Abstract
Results In our reporter cell lines, receptor guanylyl cyclase activity can be monitored in real-time via aequorin luminescence stimulated by calcium influx through the CNG channel. By using different natural as well as synthetic receptor ligands of the natriuretic and guanylin peptide families, we could show that our reporter assay monitors guanylyl cyclase activity with unrivalled high sensitivity. Receptor antagonists were also tested and, unexpectedly, were characterized as partial agonists.
Highlights
Particulate guanylyl cyclases are implicated in a growing number of pathophysiologies and, represent an important target class for drug development
4th International Conference of cGMP Generators, Effectors and Therapeutic Implications Meeting abstracts – A single PDF containing all abstracts in this Supplement is available here. http://www.biomedcentral.com/content/pdf/1471-2210-9-S1-info.pdf
We report here the generation and pharmacological characterization of three receptor guanylyl cyclase reporter cell lines
Summary
Pharmacological characterization of receptor guanylyl cyclase reporter cell lines. Address: Molecular Screening Technology, Bayer Schering Pharma AG, Aprather Weg 18a, D-42096 Wuppertal, Germany. Published: 11 August 2009 BMC Pharmacology 2009, 9(Suppl 1):P73 doi:10.1186/1471-2210-9-S1-P73. 4th International Conference of cGMP Generators, Effectors and Therapeutic Implications Meeting abstracts – A single PDF containing all abstracts in this Supplement is available here. http://www.biomedcentral.com/content/pdf/1471-2210-9-S1-info.pdf
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