/signalling: biology and clinical applications. Eur J Clin Invest 1992; 22: 443–453
  • Jasin HE, Lightfoot E, Davis LS, Rothlein R, Faanes RB, Lipsky PE. Amelioration of antigen-induced arthritis in rabbits treated with monoclonal antibodies to leukocyte adhesion molecules. Arth Rheum 1992; 35: 541–549
  • Kavanaugh A, Nichols LA, Lipsky PE. Anti-CD54 (intercellular adhesion molecule-1; ICAM-1) monoclonal antibody therapy in refractory rheumatoid arthritis. J Allergy Clin Immunol 1993; 91: 227
  • Gamble JR, Skinner MP, Berndt MC, Vadas MA. Prevention of activated neutrophil adhesion to endothelium by soluble adhesion protein GMP140. Science 1990; 249: 414–417
  • Fecondo JV, Kent S BH, Boyd AW. Inhibition of intercellular adhesion molecule 1-dependent biological activities by a synthetic peptide analog. Proc Natl Acad USA 1991; 88: 2879–2882
  • Ross L, Hassman F, Molony L. Inhibition of Molt-4-endothelial adherence by synthetic peptides from the sequence of ICAM-1. J Biol Chem 1992; 267: 8537–8543
  • Coraldo J, Mazerolles F, Le Deist F, Barbat C, Kaczorek M, Fischer A. Inhibition of CD+ T cell activation and adhesion by peptides derived from the gp160. J Immunol 1991; 147: 475–482
  • Geng J-G, Heavener GA, McEver RP. Lectin domain peptides from selectins interact with both cell surface ligands and Ca2+ ions. J Biol Chem 1992; 267: 19846–19853
  • Foxall C, Watson SR, Dowbenko D, Fennie C, Lasky LA, Kiso M, Hasegawa A, Asa D, Brandley BK. The three members of the selectin receptor family recognize a common carbohydrate epitope, the sialyl Lewisx oligosaccharide. J Cell Biol 1992; 117: 895–902
  • Parekh RB, Patel T. Carbohydrate ligands of the LECAM family as candidates for the development of anti-inflammatory compounds. J Pharm Pharmacol 1992; 44(Suppl 1)168–171
  • Musser JH. Carbohydrates as drug discovery leads. Annual Reports Med Chem 1992; 27: 301–310
  • Ball GE, O'Neill RA, Schultz JE, Lowe JB, Weston BW, Nagy JO, Brown EG, Hobbs CJ, Bednarski. Synthesis and structural analysis using 2-D NMR of sialyl Lewis X (SLex) and Lewis X (Lex) oligosaccharides: Ligands related to E-selectin (ELAM-1) binding. J Am Chem Soc 1992; 114: 5449–5451
  • Ichikawa Y, Lin Y-C, Dumas DP, Shen G-S, Garcia-Junceda E, Williams MA, Bayer R, Ketcham C, Walker LE, Paulson JC, Wong C-H. Chemical-enzymatic synthesis and conformational analysis of sialyl Lewis x and derivatives. J Am Chem Soc 1992; 114: 9283–9298
  • Lin Y-C, Hummel CW, Huang D-H, Ichikawa Y, Nicolaou KC, Wong C-H. Conformational studies of sialyl Lewis x in aqueous solution. J Am Chem Soc 1992; 114: 5452–5454
  • Miller KE, Mukhopadhyay C, Cagas P, Brush CA. Solution structure of the Lewis X oligosaccharide determined by NMR spectroscopy and molecular dynamic simulations. Biochemistry 1992; 31: 6703–6709
  • Asada M, Furukawa K, Kantor C, Gahmberg CG, Kobata A. Structural study of the sugar chains of human leukocyte cell adhesion molecules CD11/CD18. Biochemistry 1991; 30: 1561–1571
  • Green PJ, Tamatani T, Watanabe, Miyasaka M, Hasegawa A, Kiso M, Yuen C-T, Stoll MS, Feizi T. High affinity binding of the leukocyte adhesion molecule L-selectin to 3′-sulphated-Lea and Lex oligosaccharides and the predominance of sulphate in this interaction demonstrated by binding studies with a series of lipid-linked oligosaccharides. Biochem Biophys Res Commun 1992; 188: 244–251
  • Yuen C-T, Lawson AM, Chai W, Larkin M, Stoll MS, Stuart AC, Sullivan FX, Ahern TJ, Feizi T. Novel sulfated ligands for the cell adhesion molecule E-selectin revealed by the neoglycolipid technology among O-linked oligosaccharides on an ovarian cystadenoma glycoprotein. Biochemistry 1992; 31: 9126–9131
  • Suzuki Y, Toda Y, Tamatani T, Walanabe T, Suzuki T, Nakao T, Murase K, Kiso M, Hasegawa A, Tadano-Aritomi K, Ishizuka I, Miyasaka M. Sulfated gylcolipids are ligands for a lymphocyte homing receptor, L-selectin (LECAM-1), binding epitope in sulfated sugar chain. Biochem Biophys Res Commun 1993; 190: 426–434
  • Needham LK, Schnaar RL. The HNK-1 reactive sulfoglucuronyl glycolipids are ligands for L-selectin and P-selectin but not E-selectin. Proc Natl Acad USA 1993; 90: 1359–1363
  • Imai Y, Lasky LA, Rosen SD. Sulphation requirement for GlyCAM-1, an endothelial ligand for L-selectin. Nature 1993; 361: 555–557
  • Erbe DV, Wolitsky BA, Presta LG, Norton CR, Ramos RJ, Burns DK, Rumberger JM, Rao B NN, Foxall C, Brandley BK, Lasky LA. Identification of an E-selectin region critical for carbohydrate recognition and cell adhesion. J Cell Biol 1992; 119: 215–227
  • Norgard KE, Han H, Powell L, Kriegler M, Varki A, Varki NM. Enhanced interaction of L-selectin with the high endothelial venule ligand via selectively oxidized sialic acids. Proc Natl Acad USA 1993; 90: 1068–1072
  • Ackerman NR. Carbohydrate-based inhibitors of cell adhesion. 2nd IBC Symposium on Advances in Understanding and Treating Rheumatoid Arthritis, New Orleans, LA, November, 9–101992
  • Crooke ST. Therapeutic applications of oligonucleotides. Bio/technology 1992; 10: 882–886
  • Gillespie D. Perspectives for antisense nucleic acid therapy. Drug News Perspec 1992; 5: 389–396
  • Chiang M-Y, Chan H, Zounes MA, Freier SM, Lima WF, Bennett CF. Antisense oligonucleotides inhibit intercellular adhesion molecule 1 expression by two distinct mechanisms. J Biol Chem 1991; 266: 18162–18171
  • Burch RM, Weitzberg M, Blok N, Muhlhauser R, Martin D, Farmer S, Bator JM, Connor JR, Ko C, Kuhn W, McMillan BA, Raynor M, Shearer BG, Tiffany C, Wilkins DE. N-(fluorenyl-9-methoxycarbonyl) amino acids, a class of antiinflammatory agents with a different mechanism of action. Proc Natl Acad USA 1991; 88: 355–359
  • Bator JM, Weitzberg M, Burch RM. N-[9H-(2,7-dimethylfluorenyl-9-methoxy) carbonyl]-L-leucine, NPC 15669, prevents neutrophil adherence to endothelium and inhibits CD11b/CD18 upregulation. Immunopharmacol 1992; 23: 139–149
  • Burch RM, Connor JR, Bator JM, Weitzberg M, Laemont K, Noronha-Blob L, Sullivan JP, Steranka LR. NPC 15669 inhibits the reversed passsive Arthus reaction in rats by blocking neutrophil recruitment. J Pharmacol Ex Ther 1992; 263: 933–937
  • Noronha-Blob L. “Leumedins:” Leukocyte recruitment inhibitors. 2nd IBC Symposium on Advances in Understanding and Treating Rheumatoid Arthritis, New Orleans, LA, November, 9–101992
  • Cronstein BN, Kimmel SC, Levin RI, Martiniuk F, Weissman G. A mechanism for the antiinflammatory effects of corticosteroids: The glucocorticoid receptor receptor regulates leukocyte adhesion to endothelial cells and expression of endothelial-leukocyte adhesion molecule-1 and intercelluar adhesion molecule-1. Proc Natl Acad Sci USA 1992; 89: 9991–9995
  • Corkill MM, Kirkham BW, Haskard DO, Barbatis C, Gibson T, Panyani GS. Gold treatment of rheumatoid arthritis decreases synovial expression of the endothelial leukocyte adhesion receptor ELAM-1. J Rheumatol 1991; 18: 1453–1460
  • Asako H, Kubes P, Baethge BA, Wolf RE, Granger DN. Reduction of leukocyte adherence and emigration by cyclosporine and L683.590 (FK506) in postcapillary venules. Transplantation 1992; 54: 686–690
  • Greenfield SM, Hamblin AS, Shakoor ZS, Teare JP, Punchard NA, Thompson R PH. Inhibition of leucocyte adhesion molecule upregulation by tumour necrosis factor α: a novel mechanism of action of sulphasalazine. Gut 1993; 34: 252–256
  • Camp MA, Wood RG, Kinasewitz GT. Hyaluronic acid modulates gamma-interferon stimulated lymphocyte adhesion to human mesothelial cells. Clin Res 1990; 38: 958A
  • Audette CA, Burstein S. Inhibition of leukocyte adhesion by the in vivo and in vitro administration of cannabinoids. Life Sci 1990; 47: 753–759
  • Siney L, Lewis MJ. Endothelium-derived relaxing factor inhibits platelet adhesion to cultured porcine endocardial endothelium. Eur J Pharmacol 1992; 229: 223–226
  • Kotovuori P, Tontti E, Pigott R, Shepherd M, Kiso M, Hasegawa A, Renkonen R, Nortamo P, Altieri DC, Gahmberg CG. The vascular E-selectin binds to the leukocyte integrins CD11/CD18. Glycobiology 1993; 3: 131–136
  • Etzioni A, Frydman M, Pollack S, Avidor I, Phillips ML, Paulson JC, Gershoni-Baruch R. Recurrent infections caused by a novel adhesion deficiency. New Engl J Med 1992; 327: 1789–1792
  • Kroemer G, Martinez AC. Cytokines and autoimmune disease. Clin Immunol Immunopath 1991; 61: 275–295
  • Arend WP, Dayer JM. Cytokines and cytokine inhibitors or antagonists in rheumatoid arthritis. Arth Rheum 1990; 33: 305–315
  • Dayer JM, Fenner H. The role of cytokines and their inhibitors in arthritis. Balliare Clin Rheum 1992; 6: 485–516
  • Firestein GS, Zvaifler WJ. How important are T cells in chronic rheumatoid synovitis?. Arth Rheum 1990; 33: 768–773
  • Dinarello CA. Interleukin-1 and interleukin-1 antagonism. Blood 1991; 77: 1827–1852
  • Dawson J, Edwards J CW, Sedgwick AD, Lees P. IL-1α inhibits lymphocyte migration into a site of chronic inflammation. Immunol Letters 1991; 30: 319–324
  • Hannum CH, Wilcox CJ, Arend WP, Joslin FG, Dripps DJ, Heimdal PL, Armes LG, Sommer A, Eisenberg SP, Thompson RC. Interleukin-1 receptor antagonist activity of a human interleukin-1 inhibitor. Nature 1990; 343: 341–346
  • Arend WP. IL-1 receptor antagonist. J Clin Invest 1991; 88: 1445–1451
  • Arend WP, Coll BP. Interaction of recombinant monocyte-derived interleukin-1 receptor antagonist with rheumatoid synovial cells. Cytokine 1991; 3: 407–413
  • Dinarello CA, Thompson RC. Blocking IL-1: interleukin-1 receptor antagonist in vivo and in vitro. Immunol Today 1991; 12: 404–410
  • Lebsack ME, Paul CC, Bledow DC, Burch FX, Sack A, Chase W, Catalano MA. Subcutaneous IL-1 receptor antagonist in patients with rheumatoid arthritis. Arth Rheum 1991; 34: 545
  • Poutsiaka DD, Clark BD, Vannier E, Dinarello CA. Production of interleukin-1 receptor antagonist and interleukin-1β by peripheral blood mononuclear cells is differentially regulated. Blood 1991; 78: 1275–1281
  • Betini R, Sironi M, Martin-Padura I, Colotta F, Rambaldi S, Bernasconi S, Ghezzi P, Haskill SJ, Liu D, Mantovani A. Inhibitory effect of recombinant intracellular interleukin 1 receptor antagonist on endothelial cell activation. Cytokine 1992; 4: 44–47
  • Arend WP. IL-1 antagonism in inflammatory arthritis. Lancet 1993; 341: 155–156
  • Miller LC, Lynch EA, Isa S, Logan JW, Dinarello CA, Steere AC. Balance of synovial fluid IL-1β and IL-1 receptor antagonist and recovery from Lyme Arthritis. Lancet 1993; 341: 146–148
  • Fanslow WC, Sims JE, Sassenfeld H, Morrissey PJ, Gillis S, Dower KD, Widmer MB. Regulation of alloreactivity in vivo by a soluble form of the interleukin-1 receptor. Science 1990; 248: 739–742
  • Jacobs CA, Baker PE, Roux ER, Picha KS, Toivola B, Waugh S, Kennedy MK. Experimental autoimmune encephalomyelitis is exacerbated by IL-1α and suppressed by soluble IL-1 receptor. J Immunol 1991; 146: 2983–2989
  • Dinarello CA, Gelfand JA. Anticytokine strategies in the treatment of the systemic inflammatory response syndrome. JAMA 1993; 269: 1829–1835
  • Shields J, Mazzei GJ. Natural interleukin-1 inhibitors. Clin Biotechnol 1991; 3: 81–87
  • McIntyre KW, Stepan GJ, Kolinsky KD, Benjamin WR, Plocinski JM, Kaffka KL, Campen CA, Chizzonite RA, Kilian PL. Inhibition of interleukin 1 (IL-1) binding and bioactivity in vitro and modulation of acute inflammation in vivo by IL-1 receptor antagonist and anti-IL-1 receptor monoclonal antibody. J Exp Med 1991; 173: 931–939
  • Burch RM, Mahan LC. Oligonucleotides antisense to the interleukin-1 receptor mRNA block the effects of interleukin-1 in cultured murine and human fibroblasts and in mice. J Clin Invest 1991; 88: 1190–1196
  • Rosenthal GJ, Corsini E, Craig WA, Comment CE, Luster MI. Pentamidine: an inhibitor of interleukin-1 that acts via a post-translation event. Toxicol Appl Pharmacol 1991; 107: 555–561
  • Bender PE, Lee JC. Pharmacologic modulation of interleukin-1. Ann Rep Med Chem 1989; 25: 185–193
  • Schmidt JA, Tocci MJ. Interleukin-1. The Handbook of Experimental Pharmacology, Vol. 95.1. Peptide Growth Factors and Their Receptors Berlin, M Sporn, A Roberts. Springer-Verlag, Germany 1990; 473
  • Howard AD, Kostura MJ, Thornberg N, Ding G JF, Limjuco G, Weidner J, Salley JP, Hogquist KA, Chaplin DD, Mumford RA. IL-1 converting enzyme require aspartic acid residues for processing of the IL-1β precursor at two distinct sites and does not cleave 31-kDa IL-1α. J Immunol 1991; 147: 2964–2969
  • Kostura MJ, Tocci MJ, Limjuco G, Chin J, Cameron P, Hillman A, Chartrain N, Schmidt J. Identification of a monocyte specific interleukin-1 convertase activity. Proc Natl Acad Sci USA 1989; 86: 5227–5231
  • Thornberry NA, Bull HG, Calayeay JR, Chapman KT, Howard AD, Kostura MJ, et al. A novel heterodimeric cysteine protease is required for interleukin-1 beta processing in monocytes. Nature 1992; 356: 768–774
  • Lee SW, Tsou AP, Chan H, Thomas J, Petrie K, Eugui EM, Allison AC. Glucocorticoids selectively inhibity the transcription of the interleukin 1β gene and decrease the stability of interleukin 1β mRNA. Proc Natl Acad Sci USA 1988; 85: 1204–1208
  • Allison AC, Personal communication
  • Dayer JM, Fenner H. The role of cytokines and their inhibitors in arthritis. Balliere's Clin Rheum 1992; 6: 485–516
  • Deleuran B, Chu CQ, Field M, Brennan FM, Mitchell T, Brockhaus M, Feldmann M, Maini RN. Localization of TNF receptors in the synovial tissue and cartilage/pannus junction in rheumatoid arthritis: implications for local actions of TNFα. Arth Rheum 1992; 35: 1170–1178
  • Askenazi A, Masters S, Capon DJ, Charnow SM, Figari IS, Pennica D, Goeddel DV, Palladino MA, Smith DH. Protection against entoxic shock by a tumor necrosis factor receptor immunoadhesion. Proc Natl Acad Sci USA 1991; 88: 10535–10539
  • Shanahan F, Niederlehnar A, Carramanzana N, Anton P. Sulfasalazine inhibits binding of TNFα to its receptor. Immunopharm 1990; 20: 217–224
  • Martin LW, Catania A, Hiltz ME, Lipton JM. Neuropeptide α-MSH antagonises IL-6 and TNF-induced fever. Peptides 1991; 12: 297–299
  • Lee JC, Rebar L, Laydon JT. Effect of SK&F 86002 on cytokine production by human monocytes. Agents Actions 1989; 27: 277–279
  • Ziegler-Heitbrock L HW, Kafferlein E, Haas JG, Meyer N, Strobel M, Weber C, Flieger D. Gangliosides suppress tumor necrosis factor production in human monocytes. J Immunol 1992; 148: 1753–1758
  • Molnar-Kimber KL, Yonno L, Heaslip RJ, Weichman BM. Differential regulation of TNF-α and IL-1β production from endotoxin stimulated human monocytes by phosphodiesterase inhibitors. Mediators Inflam 1992; 1: 411–417
  • Maini RN, Brennan FM, Williams R, Chu CQ, Cope AP, Gibbons D, Elliott M, Feldmann M. TNF-α in rheumatoid arthritis and prospects of anti-TNF therapy. Clin Exp Rheum 1993; 11(supl 8)S173–-S175
  • Banner DW, D'Arcy A, Janes W, Gentz R, Schoenfeld H-J, Broger C, Loetscher H, Lesslauer W. Crystal structure of the soluble human 55 kd TNF receptor - human TNFβ complex: Implications for TNF receptor activation. Cell 1993; 73: 431–445
  • Kishimoto T. Interleukin-6 and its receptors; from cloning to clinic. Int Arch Aller Immunol 1992; 99: 172–177
  • Wood NC, Symons JA, Dickens E, Duff GW. In situ hybridization of IL-6 in rheumatoid arthritis. Clin Exp Immunol 1992; 87: 183–189
  • Kline B, Lu ZY, Bataille R. Clinical application of IL-6 inhibitors. Res Immunol 1992; 54: 774–776
  • Minty A, Chalon P, Derocq JM, Dumont X, Guillemot JC, Kaghad M, Labit C, Leplatois P, Liauzun P, Miloux B, Minty C, Casellas P, Loison G, Lupker J, Shire D, Ferrara P, Caput D. Interleukin-13 is a new human lymphokine regulating inflammatory and immune response. Nature 1993; 362: 248–250
  • Klein B, Wizdenes J, Xang XG, Jourdan M, Boiron JM, Brochier J, Wautaud J, Melin M, Clement C, Morel-Fournier B, Lu ZY, Mannoni P, Sany J, Batoille R. Murine anti-interleukin-6 monoclonal antibody therapy for a patient with plasma cell leukemia. Blood 1991; 5: 1198–1204
  • Barton BE, Jackson JV. Protective role in the lipopolysaccharide-galactosamine septic shock model. Infect Immun 1993; 61: 1496–1499
  • Larsen CG, Anderson AO, Apella E, Oppenheim JJ, Matsushima K. The neutrophil activating protein (NAP-1) is also chemotactic for T lymphocytes. Science 1989; 243: 1464–1465
  • Brennan FM, Zachariae C OC, Chartry D, Larsen CG, Tuma M, Maini RN, Feldmann M. Detection of interleukin 8 (IL-8) biological activity in synovial fluids from patients with rheumatoid arthritis and production of IL-8 mRNA by isolated synovial cells. Eur J Immunol 1990; 20: 2141–2144
  • Peichl P, Ceska M, Effenberger F, Hauberhauer G, Broell I, Lindley I JD. Presence of NAP-1/IL-8 in synovial fluids indicates a possible pathogenic role in rheumatoid arthritis. Scand J Immunol 1991; 34: 333–339
  • Deleuran B, Kristensen M, Palindan K, Zachariae C, Larsen CG, Zachariae E, Thestrup-Pedersen K. The effect of second-line antirheumatic drugs on interleukin-8 mRNA synthesis and protein secretion in human endothelial cells. Cytokine 1992; 4: 403–409
  • Seitz M, Dewald B, Ceska M, Gerber N, Baggiolini M. Interleukin-8 in inflammatory rheumatic diseases: synovial fluid levels in relation to rheumatoid factors, production by mononuclear cells, and effects of gold sodium thiomalate and methotrexate. Rheumatol Int 1992; 12: 159–164
  • Seitz M, Dewald B, Gerber N, Baggiolini M. Enhanced production of neutrophil-activating peptides-1 interleukin-8 in rheumatoid arthritis. J Clin Invest 1991; 87: 463–469
  • Larsen CG, Palindan K, Kristensen M, Deleuran B, Thomsen MK, Pedersen FS, Matsushima K, Thestrup-Pedersen K. ETH614, a novel inhibitor of interleukin-8 (IL-8) production. J Invest Dermatol 1990; 95: 478
  • Lee J, Horuk R, Rice GC, Bennett GL, Camerato T, Wood WI. Characterization of two high affinity human interleukin-8 receptors. J Biol Chem 1992; 267: 16283–16287
  • Hafler DA, Zhang J-W, LaSalle J, Donnelly C, Weiner HL, Wuchenpfeffernig K. The development of antigen specific therapies for autoimmune diseases; investigations in multiple sclerosis as a paradigm for rheumatoid arthritis. Clin Exp Rheumatol 1993; 11(Suppl 8)S39–S40
  • Nagler-Anderson C, Bober LS, Robinson ME, Siskind GW, Thorbecke GJ. Suppression of type II collagen-induced arthritis by intragastric administration of soluble type II collagen. Proc Natl Acad Sci USA 1986; 83: 7443–7446
  • Adorini L. Inhibition of T cell activation by MHC blockade: a possible strategy for immunointervention in autoimmune disease. J Autoimmunity 1992; 5(suppl A)73–81
  • Lamont AG, Sette A, Fujinami R, Colon SM, Milesl C, Grey HM. Inhibition of experimental autoimmune encephalomyelitis induction in SJL/J mice by using a peptide with high affintiy for I-A molecules. J Immunol 1990; 145: 1687–1692
  • Adorini L, Guery J-C, Tembleau S. Approaches toward peptide-based immunotherapy of autoimmune diseases. Springer Semin Immunopathol 1992; 14: 187–199
  • Mor E, Cohen IR. Experimental aspects of T cell vaccination. Clin Exp Rheumatol 1993; 11(Suppl 8)S55–S57
  • Van Laar JM, De Vries R RP, Breedveld FC. T cell vaccination in humans: the experience in rheumatoid arthritis. Clin Exp Rheumatol 1993; 11(Supp l8)S59–S62
  • Kingsley G, Panayi GS. Intervention with immunomodulatory agents: T cell vaccination. Management of Early Inflammatory Arthritis, P Emery. Balliere's Clin Rheumatol, London 1992; 6: 435–454
  • Chatenoud L, Ferran C, Renter A, Legendre C, Gevaert Y, Kreis H, Franchimont P, Bach JF. Systemic reaction to the monoclonal antibody OKT3 in relation to serum levels of tumor necrosis factor and interferon γ. N Engl J Med 1989; 320: 1420
  • Strand V, Lee ML. Differential patterns of response with rheumatoid arthritis following administration of an anti-CD5 immunoconjugate. Clin Exp Rheumatol 1993; 11(Suppl 8)S161–S163
  • Watts RA, Isaacs JD, Hale G, Hazleman BL, Waldmann H. CAMPATH-1H in inflammatory arthritis. Clin Exp Rheumatol 1993; 11(Suppl 8)S165–S167
  • Horneff G, Burmeister GR, Emmrich F, Kalden JR. Treatment of rheumatoid arthritis with an anti-CD4 monoclonal antibody. Arth Rheum 1991; 34: 129–140
  • Moreland LW, Bucy RP, Tilden A, Pratt PW, LoBaglio AF, Khazaeli M, Everson MP, Daddona P, Ghrayeb J, Kilgarriff C, Sanders MG, Koopman WJ. Use of a chimeric monoclonal anti-CD4 antibody in patients with refractory rheumatoid arthritis. Arth Rheum 1993; 36: 307–318
  • Horneff G, Winkler T, Kalden J, Emmrich F, Burmester G. Human anti-mouse antibody response induced by anti-CD4 monoclonal antibody therapy in patients with rheumatoid arthritis. Clin Immunol Immunopathol 1991; 59: 89–103
  • Goldblum R. Therapy of rheumatoid arthritis with mycophenolate mofetil. Clin Exp Rheumatol 1993; 11(Suppl 8)S117–S119
  • Allison AC, Mullen CD, Almquist SJ, Eugui EM. In vitro immunosuppressive effects of mycophenolic acid and an ester pro-drug RS-6144 3. Transplant Proc 1991; 23(Suppl 2)10–14
  • Bartlett RR, Schleyerbach R. Immunopharmacological profile of a novel isoxazole derivative, HWA 486, with potential antirheumatic activity 1. Disease modifying action on adjuvant arthritis of the rat. Int J Immunopharmac 1985; 7: 7–18
  • Bartlett RR, Zielinski J, Schorlemmer HU, Campion G, Musikic P, Schleyerbach R. Leflunomide: a novel immunomodulating drug. Non-steroidal Antiinflammatory DrugsSecond Edition, AJ Lewis, DJ Furst. Marcel Dekker, New York, In press
  • Popvic S, Bartlett RR. Disease modifying activity of HWA 486 on the development of SLE in MRL/I-mice. Agents Actions 1986; 19: 313–314
  • Bartlett RR, Popovic S, Rais RX. Development of autoimmunity in MRL/Ipr mice and the effect of drugs on this murine disease. Scand J Rheumatol 1988; 75: 290–299
  • Kuchle C CA, Thoenes GH, Langer KH, Schorlemmer HU, Bartlett RR, Schleyerbach R. Prevention of kidney and skin graft rejection in rats by leflunomide, a new immunomodulating agent. Transplant Proc 1991; 23: 1083–1086
  • Forre O, Waalen K, Rugstad HE, Berg KS, Solbu D, Kass E. Cyclosporine and rheumatoid arthritis. Springer Semin Immunopathol 1988; 10: 263–277
  • Thompson AW, Starzl TE. FK-506 and autoimmune disease: perspective and prospects. Autoimmunity 1992; 12: 303–313
  • Heitman J, Mouua NR, Hall MN. Proline isomerases at the crossroads of protein folding signal transduction and immunosuppression. New Biologist 1992; 4,5: 448–460
  • Morris R. Rapamycin: antifungal, antitumor antiproliferative and immunosuppressive macrolides. Transplant Rev 1992; 6: 39–87
  • Carlson RP, Baeder WL, Caccesse RG, Warner LM, Sehgal SN. Effects of orally administered rapamycin in animal models of arthritis and other autoimmune diseases. NY Acad Sci.
  • Otterness IG, Carty TJ, Loose LD. Tenidap: A new drug for arthritis. Therapeutic Approaches to Inflammatory Diseases, AJ Lewis, NS Doherty, NR Ackerman. Elsevier, New York 1989; 229–241
  • Blackburn WD, Heck LW, Loose LD, Eskra JD, Carty TJ. Inhibition of 5-lipoxygenase product formation and polymorphonuclear cell degranulation by tenidap sodium in patients with rheumatoid arthritis. Arth Rheum 1991; 34: 204
  • Otterness IG, Golden H LV, Kadin SB. A novel antiarthritic agent that inhibits in vivo basophil degranulation. Arth Rheum 1989; 32: 146, (suppl)
  • Moilanen E, Alanko J, Asmawi Z, Vapaatalo H. Tenidap, a new antiinflammatory agent, is a potent inhibitor of leukotriene B4 and prostanoid synthesis in human polymorphonuclear leukocytes. Eicosanoids 1988; 1: 35–39
  • Sipe JD, Bartle LM, Loose LD. Modification of proinflammatory cytokine production by the antirheumatic agents tenidap and naproxen. J Immunol 1992; 148: 480–484
  • Proudman KE, McMillan RM. Are tolfenanic acid and tenidap dual inhibitors of 5-lipoxygenase and cyclooxygenase?. Agents Actions 1991; 34: 121–124
  • Otterness IG, Bliven ML, Downs JT, Natoli EJ, Hanson DC. Inhibition of interleukin 1 synthesis by tenidap: a new drug for arthritis. Cytokine 1991; 3: 277–283
  • Cleveland PL, Millard PJ, Showell HJ, Fewtrell C MS. Tenidap: a novel inhibitor of calcium influx in a mast cell line. Cell Calcium 1993; 14: 1–16
  • Al-Humidan AM, Reilly KM, Leeming M RG, Russell R GG. Tenidap inhibits bone resorption induced by PTH, 1,25 Vit D3, IL-1, TNF and PGE2 in vitro by mechanisms independent of prostaglandin synthesis. Arth Rheum 1991; 34(suppl)S192
  • Gordon P. Antiinflammatory actions of an immunomodulator: therafectin, 1,2-O-isopropylidene-3–0-3′-(N', N'-dimethylamino-n-propyl)-D-glucofuranose hydrochloride. Inflammation, mechanisms and treatment, DA Willoughby, JP Giroud. University Park Press, Baltimore 1980; 169–80
  • Kieval RI, Young CT, Prohazka D, Brinckerhoff CE, Trentham DE. Evaluation of a modified hexose sugar, amiprilose hydrochloride, in experimental models of synovitis. J Rheumatol 1989; 16: 67–74
  • Hadden JW. Effects of isoprinosine, levamisole, muramyldipeptide and 1,2-O-isopropylidene-3–0-3′-(N'-N'-dimethylamino-n-propyl)-D-glucofuranose (SM-1213) on lymophocyte and marcopage function in vitro. Cancer Treat Rep 1978; 62: 1981–1985
  • Goldsmith JM, Huprikar J, Wu S JY, Phair JP. Interleukin 1 and interleukin 2 production in homosexual men: a controlled trial of therafectin (SM-1213) a possible immunomodulator. J Immunopharmacol 1986; 8: 1–14
  • Morrison CJ, Gordon P, Hashimoto T. Enhanced killing of Candida albicans by cultured peritoneal exudate cells treated with SM-1213, a synthetic immunomodulator. Antimicrob Agents Chemother 1984; 26: 74–77
  • Garrett ER, Van Peer A. Pharmacokinetics of intravenous and oral 1,2-O-isopropylidene-3–0-3′-(N'-N'-dimethylamino-n-propyl)-D-glucofuranose hydrocholoride in the dog as a function of dose and characterization of metabolites. J Pharm Sci 1983; 72: 1045–1057
  • Garrett ER, Van Peer A, Altmayer P, Schuermann W, Lucker P. Pharmacokinetics of the immunomdulatory 1,2-O-isopropylidene-3–0-3′-(N'-N'-dimethylamino-n-propyl)-D-glucofuranose hydrocholoride in normal human volunteers. J Pharmacokinet Biopharm 1982; 10: 247–64
  • Caldwell JR, Saville PD, Bedsole GD, Pleskow WW, Young CL. Therafectin (amiprilose HCI) in rheumatoid arthritis: a 6 month double blind, placebo-controlled study, followed by a 6 month open extension. Arth Rheum 1987; 30: S57
  • Horwitz DA, Linker-Israeli M, Gray JD, Ehresmann GR. Therafectin, (amiprilose HCI) in rheumatoid arthritis: correlation between clinical improvement and connection of immune dysfunction. Arth Rheum 1987; 30: S57
  • Ehresman GR, Maclaughlin KE, Horwitz DA. Dose-related clinical efficacy of therafectin (amiprilose HCI) in rheumatoid arthritis. Arth Rheum 1987; 30: S34
  • Riskin WG, Gillings DB, Scarlett JA. Amprilose hydrochloride for rheumatoid arthritis. Ann Intern Med 1989; 111: 455–465
  • Veys EM, Mielants H, Verbruggen G, DeKeyser F. Intervention with immunomodulatory agents: new pharmacological developments. Management of Early Inflammatory Arthritis, P Emery. Balliere's Clin Rheumatol, London 1992; 6: 435–454
  • Otterness IG, Pettipher ER. Future therapy for arthritis. Non-steroidal Antiinflammatory DrugsSecond Edition, AJ Lewis, DJ Furst. Marcel Dekker, New York, In press

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