Improved trypanocidal activities of cathepsin L inhibitors

International Journal of Antimicrobial Agents

Volumn 22, Issue 2, 2003, Pages 155-159

  Nkemngu, Njinkeng Joseph ^a   Grande, Rachel ^b   Hansell, Elizabeth ^b   McKerrow, James H ^b   Caffrey, Conor R ^b   Steverding, Dietmar ^a,c  

^a UNIVERSITY OF HEIDELBERG   (Germany)

^b UNIVERSITY OF CALIFORNIA   (United States)

^c UNIVERSITY OF BRISTOL   (United Kingdom)

Author keywords

Cathepsin L inhibitors; Cysteine proteinase; Sleeping sickness; Trypanosoma brucei brucei; Trypanosoma brucei rhodesiense

Indexed keywords

1 NAPHTHALENYLSULFONYLISOLEUCYLTRYPTOPHANAL; BRUCIPAIN; CATHEPSIN L; CATHEPSIN L INHIBITOR; CYSTEINE PROTEINASE INHIBITOR; DIMINAZENE ACETURATE; MICROBIAL ENZYME; N BENZYLOXYCARBONYLPHENYLALANYL TERT BUTYLTYROSYLDIAZOMETHYLKETONE; N BENZYLOXYCARBONYLPHENYLALANYLALANYLDIAZOMETHYLKETONE; N BEZYLOXYCARBONYLPHENYLALANYLTRYROSINAL; RECOMBINANT ENZYME; RHODESAIN; SURAMIN; UNCLASSIFIED DRUG;

AFRICAN TRYPANOSOMIASIS; ANTIPROTOZOAL ACTIVITY; ARTICLE; BLOOD; CONTROLLED STUDY; DRUG POTENCY; DRUG SELECTIVITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; IN VITRO STUDY; LYSOSOME; NONHUMAN; PRIORITY JOURNAL; PROTEIN DEGRADATION; PROTEIN PURIFICATION; TRYPANOSOMA BRUCEI;

EID: 0042090138     PISSN: 09248579     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0924-8579(03)00096-7     Document Type: Article

References (31)

1. WHO. African trypanosomiasis or sleeping sickness. World Health Org. Fact Sheet 2001;259 ( http://www.who.int/inf-fs/en/fact259.html ).
2. Kristjanson P.M., Swallow B.M., Rowlands G.J., Kruska R.L., de Leeuw P.N. Measuring the costs of African animal trypanosomosis, the potential benefits of control and returns to research. Agric. Syst. 59:1999;79-98.
3. Croft S.L. The current status of antiparasitic chemotherapy. Parasitology. 114:(Suppl.):1997;S3-S15.
4. Geerts S., Holmes P.H., Diall O., Eisler M.C. African bovine trypanosomiasis: the problem of drug resistance. Trends Parasitol. 17:2001;25-28.
5. Matovu E., Seebeck T., Enyaru J.C.K., Kaminsky R. Drug resistance in Trypanosoma brucei ssp., the causative agents of sleeping sickness in man and nagana in cattle. Microbes Infect. 3:2001;763-770.
6. McKerrow J.H., Engel J.C., Caffrey C.R. Cysteine protease inhibitors as chemotherapy for parasitic infections. Bioorg. Med. Chem. 7:1999;639-644.
7. Caffrey C.R., Scory S., Steverding D. Cysteine proteinase of trypanosome parasites: novel targets for chemotherapy. Curr. Drug Targets. 1:2000;155-162.
8. Caffrey C.R., Hansell E., Lucas K.D., et al. Active site mapping, biochemical properties and subcellular localization of rhodesain, the major cysteine protease of Trypanosoma brucei rhodesiense. Mol. Biochem. Parasitol. 118:2001;61-73.
9. Lonsdale-Eccles J.D., Grab D.J. Lysosomal and non-lysosomal peptidyl hydrolases of the bloodstream forms of Trypanosoma brucei brucei. Eur. J. Biochem. 169:1987;467-475.
10. Authié E. Trypanosomiasis and trypanotolerance in cattle: a role for congopain. Parasitol. Today. 10:1994;360-364.
11. Troeberg L., Pike R.N., Morty R.E., Berry R.K., Coetzer T.H.T., Lonsdale-Eccles J.D. Proteases from Trypanosoma brucei brucei. Purification, characterisation and interactions with host regulatory molecules. Eur. J. Biochem. 238:1996;728-736.
12. 2. Exp. Parasitol. 91:1999;327-333.
13. Troeberg L., Morty R.E., Pike R.N., et al. Cysteine proteinase inhibitors kill cultured bloodstream forms of Trypanosoma brucei brucei. Exp. Parasitol. 91:1999;349-355.
14. Eakin A.E., Mills A.A., Harth G., McKerrow J.H., Craik C.S. The sequence, organization, and expression of the major cysteine protease (cruzain) from Trypanosoma cruzi. J. Biol. Chem. 267:1992;7411-7420.
15. Hirumi H., Hirumi K., Doyle J.J., Cross G.A.M. In vitro cloning of animal-infective bloodstream forms of Trypanosoma brucei. Parasitology. 80:1980;371-382.
16. Baltz T., Baltz D., Giroud C., Crockett J. Cultivation in a semi-defined medium of animal infective forms of Trypanosoma brucei, T. equiperdum, T. evansi, T. rhodesiense and T. gambiense. EMBO J. 4:1985;1273-1277.
17. Merschjohann K., Sporer F., Steverding D., Wink M. In vitro effect of alkaloids on bloodstream forms of Trypanosoma brucei and T. congolense. Planta Med. 67:2001;623-627.
18. 50 in studies of drug resistance of malaria parasites. Acta Trop. 55:1993;257-261.
19. Rodriguez J., Deinhardt F. Preparation of a semipermanent mounting medium for fluorescent antibody studies. Virology. 12:1960;316-317.
20. Woo J.-T., Sigeizumi S., Yamaguchi K., et al. Peptidyl aldehyde derivatives as potent and selective inhibitors of cathepsin L. Biorg. Med. Chem. Lett. 5:1995;1501-1504.
21. Shaw E., Mohanty S., Colic A., Stoka V., Turk V. The affinity-labelling of cathepsin S with peptidyl diazomethyl ketones. Comparison with the inhibition of cathepsin L and calpain. FEBS Lett. 334:1993;340-342.
22. Yasuma T., Oi S., Choh N., et al. Synthesis of peptide aldehyde derivatives as selective inhibitors of human cathepsin L and their inhibitory effect on bone resorption. J. Med. Chem. 41:1998;4301-4308.
23. Grab D.J., Wells C.W., Shaw M.K., Webster P., Russo D.C.W. Endocytosed transferrin in African trypanosomes is delivered to lysosomes and may not be recycled. Eur. J. Cell Biol. 59:1992;398-404.
24. Steverding D., Stierhof Y.-D., Fuchs H., Tauber R., Overath P. Transferrin-binding protein complex is the receptor for transferrin uptake in Trypanosoma brucei. J. Cell. Biol. 131:1995;1173-1182.
25. Kabiri M., Steverding D. Trypanosoma evansi: demonstration of a transferrin receptor derived from expression site-associated genes 6 and 7. J. Parasitol. 87:2001;1189-1191.
26. Robertson C.D., North M.J., Lockwood B.C., Coombs G.H. Analysis of the proteinase of Trypanosoma brucei. J. Gen. Microbiol. 136:1990;921-925.
27. Schechter I., Berger A. On the size of the active site in proteases. I. Papain. Biochem. Biophys. Res. Commun. 27:1967;157-162.
28. Caffrey C.R., Schanz M., Nkemgu-Njinkeng J., et al. Screening of acyl hydrazide proteinase inhibitors for antiparasitic activity against Trypanosoma brucei. Int. J. Antimicrob. Agents. 19:2002;227-231.
29. Hanzlik R.P., Thompson S.A. Vinylogous amino acid esters: a new class of inactivators for thiol proteases. J. Med. Chem. 27:1984;711-712.
30. Palmer J.T., Rasnick D., Klaus J.L., Brömme D. Vinyl sulfones as mechanism-based cysteine protease inhibitors. J. Med. Chem. 38:1995;3193-3196.
31. Engel J.C., Doyle P.S., Hsieh I., McKerrow J.H. Cysteine protease inhibitors cure an experimental Trypanosoma cruzi infection. J. Exp. Med. 188:1998;725-734.