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Industry and Academics Team Up to De-orphanise GPCRs - Industry and Academia team up in three-way collaboration to identify natural substances that can bind to orphan G-protein-coupled receptors. Findings could lead to new targets for drug discovery
Industry and Academics Team Up to De-orphanise GPCRs


NewswireToday - /newswire/ - London, United Kingdom, 2009/09/23 - Industry and Academia team up in three-way collaboration to identify natural substances that can bind to orphan G-protein-coupled receptors. Findings could lead to new targets for drug discovery.

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DiscoveRx Corporation, GlaxoSmithKline (GSK) and Medical Research Council Technology (MRCT) have announced a three way alliance to seek out natural substances that bind to G-protein-coupled receptors (GPCRs). Through the identification of the natural ligand for these receptors it is anticipated that this work will identify and validate new drug targets that could ultimately help develop new therapies, as compounds that modulate GPCRs are already the basis of many licensed medicines.

The human genome encodes roughly 350 GPCRs, which respond to substances, also known as ligands. These ligands include hormones, growth factors and proteins. Activation of the receptor by the ligand triggers signaling systems within the cell. These signalling systems are pivotal to normal cell biology and are involved in disease processes.

Despite intensive efforts, there remain at least 100 orphan GPCRs - those receptors which have no known ligand or function. Identifying the ligand and role of these orphan GPCRs could potentially open up new areas of biology for therapeutic intervention and drug discovery.

This new industrial/academic collaboration will use the novel PathHunter™ ß-arrestin assay technology on an unprecedented scale to identify the ligands for some of these orphan GPCRs. This systematic approach will target the 100 “Family A” GPCRs which remain classified as orphan receptors with no known biological ligand. Following the identification of ligands, certain receptors will progress into high throughput compound screens to be performed at either MRC-T or GSK to identify lead molecules to support drug discovery.

GSK has had significant success at pairing orphan GPCRs with ligands and will provide the GPCR ligand banks, laboratory equipment and laboratory space. DiscoveRx will provide access to stable cell lines expressing orphan GPCRs formatted in the PathHunter™ ß-arrestin assay (~90 orphan GPCRs) and MRCT will provide scientific staff to perform project activities and identify academic collaborators to characterise ligand matched GPCRs.

About GPCRs (G protein-coupled receptors)
G-protein coupled receptors (GPCRs) are a family of proteins that are found widely throughout the body and play a fundamental role in physiology and pathophysiology. As such, they are potential targets for therapeutic intervention in many, if not most, diseases. In 2000, 26 of the top 100 pharmaceutical products were compounds that target GPCRs accounting for sales of over US$23.5 billion. This represents around 9% of total global pharmaceutical sales, thus making the GPCR super family the most successful of any target class in terms of therapeutic benefit and commercial sale.

About DiscoveRx
Founded in 2000, DiscoveRx ( is a privately held, venture-backed company headquartered in Fremont, California, with an additional office in Birmingham, United Kingdom. The Company pioneered the use of β-galactosidase enzyme fragment complementation in biochemical and cell based assays for discovery research, and holds extensive intellectual property in this area. DiscoveRx is dedicated to the development and commercialization of innovative solutions to study GPCRs, Kinases and other major drug target classes, and many of their innovative products have been widely adopted in pharmaceutical and biotech drug screening laboratories worldwide. The Company currently offers the broadest portfolio of non-force coupled cell-based functional assays for known and orphan G-protein coupled receptors.

About the Medical Research Council
The Medical Research Council is dedicated to improving human health through excellent science. It invests on behalf of the UK taxpayer. Its work ranges from molecular level science to public health research, carried out in universities, hospitals and a network of its own units and institutes. The MRC liaises with the Health Departments, the National Health Service and industry to take account of the public’s needs. The results have led to some of the most significant discoveries in medical science and benefited the health and wealth of millions of people in the UK and around the world.

About Medical Research Council Technology (MRCT)
MRCT ( is the exclusive commercialisation agent for the UK Medical Research Council, working to translate cutting edge scientific discoveries into commercial products. MRCT bridges the gap between innovative basic science and making medicine. MRCT works to provide drug-like candidate molecules to innovative new drug targets, and to translate innovative antibody-based drug targets into potent and selective therapeutic antibody candidates, giving pharmaceutical and biotechnology companies new starting points for drug discovery and development, based on MRC advances in science. MRCT’s Therapeutic Antibody Group scientists have a proven track record of success in antibody humanisation which extends over 20 years and has produced 10 clinical candidates and two regulatory approved humanised antibodies: Elan/Biogen Idec’s Tysabri® and Chugai/Roche’s Actemra®.

About GlaxoSmithKline
One of the world’s leading research-based pharmaceutical and healthcare companies – is committed to improving the quality of human life by enabling people to do more, feel better and live longer.

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Industry and Academics Team Up to De-orphanise GPCRs

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