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G protein-coupled receptors (GPCRs)


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.


Rainin TerraRack™ benefits cell differentiation studies

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...


The evolving field of PCR: which method will you choose?

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…


Cell-based assays for protein-protein interactions

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…


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…


G protein coupled receptors – exploiting flexible conformations

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…


GPCR screening and drug discovery: Challenges and latest trends

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…


Status and challenges in structure-based drug discovery for G protein-coupled receptors

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…


Lead discovery for targeting G protein-coupled receptors

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…


DiscoveRx Interview

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…