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GPCRs: Cell based label-free assays in GPCR drug discovery

20 August 2013 | By Niklas Larsson, Linda Sundström, Erik Ryberg and Lovisa Frostne (AstraZeneca)

G protein-coupled receptors are one of the major classes of therapeutic targets for a broad range of diseases. The most commonly used assays in GPCR drug discovery measure production of second messengers such as cAMP or IP3 that are the result of activation of individual signalling pathways. Such specific assays…

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Label-free quantitative proteomics: Why has it taken so long to become a mainstream approach?

13 June 2013 | By Thierry Le Bihan, SynthSys and Institute of Structural and Molecular Biology, University of Edinburgh

In recent years, mass spectrometry (MS) based proteomics has moved from being a qualitative tool (used to mainly identify proteins) to a more reliable analysis tool, allowing relative quantitation as well as absolute quantitation of a large number of proteins. However, the developed quantitative methods are either specific for certain…

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What is label-free screening and why use it in drug discovery?

18 December 2012 | By Matthew A. Cooper and Reena Halai, Institute for Molecular Bioscience, the University of Queensland

In the journey of a molecule from its origins in a compound library to candidate drug status, a large variety of profiling must occur to define activity, selectivity, potency, adverse effects, pharmacology and in vivo efficacy. Advances in biophysical methods that can analyse drug interactions with a molecular target, a…