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Target identification for small bioactive molecules: finding the needle in the haystack
S Ziegler, V Pries, C Hedberg… - Angewandte Chemie …, 2013 - Wiley Online Library
Identification and confirmation of bioactive small‐molecule targets is a crucial, often decisive
step both in academic and pharmaceutical research. Through the development and …
step both in academic and pharmaceutical research. Through the development and …
Signalling scaffolds and local organization of cellular behaviour
Cellular responses to environmental cues involve the mobilization of GTPases, protein
kinases and phosphoprotein phosphatases. The spatial organization of these signalling …
kinases and phosphoprotein phosphatases. The spatial organization of these signalling …
Target profiling of small molecules by chemical proteomics
U Rix, G Superti-Furga - Nature chemical biology, 2009 - nature.com
The medical and pharmaceutical communities are facing a dire need for new druggable
targets, while, paradoxically, the targets of some drugs that are in clinical use or …
targets, while, paradoxically, the targets of some drugs that are in clinical use or …
Creating order from chaos: cellular regulation by kinase anchoring
Second messenger responses rely on where and when the enzymes that propagate these
signals become active. Spatial and temporal organization of certain signaling enzymes is …
signals become active. Spatial and temporal organization of certain signaling enzymes is …
Mass spectrometry-based proteomics in preclinical drug discovery
Preclinical stages in the drug discovery process require a multitude of biochemical and
genetic assays in order to characterize the effects of drug candidates on cellular systems …
genetic assays in order to characterize the effects of drug candidates on cellular systems …
Triplex protein quantification based on stable isotope labeling by peptide dimethylation applied to cell and tissue lysates
PJ Boersema, TT Aye, TAB van Veen, AJR Heck… - …, 2008 - Wiley Online Library
Stable isotope labeling is at present one of the most powerful methods in quantitative
proteomics. Stable isotope labeling has been performed at both the protein as well as the …
proteomics. Stable isotope labeling has been performed at both the protein as well as the …
Mechanisms of protein kinase A anchoring
P Skroblin, S Grossmann, G Schäfer… - International review of …, 2010 - Elsevier
The second messenger cyclic adenosine monophosphate (cAMP), which is produced by
adenylyl cyclases following stimulation of G-protein-coupled receptors, exerts its effect …
adenylyl cyclases following stimulation of G-protein-coupled receptors, exerts its effect …
AKAP complex regulates Ca2+ re‐uptake into heart sarcoplasmic reticulum
B Lygren, CR Carlson, K Santamaria, V Lissandron… - EMBO …, 2007 - embopress.org
The β‐adrenergic receptor/cyclic AMP/protein kinase A (PKA) signalling pathway regulates
heart rate and contractility. Here, we identified a supramolecular complex consisting of the …
heart rate and contractility. Here, we identified a supramolecular complex consisting of the …
An entirely specific type I A-kinase anchoring protein that can sequester two molecules of protein kinase A at mitochondria
A-kinase anchoring proteins (AKAPs) tether the cAMP-dependent protein kinase (PKA) to
intracellular sites where they preferentially phosphorylate target substrates. Most AKAPs …
intracellular sites where they preferentially phosphorylate target substrates. Most AKAPs …
Phosphodiesterases: evolving concepts and implications for human therapeutics
Phosphodiesterases (PDEs) are a superfamily of enzymes that hydrolyze cyclic nucleotides.
While the 11 PDE subfamilies share common features, key differences confer signaling …
While the 11 PDE subfamilies share common features, key differences confer signaling …