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Highly functionalized terpyridines as competitive inhibitors of AKAP-PKA interactions

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Item Type:Article
Title:Highly functionalized terpyridines as competitive inhibitors of AKAP-PKA interactions
Creators: Schäfer, G., Milić, J, Eldahshan, A, Götz, F., Zühlke, K., Schillinger, C., Kreuchwig, A., Elkins, J.M., Abdul Azeez, K.R.A., Oder, A., Moutty, M.C., Masada, N., Beerbaum, M., Schlegel, B., Niquet, S., Schmieder, P. ORCID logoORCID: https://orcid.org/0000-0001-9968-9327, Krause, G., von Kries, J.P. ORCID logoORCID: https://orcid.org/0000-0003-4716-4988, Cooper, D.M.F., Knapp, S., Rademann, J. ORCID logoORCID: https://orcid.org/0000-0001-6678-3165, Rosenthal, W. and Klussmann, E. ORCID logoORCID: https://orcid.org/0000-0003-4004-5003
Abstract:A good fit: Interactions between A-kinase anchoring proteins (AKAPs) and protein kinase A (PKA) play key roles in a plethora of physiologically relevant processes whose dysregulation causes or is associated with diseases such as heart failure. Terpyridines have been developed as α-helix mimetics for the inhibition of such interactions and are the first biologically active, nonpeptidic compounds that block the AKAP binding site of PKA.
Keywords:AKAP, Peptide Mimetics, Protein Kinase A, Protein-Protein Interactions, Suzuki Coupling, Terpyridines
Source:Angewandte Chemie International Edition
ISSN:1433-7851
Publisher:Wiley
Volume:52
Number:46
Page Range:12187-12191
Date:11 November 2013
Official Publication:https://doi.org/10.1002/anie.201304686
PubMed:View item in PubMed

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