Publication | Closed Access
8‐pCPT‐2′‐O‐Me‐cAMP‐AM: An Improved Epac‐Selective cAMP Analogue
115
Citations
6
References
2008
Year
Biological CharacterisationMolecular BiologyOrganic ChemistryPeptide ScienceChemistryChemical BiologyCellular PhysiologyMolecular PharmacologyHigh PotencyReceptor Tyrosine KinaseCell SignalingMolecular PhysiologyBiochemistryEpac-selective PrecursorG Protein-coupled ReceptorIon ChannelsNon-peptide LigandProtein PhosphorylationSignal TransductionNatural SciencesPeptide LibraryPeptide TherapeuticMedicine
An Epac-selective precursor with high potency: Signalling by the second messenger cAMP is mediated by its receptor proteins protein kinase A (PKA), Epac and cyclic-nucleotide-regulated ion channels. This manuscript describes the synthesis and biological characterisation of a precursor that selectively activates Epac and that is 100 to 1000 times more efficient under biological conditions than the parental compound.
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