Plasmodium falciparum GAPDH als Zielstruktur bei der Medikamentenentwicklung

• Forschungsstelle: TPH
• Projektnummer: 2.03
• Projekttitel Englisch: Plasmodium falciparum GAPDH as a malaria drug target

Schlüsselwörter (Englisch)

Malaria, drug development, high-througput screening, GAPDH

Kurzbeschreibung (Englisch)

Cloning and expression of Plasmodium falciparum glyceraldehyde-3-phosphate dehydrogenase (pfGAPDH) in enzymatically active form in E. coli has enabled us to investigate the functional role of this enzyme in the malaria parasite and to perform a high-throughput screening for inhibitors of its enzymatic activity. Several hundred primary hits were selected for further analysis.

Projektziele (Englisch)

Goal of the next project phase is to profile primary hits identified by screening of a library of more than 400'000 compounds for pfGAPDH inhibitors and to identify a drug development candidate among them. An enlarged project team will then propose a multidimensional lead optimization program with the final goal of developing a new anti-malarial drug suitable for therapy and/or prophylaxis.

Publikationen / Ergebnisse (Englisch)

Identification and recombinant expression of glyceraldehyde-3-phosphate dehydrogenase of Plasmodium falciparum. Daubenberger, C. A., Pöltl-Frank, F., Jiang, G., Lipp, H.-J., Certa, U., and Pluschke, G., Gene, 246, 255 (2000)