Literature DB >> 12734752

Combinatorial chemistry as a new approach in antiparasitic drug discovery.

Andreas Link1.   

Abstract

Key challenges in antiparasitic drug discovery are target selection and identification of appropriate small molecules as potential ligands for these targets. Novel tools and techniques continue to be developed to address both of these problems. This report focuses on the application of a suite of technologies summarized as combinatorial chemistry. Recent success using these technologies is explored, reasons for frequent failure are given and discussed.

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Year:  2003        PMID: 12734752     DOI: 10.1007/s00436-002-0772-7

Source DB:  PubMed          Journal:  Parasitol Res        ISSN: 0932-0113            Impact factor:   2.289


  20 in total

1.  Comparison of resin and solution screening methodologies in combinatorial chemistry and the identification of a 100 nM inhibitor of trypanothione reductase.

Authors:  H K Smith; M Bradley
Journal:  J Comb Chem       Date:  1999 Jul-Aug

2.  Tyrosylprotein sulfotransferase inhibitors generated by combinatorial target-guided ligand assembly.

Authors:  John W Kehoe; Dustin J Maly; Dawn E Verdugo; Joshua I Armstrong; Brian N Cook; Ying-Bin Ouyang; Kevin L Moore; Jonathan A Ellman; Carolyn R Bertozzi
Journal:  Bioorg Med Chem Lett       Date:  2002-02-11       Impact factor: 2.823

3.  Development of a virtual screening method for identification of "frequent hitters" in compound libraries.

Authors:  Olivier Roche; Petra Schneider; Jochen Zuegge; Wolfgang Guba; Manfred Kansy; Alexander Alanine; Konrad Bleicher; Franck Danel; Eva-Maria Gutknecht; Mark Rogers-Evans; Werner Neidhart; Henri Stalder; Michael Dillon; Eric Sjögren; Nader Fotouhi; Paul Gillespie; Robert Goodnow; William Harris; Phil Jones; Mikio Taniguchi; Shinji Tsujii; Wolfgang von der Saal; Gerd Zimmermann; Gisbert Schneider
Journal:  J Med Chem       Date:  2002-01-03       Impact factor: 7.446

4.  A common mechanism underlying promiscuous inhibitors from virtual and high-throughput screening.

Authors:  Susan L McGovern; Emilia Caselli; Nikolaus Grigorieff; Brian K Shoichet
Journal:  J Med Chem       Date:  2002-04-11       Impact factor: 7.446

5.  Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library.

Authors:  C D Carroll; H Patel; T O Johnson; T Guo; M Orlowski; Z M He; C L Cavallaro; J Guo; A Oksman; I Y Gluzman; J Connelly; D Chelsky; D E Goldberg; R E Dolle
Journal:  Bioorg Med Chem Lett       Date:  1998-09-08       Impact factor: 2.823

6.  The substrate specificity of a recombinant cysteine protease from Leishmania mexicana: application of a combinatorial peptide library approach.

Authors:  P M St Hilaire; L C Alves; S J Sanderson; J C Mottram; M A Juliano; L Juliano; G H Coombs; M Meldal
Journal:  Chembiochem       Date:  2000-08-18       Impact factor: 3.164

7.  Adenosine analogues as selective inhibitors of glyceraldehyde-3-phosphate dehydrogenase of Trypanosomatidae via structure-based drug design.

Authors:  J C Bressi; C L Verlinde; A M Aronov; M L Shaw; S S Shin; L N Nguyen; S Suresh; F S Buckner; W C Van Voorhis; I D Kuntz; W G Hol; M H Gelb
Journal:  J Med Chem       Date:  2001-06-21       Impact factor: 7.446

8.  Conformational changes in Leishmania mexicana glyceraldehyde-3-phosphate dehydrogenase induced by designed inhibitors.

Authors:  S Suresh; J C Bressi; K J Kennedy; C L Verlinde; M H Gelb; W G Hol
Journal:  J Mol Biol       Date:  2001-06-01       Impact factor: 5.469

9.  Spatially addressed synthesis of amino- and amino-oxy-substituted 1, 3,5-triazine arrays on polymeric membranes.

Authors:  D Scharn; H Wenschuh; U Reineke; J Schneider-Mergener; L Germeroth
Journal:  J Comb Chem       Date:  2000 Jul-Aug

10.  Selective inhibition of trypanosomal glyceraldehyde-3-phosphate dehydrogenase by protein structure-based design: toward new drugs for the treatment of sleeping sickness.

Authors:  C L Verlinde; M Callens; S Van Calenbergh; A Van Aerschot; P Herdewijn; V Hannaert; P A Michels; F R Opperdoes; W G Hol
Journal:  J Med Chem       Date:  1994-10-14       Impact factor: 7.446

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