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cAMP Signaling

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Cover of 'cAMP Signaling'

Table of Contents

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    Book Overview
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    Chapter 1 Simultaneous Assessment of cAMP Signaling Events in Different Cellular Compartments Using FRET-Based Reporters
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    Chapter 2 Recording Intracellular cAMP Levels with EPAC-Based FRET Sensors by Fluorescence Lifetime Imaging
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    Chapter 3 A Novel Approach Combining Real-Time Imaging and the Patch-Clamp Technique to Calibrate FRET-Based Reporters for cAMP in Their Cellular Microenvironment
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    Chapter 4 Structure-Based, In Silico Approaches for the Development of Novel cAMP FRET Reporters
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    Chapter 5 Automated Image Analysis of FRET Signals for Subcellular cAMP Quantification
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    Chapter 6 Channel-Based Reporters for cAMP Detection
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    Chapter 7 Imaging Sub-plasma Membrane cAMP Dynamics with Fluorescent Translocation Reporters
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    Chapter 8 Adenoviral Transduction of FRET-Based Biosensors for cAMP in Primary Adult Mouse Cardiomyocytes
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    Chapter 9 Generation of Transgenic Mice Expressing FRET Biosensors
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    Chapter 10 Photoactivatable Adenylyl Cyclases (PACs) as a Tool to Study cAMP Signaling In Vivo: An Overview
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    Chapter 11 Selective Disruption of the AKAP Signaling Complexes.
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    Chapter 12 Screening for Small Molecule Disruptors of AKAP–PKA Interactions
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    Chapter 13 Structure-Based Bacteriophage Screening for AKAP-Selective PKA Regulatory Subunit Variants.
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    Chapter 14 A yeast-based high-throughput screen for modulators of phosphodiesterase activity.
  16. Altmetric Badge
    Chapter 15 Separation of PKA and PKG Signaling Nodes by Chemical Proteomics
  17. Altmetric Badge
    Chapter 16 Development of Computational Models of cAMP Signaling
Attention for Chapter 12: Screening for Small Molecule Disruptors of AKAP–PKA Interactions
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Chapter title
Screening for Small Molecule Disruptors of AKAP–PKA Interactions
Chapter number 12
Book title
cAMP Signaling
Published in
Methods in molecular biology, March 2015
DOI 10.1007/978-1-4939-2537-7_12
Pubmed ID
Book ISBNs
978-1-4939-2536-0, 978-1-4939-2537-7
Authors

Schächterle, Carolin, Christian, Frank, Fernandes, João Miguel Parente, Klussmann, Enno, Carolin Schächterle, Frank Christian, João Miguel Parente Fernandes, Enno Klussmann

Abstract

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 kinase that controls a plethora of cellular functions. A-kinase anchoring proteins (AKAPs) are multivalent scaffolding proteins that directly interact with PKA. AKAPs spatially and temporally restrict PKA activity to defined cellular compartments and thereby contribute to the specificity of PKA signaling. However, it is largely unknown which of the plethora of PKA-dependent signaling events involve interactions of PKA with AKAPs. Moreover, AKAP-PKA interactions appear to play a role in a variety of cardiovascular, neuronal, and inflammatory diseases, but it is unclear whether these interactions are suitable drug targets. Here we describe an enzyme-linked immunosorbent assay (ELISA) for the screening of small molecule libraries for inhibitors of AKAP-PKA interactions. In addition, we describe a homogenous time-resolved fluorescence (HTRF) assay for use in secondary validation screens. Small molecule inhibitors are invaluable molecular tools for elucidating the functions of AKAP-PKA interactions and may eventually lead to new concepts for the treatment of diseases where AKAP-PKA interactions represent potential drug targets.

Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 5 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 5 100%

Demographic breakdown

Readers by professional status Count As %
Student > Master 2 40%
Student > Bachelor 2 40%
Student > Ph. D. Student 1 20%
Readers by discipline Count As %
Medicine and Dentistry 2 40%
Pharmacology, Toxicology and Pharmaceutical Science 1 20%
Agricultural and Biological Sciences 1 20%
Biochemistry, Genetics and Molecular Biology 1 20%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 23 March 2015.
All research outputs
#20,265,771
of 22,796,179 outputs
Outputs from Methods in molecular biology
#9,899
of 13,111 outputs
Outputs of similar age
#216,376
of 256,364 outputs
Outputs of similar age from Methods in molecular biology
#59
of 81 outputs
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We're also able to compare this research output to 81 others from the same source and published within six weeks on either side of this one. This one is in the 1st percentile – i.e., 1% of its contemporaries scored the same or lower than it.