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Journal of Biomolecular Screening
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Application of the BD ACTOneTM Technology for the High-Throughput Screening of Gs-Coupled Receptor Antagonists

András Visegrády

Lead Discovery Unit, visegrady{at}richter.hu

András Boros

Pharmacological and Drug Safety Research, Gedeon Richter Plc, Budapest, Hungary

Zsolt Némethy

Pharmacological and Drug Safety Research, Gedeon Richter Plc, Budapest, Hungary

Béla Kiss

Pharmacological and Drug Safety Research, Gedeon Richter Plc, Budapest, Hungary

György M. Keseru

Lead Discovery Unit

A novel technology for monitoring the changes of 3,'5'-adenosine cyclic monophosphate (cAMP) in live cells suitable for drug screening relies on the use of cyclic nucleotide-gated channels as biosensors coexpressed with the appropriate target receptor. The technique (termed BD ACTOneTM) offers measurement of cAMP-dependent calcium influx or membrane depolarization with conventional fluorescent methods both in kinetic and in endpoint modes, optimal for high-throughput and subsequent compound screening. The utility of the technique is reported here based on assay development and high-throughput screening for small-molecule antagonists of the peptide parathyroid hormone 2 receptor (PTH2R). The dual-signaling properties of the receptor were retained in the recombinant system, and the observed pharmacological profile corresponded to data from radiolabeled cAMP determination. The membrane-potential-based high-throughput assay produced reproducible actives and led to the identification of several chemical scaffolds with potential utility as PTH2R ligands. (Journal of Biomolecular Screening 2007:1068-1073)

Key Words: cyclic nucleotide-gated channel • high-throughput screening • cAMP • G-protein-coupled receptor • peptide parathyroid hormone 2 receptor

Journal of Biomolecular Screening, Vol. 12, No. 8, 1068-1073 (2007)
DOI: 10.1177/1087057107309035
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