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8‐pCPT‐2′‐O‐Me‐cAMP‐AM: An Improved Epac‐Selective cAMP Analogue
Author(s) -
Vliem Marjolein J.,
Ponsioen Bas,
Schwede Frank,
Pannekoek WillemJan,
Riedl Jurgen,
Kooistra Matthijs R. H.,
Jalink Kees,
Genieser HansGottfried,
Bos Johannes L.,
Rehmann Holger
Publication year - 2008
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200800216
Subject(s) - second messenger system , protein kinase a , chemistry , nucleotide , potency , kinase , receptor , biochemistry , in vitro , gene
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.