Highly Functionalized Terpyridines as Competitive Inhibitors of AKAP-PKA Interactions
نویسندگان
چکیده
منابع مشابه
Highly Functionalized Terpyridines as Competitive Inhibitors of AKAP–PKA Interactions**
Protein kinase A (PKA) is a ubiquitous kinase that phosphorylates a broad variety of substrates. A-kinase anchoring proteins (AKAPs) confer specificity to PKA signaling by tethering the kinase to distinct cellular compartments, thereby limiting the access of PKA to a defined pool of its substrates. Interactions between AKAPs and PKA play key roles in a plethora of physiologically relevant proce...
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Protein-protein interactions (PPIs) are highly specific and diverse. Their selective inhibition with peptides, peptidomimetics, or small molecules allows determination of functions of individual PPIs. Moreover, inhibition of disease-associated PPIs may lead to new concepts for the treatment of diseases with an unmet medical need. Protein kinase A (PKA) is an ubiquitously expressed protein kinas...
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The synthesis of several symmetrically 4,4''-functionalized 2,2':6',2''-terpyridines is reported. In addition to the biscarboxylic acid 4,4''-tpy(CO₂H)₂ (3), the anthryl esters 4,4''-tpy(CO₂CH₂Anth) ₂(5a) and 4,4''-tpy(CO₂CH₂CH₂OAnth)₂ (5b) were synthesized. Furthermore, both anthryl esters were used to synthesize symmetric iron(II)-bis(terpyridine)complexes 6a-b. Irradiation experiments were c...
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Localization of cyclic AMP (cAMP)-dependent protein kinase (PKA) by A kinase-anchoring proteins (AKAPs) restricts the action of this broad specificity kinase. The high-resolution crystal structures of the docking and dimerization (D/D) domain of the RIIalpha regulatory subunit of PKA both in the apo state and in complex with the high-affinity anchoring peptide AKAP-IS explain the molecular basi...
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Central to organization of signaling pathways are scaffolding, anchoring and adaptor proteins that mediate localized assembly of multi-protein complexes containing receptors, second messenger-generating enzymes, kinases, phosphatases, and substrates. At the postsynaptic density (PSD) of excitatory synapses, AMPA (AMPAR) and NMDA (NMDAR) glutamate receptors are linked to signaling proteins, the ...
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ژورنال
عنوان ژورنال: Angewandte Chemie International Edition
سال: 2013
ISSN: 1433-7851
DOI: 10.1002/anie.201304686