Klin Padiatr 2019; 231(03): 159-160
DOI: 10.1055/s-0039-1687132
Abstracts
Georg Thieme Verlag KG Stuttgart · New York

Screening assay to identify potential Taspase1 inhibitors

V Luciano
1   Institute of Pharmaceutical Biology/DCAL, Goethe-University of Frankfurt, Biocenter, Max-von-Laue-Str. 9, D-60438 Frankfurt/Main, Germany
,
J Heering
2   Institute of Pharmaceutical Chemistry, Goethe-University of Frankfurt, Biocenter, Max-von-Laue-Str. 9, D-60438 Frankfurt/Main, Germany
,
E Proschak
2   Institute of Pharmaceutical Chemistry, Goethe-University of Frankfurt, Biocenter, Max-von-Laue-Str. 9, D-60438 Frankfurt/Main, Germany
,
R Marschalek
1   Institute of Pharmaceutical Biology/DCAL, Goethe-University of Frankfurt, Biocenter, Max-von-Laue-Str. 9, D-60438 Frankfurt/Main, Germany
› Institutsangaben
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Publikationsdatum:
20. Mai 2019 (online)

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Introduction:

Taspase1 is necessary to process the MLL protein and the oncogenic AF4-MLL fusions protein. In order to activate Taspase1, two proenzymes have to form a homodimer which causes an autoprotolytical activation. Unfortunately, Taspase1 is no classical "enzyme" rather than a "single action protein".

Methods:

A special HTRF-assay has been designed in combination with special Taspase1 mutants as read-out system to monitor Taspase1 activity over longer time periods (up to 48h). In addition, we also established a cell-free system to measure Taspase1 activity.

Results & Conclusion:

The developed screening assays allow to perform high-throughput screens to identify potential inhibitors for the treatment of t(4;11) leukemia patients.