By a News Reporter-Staff News Editor at Drug Week -- Investigators discuss new findings in Biomolecular Screening. According to news reporting originating from Gottingen, Germany, by NewsRx correspondents, research stated, "Protein phosphatases (PP) are interesting drug targets. However, their ubiquitous presence and involvement in different, partially opposing signal pathways suggest that specificity may be achieved rather by targeting their interaction with subunits determining substrate specificity than the enzyme itself."
Our news editors obtained a quote from the research from the University of Gottingen, "An interesting subunit is phosphatase inhibitor-1 (I-1), which, in its protein kinase A-phosphorylated form (I-1(P)), inhibits the catalytic subunit of type 1 phosphatase (PP1c). In the current study, we established a colorimetric and a fluorescence-based assay system for the identification of compounds interfering with the inhibitory effect of I-1(P) on PP1c. The fluorescence assay exhibited 500-fold higher sensitivity toward PP1c. A nine-residue peptide containing the PP1c-binding motif (RVxF) of I-1 stimulated PP1c activity in the presence of I-1(P) (EC50 27 mu M and 2.3 mu M in the colorimetric and fluorescence assay, respectively). This suggests that the peptide interfered with the inhibitory effect of I-1(P) on PP1c and represents a proof-of-principle. The calculated Z factor for PP1c (0.84) and the PP1c-I-1(P) complex (0.73) confirmed the suitability of the fluorescence assay for high-throughput screenings (HTS)."
According to the news editors, the research concluded: "By testing several thousand small molecules, we suggest the advantages of kinetic measurements over single-point measurements using the fluorescence-based assay in an HTS format."
For more information on this research see: Development of a Colorimetric and a Fluorescence Phosphatase-Inhibitor Assay Suitable for Drug Discovery Approaches. Journal of Biomolecular Screening, 2013;18(8):899-909. Journal of Biomolecular Screening can be contacted at: Sage Publications Inc, 2455 Teller Rd, Thousand Oaks, CA 91320, USA. (Sage Publications - www.sagepub.com/; Journal of Biomolecular Screening - jbx.sagepub.com)
The news editors report that additional information may be obtained by contacting H. Sotoud, University of Gottingen, Dept. of Pharmacol, Univ Med Center Goettingen, D-37073 Gottingen, Germany. Additional authors for this research include P. Gribbon, B. Ellinger, J. Reinshagen, P. Boknik, L. Kattner, A. El-Armouche and T. Eschenhagen (see also Biomolecular Screening).
Keywords for this news article include: Europe, Germany, Gottingen, Biomolecular Screening
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