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Abstract for Homogenous Luminescent HTS-formatted Technologies
for cAMP- and cGMP-Dependent Phosphodiesterases
Said A Goueli1,2, Kevin Hsiao1, Marina Zdanovskaia1, and Jolanta
Vidugiriene1
1Promega Corporation Madison, WI
2University of Wisconsin School of Medicine and Public
Health, Madison, WI
Cyclic nucleotide phosphodiesterases (PDEs) comprise eleven
different gene families of enzymes that are encoded by at least 21
different genes and accounting for at least 55 isoforms. They have
been implicated in controlling specific cellular functions including
cardiovascular, pulmonary, and inflammatory diseases and they play
potential role as targets for treatment of cancer and some
other diseases. Inhibition of PDEs was shown to induce chronic
lymphocytic leukemia (CLL) apoptosis and more evidence support
targeting PDEs for treatments of several types of cancer. Thus, the
development of novel isoform-specific inhibitors may be useful for
the development of therapeutic agents against cancer. We have
development a homogenous PDE-Glo™ Phosphodiesterase Assay for
high-throughput screening (HTS) for novel inhibitors of PDE. The HTS
formatted assays can be used to monitor the activity of cAMP-PDEs
and cGMPPDEs and can be carried out in two simple steps in 96-,
384-, or 1536-well formatted plates. The Assay is luminescent and
thus it encounters minimal interference from fluorescent compounds
and the robustness of the assays are indicated by their remarkably
high Z´ value (>0.8). In summary, the PDE-Glo luminescent assay can
be used for screening libraries of compounds targeting in PDEs that
might be developed into potential drugs for treatment of cancer and
some other diseases. |
