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G protein-coupled receptors (GPCRs) sense molecules outside the cell and activate inside signal transduction pathways and, ultimately, cellular responses. They are called seven-transmembrane receptors because they pass through the cell membrane seven times.
21 April 2017 | By METTLER TOLEDO
METTLER TOLEDO’s Rainin TerraRack™ pipette tip racks are proving advantageous for the University of Glasgow’s Centre for Cell Engineering, where scientists are investigating cell differentiation and behavior on a variety of materials...
14 October 2015 | By GE Healthcare
In this webinar, we discuss SPR fragment screening of wild type GPCRs enabled by sensitive biosensors and optimised membrane protein assays...
23 December 2014 | By Natalia Meani and Manuela Vecchi
Recognised as one of the major scientific breakthroughs of the 20th century, polymerase chain reaction (PCR) is a quick and simple method to create, in a test tube, millions of copies of a given DNA segment from a complex mixture of genetic material. This method has greatly stimulated biochemical, molecular…
22 September 2014 | By Domain Therapeutics
The world-renowned GPCR specialist will assemble a team of experts in drug discovery and development to guide Domain’s programs...
22 October 2013 | By 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…
Read the free digital version of the August / September edition of European Pharmaceutical Review magazine...
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…
In this Drug Targets In-Depth Focus: GPCR allosteric modulation: new opportunities and challenges for drug discovery; Chloride channels and cardiac arrhythmia: novel therapeutic targets?
3 September 2012 | By 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…
26 April 2012 | By Sofia M.A. Martins, João R.C. Trabuco, Gabriel A. Monteiro and Duarte Miguel Prazeres, Institute for Biotechnology and Bioengineering, Instituto Superior Técnico, Technical University of Lisbon
G-protein coupled receptors (GPCRs) are one of the most popular drug targets today. Almost one third of the approved drugs currently available rely on some kind of interaction with these receptors. The annual revenues are around USD 30 billion (109) and the fact that one quarter of the top US…
13 December 2011 | By Henri Xhaard, Head of Computational Drug Discovery Group, Centre for Drug Research, University of Helsinki
The central location of G protein-coupled receptors (GPCRs) at the interface between the interior and exterior of cells, as well as their key role in signalling events, make GPCRs a prominent class of pharmaceutical targets. To date, approximately 40 per cent of known drugs are thought to act on GPCRs…
19 October 2011 | By Sandra Siehler and Sandra W. Cowan-Jacob, Novartis Institutes for BioMedical Research
G protein-coupled receptors (GPCRs) control a plethora of key physiological functions in every cell of an organism. GPCRs are therefore involved in many diseases, since altered ligand or receptor levels and genetic or epigenetic modifications can lead to GPCR dysfunction and hence a pathophysiological phenotype. About one third of currently…
Profiling of putative lead compounds against a representative panel of important enzymes, receptors, ion channels and transporters is an excellent way to establish a preliminary view of potential issues that might later hamper development.
31 May 2011 | By AstraZeneca
AstraZeneca & Heptares entered a four-year collaboration focused on the potential discovery & development of new medicines...
19 April 2011 | By Sailaja Kuchibhatla, Senior Vice President Business Development DiscoveRx Corporation
“The goal of DiscoveRx has always been centred on creating technologies that enable the highest levels of innovation and development to enrich drug discovery,” Sailaja Kuchibhatla, Senior Vice President Business Development, asserts. Founded in 2000, DiscoveRx solved an unmet need within the GPCR industry by commercialising a functional, naturally coupled…
