8‐pCPT‐2′‐O‐Me‐cAMP‐AM: An Improved Epac‐Selective cAMP Analogue

Marjolein J. Vliem, Bas Ponsioen, Frank Schwede, Willem‐Jan Pannekoek, Jürgen Riedl, Matthijs R.H. Kooistra, Kees Jalink, Hans‐Gottfried Genieser, Johannes L. Bos, Holger Rehmann

ChemBioChem · 2008 · 116 citations · 6 references

Concepts

Abstract

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.

References

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