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G protein assays - Articles and news items

Figure 1: Principle of protein fragment complementation. Two interacting proteins are fused to N and C terminal fragments of a fluorescent or luminescent reporter protein (generic depicted in yellow). Upon interaction, the activity of the reporter is reconstituted and can be read out as fluorescence upon excitation (2) or as luminescence upon substrate addition (3)

Cell-based assays for protein-protein interactions

Issue 5 2013, Screening / 22 October 2013 / Mark Wade, Center for Genomic Science of IIT@SEMM

Protein-protein interactions (PPI) form the backbone of all cellular signalling networks, and aberrant PPI contribute to the pathology of several diseases. Thus, strategies to identify PPI modulators are expected to be therapeutically beneficial. However, there are very few examples of clinically approved PPI modulators, reflecting the difficulties of identifying effective compounds for this target class. This perspective reviews the challenges associated with targeting PPI, and summarises the major strategies used to detect and disrupt PPI, with a particular focus on cell-based assays for PPI.

Figure 1: Classification Scheme of GPCRs. R (Rhodopsin-like), S (Secretin-like), G (Glutamate-like), Others (Adhesion, Frizzled, Taste type-2, unclassified)

G protein coupled receptors – exploiting flexible conformations

Drug Targets, Issue 4 2012 / 3 September 2012 / Kathryn L. Chapman, Imperial Drug Discovery Centre, Imperial College London and John B.C. Findlay & Gemma K. Kinsella, Department of Biology, National University of Ireland Maynooth

G-protein coupled receptors (GPCRs) are a diverse super-family of proteins located within the plasma membrane of eukaryotic cells which have a common architecture consisting of seven-transmembrane (7-TM) segments, connected by extracellular (ECL) and intracellular (ICL) loops. They differ from other 7-TM proteins in their ability to activate guanine-nucleotide binding proteins or β-arrestin and so initiate a signalling cascade. They have a wide range of physiological roles and provide many successful drug targets, playing a role in disorders including allergies, cardiovascular dysfunction, depression, obesity, cancer, pain, diabetes and a variety of central nervous system conditions. This review will give a general overview of GPCRs and how their structures and activities can be used in drug discovery…

 

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