Selective Inhibition of Trypanosomal Glyceraldehyde-3-phosphate Dehydrogenase by Protein Structure-Based Design: Toward New Drugs for the Treatment of Sleeping Sickness

Within the framework of a project aimed at rational design of drugs against diseases caused by trypanosomes and related hemoflagellate parasites, selective inhibitors of trypanosomal glycolysis were designed, synthesized, and tested. The design was based upon the crystallographically determined stru...

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Veröffentlicht in:	Journal of medicinal chemistry 1994-10, Vol.37 (21), p.3605-3613
Hauptverfasser:	Verlinde, Christophe L. M. J, Callens, Mia, Van Calenbergh, Serge, Van Aerschot, Arthur, Herdewijn, Piet, Hannaert, Veronique, Michels, Paul A. M, Opperdoes, Fred R, Hol, Wim G. J
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine - chemistry Adenosine - pharmacology Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antiparasitic agents Binding Sites Biological and medical sciences Deoxyadenosines - chemical synthesis Deoxyadenosines - pharmacology Drug Design Glyceraldehyde-3-Phosphate Dehydrogenases - antagonists & inhibitors Glyceraldehyde-3-Phosphate Dehydrogenases - chemistry Humans Hydrogen Bonding Leishmania mexicana - enzymology Medical sciences Molecular Structure NAD - chemistry NAD - metabolism Pharmacology. Drug treatments Protein Conformation Structure-Activity Relationship Trypanosoma brucei brucei - enzymology Trypanosomiasis, African - drug therapy
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