Journal of Biomolecular Screening

 

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Journal of Biomolecular Screening, Vol. 9, No. 5, 434-438 (2004)
DOI: 10.1177/1087057104264031

Screening Assay for the Identification of Deoxyhypusine Synthase Inhibitors

Marc-Nicola Sommer

Axxima Pharmaceuticals AG, Max-Lebsche-Platz 32, D-81377 München, Germany

Dorian Bevec

Axxima Pharmaceuticals AG, Max-Lebsche-Platz 32, D-81377 München, Germany

Bert Klebl

Axxima Pharmaceuticals AG, Max-Lebsche-Platz 32, D-81377 München, Germany

Birgit Flicke

Axxima Pharmaceuticals AG, Max-Lebsche-Platz 32, D-81377 München, Germany

Kerstin Hölscher

Axxima Pharmaceuticals AG, Max-Lebsche-Platz 32, D-81377 München, Germany

Tatjana Freudenreich

Axxima Pharmaceuticals AG, Max-Lebsche-Platz 32, D-81377 München, Germany

Ilona Hauber

Heinrich-Pette-Institute for Experimental Virology and Immunology, Martinistrasse 52, D-20251 Hamburg, Germany

Joachim Hauber

Heinrich-Pette-Institute for Experimental Virology and Immunology, Martinistrasse 52, D-20251 Hamburg, Germany

Helmut Mett

Axxima Pharmaceuticals AG, Max-Lebsche-Platz 32, D-81377 München, Germany

The 1st step in the posttranslational hypusine [N{epsilon}-(4-amino-2-hydroxybutyl)lysine] modification of eukaryotic translation initiation factor 5A (eIF5A) is catalyzed by deoxyhypusine synthase (DHS). The eIF5A intermediate is subsequently hydroxylated by deoxyhypusine hydroxylase (DHH), thereby converting the eIF5A precursor into a biologically active protein. Depletion of eIF5A causes inhibition of cell growth, and the identification of eIF5A as a cofactor of the HIV Rev protein turns this host protein and therefore DHS into an interesting target for drugs against abnormal cell growth and/or HIV replication. The authors developed a 96-well format DHS assay applicable for the screening of DHS inhibitors. Using this assay, they demonstrate DHS inhibition by AXD455 (Semapimod, CNI-1493). This assay represents a powerful tool for the identification of new DHS inhibitors with potency against cancer and HIV.

Key Words: DHS • eIF5A • spermidine • 96-well • HIV


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