Combinatorial chemistry as a new approach in antiparasitic drug discovery

Parasitology Research

Volumn 90, Issue SUPPL. 2, 2003, Pages

  Link, Andreas ^a  

^a PHILIPPS UNIVERSITY MARBURG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIPARASITIC AGENT; ANTIPROTOZOAL AGENT; RECOMBINANT ENZYME;

COMBINATORIAL CHEMISTRY; DRUG POTENCY; DRUG PURIFICATION; DRUG SCREENING; DRUG SYNTHESIS; ENZYME INHIBITION; GIARDIA LAMBLIA; LEISHMANIA MEXICANA; NONHUMAN; PLASMODIUM FALCIPARUM; PRIORITY JOURNAL; REVIEW; TRYPANOSOMA BRUCEI; TRYPANOSOMA CRUZI; X RAY CRYSTALLOGRAPHY;

GIARDIA; GIARDIA INTESTINALIS; LEISHMANIA MEXICANA; PLASMODIUM FALCIPARUM; TRYPANOSOMA; TRYPANOSOMA BRUCEI; TRYPANOSOMA CRUZI;

EID: 0037625384     PISSN: 09320113     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00436-002-0772-7     Document Type: Review

References (21)

1. Aronov AM, Munagala NR, Kuntz ID, Wang CC (2001) Virtual screening of combinatorial libraries across a gene family: in search of inhibitors of Giardia lamblia guanine phosphoribo-syltransferase. Antimicrob Agents Chemother 45:2571-2576
2. Backes BJ, Virgilio AA, Ellman JA (1996) Activation method to prepare a highly reactive acylsulfonamide "safety-catch" linker for solid-phase synthesis. J Am Chem Soc 118:3055-3056
3. Bressi JC, Verlinde CL, Aronov AM, Shaw ML, Shin SS, Nguyen LN, Suresh S, Buckner FS, Van Voorhis WC, Kuntz ID, Hol WG, Gelb MH (2001) Adenosine analogues as selective inhibitors of glyceraldehyde-3-phosphate dehydrogenase of Trypanosomatidae via structure-based drug design. J Med Chem 44:2080-2093
4. Carroll CD, Patel H, Johnson TO, Guo T, Orlowski M, He ZM, Cavallaro CL, Guo J, Oksman A, Gluzman IY, Connelly J, Chelsky D, Goldberg DE, Dolle RE (1998) Identification of potent inhibitors of Plasmodium falciparum plasmepsin 11 from an encoded statine combinatorial library. Bioorg Med Chem Lett 8:2315-2320
5. +-binding sites of parasite enzymes. J Comb Chem 2:537-544
6. Golisade A, Herforth C, Quirijnen L, Maes L, Link A (2002) Improving an antitrypanosomal lead applying nucleophilic substitution on a safety catch linker. Bioorg Med Chem 10:159-165
7. Huang L, Lee A, Ellman JA (2002) Identification of potent and selective mechanism-based inhibitors of the cysteine protease cruzain using solid-phase parallel synthesis. J Med Chem 45:676-684
8. Kehoe JW, Maly DJ, Verdugo DE, Armstrong JI, Cook BN, Ouyang YB, Moore KL, Ellman JA, Bertozzi CR (2002) Tyrosylprotein sulfotransferase inhibitors generated by combinatorial target-guided ligand assembly. Bioorg Med Chem Lett 12:329-332
9. + analogue is a nanomolar inhibitor of trypanosomal glyceraldehyde-3-phosphate dehydrogenase. Bioorg Med Chem Lett 11:95-98
10. Lipinski C, Lombardo F, Dominy B, Feeney P (1997) Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev 46:3-25
11. McGovern SL, Caselli E, Grigorieff N, Shoichet BK (2002) A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening. J Med Chem 45:1712-1722
12. Otto S, Furlan RL, Sanders JK (2002) Dynamic combinatorial chemistry. Drug Discov Today 7:117-125
13. Pitcovsky TA, Mucci J, Alvarez P, Leguizamon MS, Burrone O, Alzari PM, Campetella O (2001) Epitope mapping of transsialidase from Trypanosoma cruzi reveals the presence of several cross-reactive determinants. Infect Immun 69:1869-1875
14. Reents R, Jeyaraj DA, Waldmann H (2002) Enzymatically cleavable linker groups in polymer-supported synthesis. Drug Discov Today 7:71-76
15. Ring CS, Sun E, McKerrow JH, Lee GK, Rosenthal PJ, Kuntz ID, Cohen FE (1993) Structure-based inhibitor design by using protein models for the development of antiparasitic agents. Proc Natl Acad Sci U S A 90:3583-3587
16. Roche O, Schneider P, Zuegge J, Guba W, Kansy M, Alanine A, Bleicher K, Danel F, Gutknecht EM, Rogers-Evans M, Neidhart W, Stalder H, Dillon M, Sjogren E, Fotouhi N, Gillespie P, Goodnow R, Harris W, Jones P, Taniguchi M, Tsujii S, von der Saal W, Zimmermann G, Schneider G (2002) Development of a virtual screening method for identification of "frequent hitters" in compound libraries. J Med Chem 45:137-142
17. Scharn D, Wenschuh H, Reineke U, Schneider-Mergener J, Germeroth L (2000) Spatially addressed synthesis of amino- and amino-oxy-substituted 1, 3,5-triazine arrays on polymeric membranes. J Comb Chem 2:361-369
18. Smith HK, Bradley M (1999) Comparison of resin and solution screening methodologies in combinatorial chemistry and the identification of a 100 nM inhibitor of trypanothione reductase. J Comb Chem 1:326-332
19. St Hilaire PM, Alves LC, Sanderson SJ, Mottram JC, Juliano MA, Juliano L, Coombs GH, Meldal M (2000) The substrate specificity of a recombinant cysteine protease from Leishmania mexicana: application of a combinatorial peptide library approach. Chembiochem 1:115-122
20. Suresh S, Bressi JC, Kennedy KJ, Verlinde CL, Gelb MH, Hol WG (2001) Conformational changes in Leishmania mexicana glyceraldehyde-3-phosphate dehydrogenase induced by designed inhibitors. J Mol Biol 309:423-435
21. Verlinde CL, Callens M, Van Calenbergh S, Van Aerschot A, Herdewijn P, Hannaert V, Michels PA, Opperdoes FR, Hol WG (1994) Selective inhibition of trypanosomal glyceraldehyde-3-phosphate dehydrogenase by protein structure-based design: toward new drugs for the treatment of sleeping sickness. J Med Chem 37:3605-3613