An orally active reversible inhibitor of cathepsin S inhibits human trans vivo delayed-type hypersensitivity

European Journal of Pharmacology

Volumn 538, Issue 1-3, 2006, Pages 168-174

  Desai, Sudha N ^a   White, Della M ^a   O'Shea, Kathryn M ^a   Brown, Maryanne L ^a   Cywin, Charles L ^a   Spero, Denice M ^a   Panzenbeck, Maret J ^a  

^a BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

Author keywords

Antagonist; Cathepsin S; Delayed type hypersensitivity

Indexed keywords

ANTIBODY; CATHEPSIN S; CATHEPSIN S INHIBITOR; ENZYME INHIBITOR; HLA DP ANTIBODY; HLA DP ANTIGEN; HLA DQ ANTIBODY; HLA DQ ANTIGEN; HLA DR ANTIBODY; HLA DR ANTIGEN; MAJOR HISTOCOMPATIBILITY ANTIGEN CLASS 2; TETANUS TOXOID; UNCLASSIFIED DRUG; CATHEPSIN;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIGEN PRESENTING CELL; ARTICLE; CELL FUNCTION; CONTROLLED STUDY; DELAYED HYPERSENSITIVITY; DISEASE MODEL; DRUG EFFECT; FEMALE; FOOT EDEMA; FOOT PAD; HUMAN; HUMAN CELL; IC 50; IN VIVO STUDY; MONOCYTE; MOUSE; NEUTROPHIL; NONHUMAN; NORMAL HUMAN; PERIPHERAL BLOOD MONONUCLEAR CELL; PRIORITY JOURNAL; ANIMAL; BIOAVAILABILITY; C57BL MOUSE; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG ANTAGONISM; GENETICS; IMMUNOLOGY; MOUSE MUTANT; ORAL DRUG ADMINISTRATION; PATHOLOGY; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; CATHEPSINS; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME INHIBITORS; HYPERSENSITIVITY, DELAYED; MICE; MICE, INBRED C57BL; MICE, KNOCKOUT; MOLECULAR STRUCTURE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 33747111460     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2006.03.051     Document Type: Article

References (28)

1. Biroc S.L., Gay S., Hummel K., Magill C., Palmer J.T., Spencer D.R., Sa S., Klaus J.L., Michel B.A., Rasnick D., and Gay R.E. Cysteine protease activity is up-regulated in inflamed ankle joints of rats with adjuvant-induced arthritis and decreases with in vivo administration of a vinyl sulfone cysteine protease inhibitor. Arthritis Rheum. 44 (2001) 703-711
2. Chapman H.A. Endosomal proteolysis and MHC class II function. Curr. Opin. Immunol. 10 (1998) 93-102
3. Carrodeguas L., Orosz C.G., Waldman W.J., Sedmak D.D., Adams P.W., and VanBuskirk A.M. Trans vivo analysis of human delayed-type hypersensitivity reactivity. Hum. Immunol. 60 (1999) 640-651
4. Cywin C.L., Firestone R.A., McNeil D.W., Grygon C.A., Crane K.M., White D.M., Kinkade P.R., Hopkins J.L., Davidson W., Labadia M.E., Wildeson J., Morelock M.M., Peterson J.D., Raymond E.L., Brown M.L., and Spero D.M. The design of potent hydrazones and disulfides as cathepsin S inhibitors. Bioorg. Med. Chem. 11 (2003) 1-8
5. Driessen C., Bryant R.A.R., Lennon-Dumenil A.-M., Villadangos J.A., Bryant P.W., Shi G.-P., Chapman H.A., and Ploegh H.L. Cathepsin S controls the trafficking and maturation of MHC class II molecules in dendritic cells. J. Cell Biol. 147 (1999) 775-790
6. Fiebiger E., Meraner P., Weber E., Fang I.F., Stingl G., Ploegh H., and Maurer D. Cytokines regulate proteolysis in major histocompatibility complex class II-dependent antigen presentation by dendritic cells. J. Exp. Med. 193 (2001) 881-892
7. Flannery T., Gibson D., Mirakhur M., McQuaid S., Greenan C., Trimble A., Walker B., McCormick D., and Johnston P.G. The clinical significance of cathepsin S expression in human astrocytomas. Am. J. Pathol. 163 (2003) 175-182
8. Gay S., Gay R.E., and Koopman W.J. Molecular and cellular mechanisms of joint destruction in rheumatoid arthritis-Two cellular mechanisms explain joint destruction. Ann. Rheum. Dis. 52 (1993) S39-S47
9. Lemere C.A., Munger J.S., Shi G.P., Natkin L., Haass C., Chapman H.A., and Selkoe D.J. The lysosomal cysteine protease, cathepsin S, is increased in Alzheimer's disease and Down-syndrome brain-an immunocytochemical study. Am. J. Pathol. 146 (1995) 848-860
10. Munger J.S., Haass C., Lemere C.A., Shi G.-P., Wong W.S.F., Teplow D.B., Selkoe D.J., and Chapman H.A. Lysosomal processing of amyloid precursor protein to A beta peptides: a distinct role for cathepsin S. Biochem. J. 311 (1995) 299-305
11. Nakagawa T.Y., and Rudensky A.Y. The role of lysosomal proteinases in MHC class II-mediated antigen processing and presentation. Immunol. Rev. 172 (1999) 121-129
12. Nakagawa T.Y., Brissette W.H., Lira P.D., Griffiths R.J., Petrushova N., Stock J., McNeish J.D., Eastman S.E., Howard E.D., Clarke S.R., Rosloniec E.F., Elliott E.A., and Rudensky A.Y. Impaired invariant chain degradation and antigen presentation and diminished collagen-induced arthritis in cathepsin S null mice. Immunity 10 (1999) 207-217
13. Noseworthy J.H., Lucchinetti C., Rodriguez M., and Weinshenker B.G. Multiple sclerosis. N. Engl. J. Med. 343 (2000) 938-952
14. Reddy V.Y., Zhang Q.Y., and Weiss S.J. Pericellular mobilization of the tissue-destructive cysteine proteinases, cathepsin B, cathepsin L and cathepsin S, by human monocyte-derived macrophages. Proc. Natl. Acad. Sci. U. S. A. 92 (1995) 3849-3853
15. Riese R.J., Wolf P.R., Brömme D., Natkin L.R., Villadangos J.A., Ploegh H.L., and Chapman H.A. Essential role for cathepsin S in MHC class II-associated invariant chain processing and peptide loading. Immunity 4 (1996) 357-366
16. Saegusa K., Ishimaru N., Yanagi K., Arakaki R., Ogawa K., Saito I., Katunuma N., and Hayashi Y. Cathepsin S inhibitor prevents autoantigen presentation and autoimmunity. J. Clin. Invest. 110 (2002) 361-369
17. Shi G.-P., Munger J.S., Meara J.P., Rich D.H., and Chapman H.A. Molecular cloning and expression of human alveolar macrophage cathepsin S, an elastinolytic cysteine protease. J. Biol. Chem. 267 (1992) 7258-7262
18. Shi G.-P., Webb A.C., Foster K.E., Knoll J.H., Lemere C.A., Munger J.S., and Chapman H.A. Human cathepsin S: chromosomal localization, gene structure, and tissue distribution. J. Biol. Chem. 269 (1994) 11530-11536
19. Shi G.-P., Villadangos J.A., Dranoff G., Small C., Gu L., Haley K.J., Riese R., Ploegh H.L., and Chapman H.A. Cathepsin S required for normal MHC class II peptide loading and germinal center development. Immunity 10 (1999) 197-206
20. Shi G.-P., Sukhova G.K., Kuzuya M., Ye Q., Du J., Zhang Y., Pan J._H., Lu M.L., Cheng X.W., Iguchi A., Perrey S., Lee A.M._E., Chapman H.A., and Libby P. Deficiency of the cysteine protease cathepsin S impairs microvessel growth. Circ. Res. 92 (2003) 493-500
21. Sukhova G.K., Shi G.P., Simon D.I., Chapman H.A., and Libby P. Expression of the elastolytic cathepsins S and K in human atheroma and regulation of their production in smooth muscle cells. J. Clin. Invest. 102 (1998) 576-583
22. Sukhova G.K., Zhang Y., Pan J.-H., Wada Y., Yamamoto T., Naito M., Kodama T., Tsimikas S., Witztum J.L., Lu M.L., Sakara Y., Chin M.T., Libby P., and Shi G.-P. Deficiency of cathepsin S reduces atherosclerosis in LDL receptor-deficient mice. J. Clin. Invest. 111 (2003) 897-906
23. Thurmond R.L., Sun S., Sehon C.A., Baker S.M., Cai H., Gu Y., Jiang W., Riley J.P., Williams K.N., Edwards J.P., and Karlsson L. Identification of a potent and selective noncovalent cathepsin S inhibitor. J. Pharmacol. Exp. Therap. 308 (2004) 268-276
24. Villadangos J.A., and Ploegh H.L. Proteolysis in MHC class II antigen presentation: who's in charge?. Immunity 12 (2000) 233-239
25. Villadangos J.A., Riese R.J., Peters C., Chapman H.A., and Ploegh H.L. Degradation of mouse invariant chain: roles of cathepsins S and D and the influence of major histocompatibility complex polymorphism. J. Exp. Med. 186 (1997) 549-560
26. Villadangos J.A., Bryant R.A., Deussing J., Driessen C., Lennon-Dumenil A.M., Riese R.J., Roth W., Saftig P., Shi G.P., Chapman H.A., Peters C., and Ploegh H.L. Proteases involved in MHC class II antigen presentation. Immunol. Rev. 172 (1999) 109-120
27. Ward Y.D., Thomson D.S., Frye L.L., Cywin C.L., Morwick T., Emmanuel M.J., Zindell R., McNeil D., Bekkali Y., Girardot M., Hrapchak M., DeTuri M., Crane K., White D., Pav S., Wang Y., Hao M.H., Grygon C.A., Labadia M.E., Freeman D.M., Davidson W., Hopkins J.L., Brown M.L., and Spero D.M. Design and synthesis of dipeptide nitriles as reversible and potent cathepsin S inhibitors. J. Med. Chem. 45 (2002) 5471-5482
28. Wiendl H., Lautwein A., Mitsdorffer M., Krause S., Erfurth S., Wienhold W., Morgalla M., Weber E., Overkleeft H.S., Lochmuller H., Melms A., Tolosa E., and Driessen C. Antigen processing and presentation in human muscle: cathepsin S is critical for MHC class II expression and upregulated in inflammatory myopathies. J. Neuroimmunol. 138 (2003) 132-143