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Exploring the efficacy of small molecule inhibitors of AKAP‐PKA interactions
Author(s) -
Moutty Marie Christine,
Zühlke Kerstin,
Milic Jelena,
Tabor Vedrana,
Goncalves Andrey,
Noack Claudia,
Christian Frank,
Grossmann Solveig,
Kries Jens Peter,
Rosenthal Walter,
Klussmann Enno
Publication year - 2011
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.25.1_supplement.573.2
A‐kinase anchoring proteins (AKAPs) are a protein family with crucial functions in compartmentalized intracellular signalling pathways. They target other proteins including protein kinases, phosphatases and phosphodiesterases to defined locations in the cell and thereby locally restrict the corresponding enzymatic acitvities. A particular focus of our group is the elucidation of the role of AKAP‐PKA (cAMP‐dependent protein kinase A) interactions in the regulation of cardiac myocyte contractility and water reabsorption in collecting duct principal cells. Since these processes are connected to cardiovasular diseases we are are validating AKAP‐PKA interactions as potential drug targets. The specific disruption of AKAP‐PKA interactions with small molecule inhibitors may lead to a new concept in the treatment of chronic heart failure. This work was supported by grants from the Deutsche Forschungsgemeinschaft (Kl1415/4‐2) and the GoBio program of the Bundesministerium für Bildung und Forschung (FKZ 0315516).