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Arrestin developments
November 2009
by Jeffrey Bouley  |  Email the author


FREMONT, Calif.—DiscoveRx Corp. kicked off the month of October with an announcement that it had signed a global agreement with United Kingdom-based pharma giant GlaxoSmithKline (GSK) to provide access to its PathHunter β-Arrestin parental cell lines, clones and associated reagents for use in GSK's internal G-protein-coupled receptor (GPCR) screening and profiling efforts.  
DiscoveRx framed the deal, along with what it calls "similar ones signed with other major drug discovery organizations," as being one that "further validates PathHunter ß-Arrestin as a key platform to study GPCR biology."  
The Oct. 1 deal carries some special weight, though, given the size and stature of the entity involved, and Sailaja Kuchibhatla, senior vice president of business development at DiscoveRx, says, "The GSK global agreement vouches that the platform is a must and hence all sites on a worldwide basis have adopted the platform."  
It's a deal that also comes hot on the heels of another one, announced just eight days earlier, with GSK and the UK's Medical Research Council Technology (MRCT), forming a three-way alliance to seek out natural substances that bind to GPCRs. Through the identification of the natural ligands for these receptors, the partners anticipate 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.
That earlier deal, Kuchibhatla says, points to the value of PathHunter b-Arrestin specifically for GSK's de-orphanization campaign rather than GPCR work in general, but notes that it "is a precedence setting deal whereby a leading academic institute, a biotech tool company such as DiscoveRx and a premier pharma company have struck a strategic collaboration to discover novel drugs," she says, adding: "DiscoveRx continues to innovate in field of GPCR and kinase drug discovery with industry-leading cell-based assay platforms for screening and profiling."  
In the three-way collaboration, the parties note that the human genome encodes roughly 350 GPCRs, which respond to ligands, such as hormones, growth factors and proteins. Despite intensive efforts, though, they notes that there remain at least 100 orphan GPCRs—receptors that have no known ligand or function.
Identifying the ligands and roles of these orphan GPCRs could potentially open up new areas of biology for therapeutic intervention and drug discovery, Kuchibhatla notes, and this industrial/academic collaboration formed in late September will use the PathHunter β-Arrestin assay technology on what DiscoveRx calls "an unprecedented scale" to identify the ligands for some of these orphan GPCRs.  
DiscoveRx is no stranger to the area of orphan GPCRs. Along with more than 140 known GPCR targets, it also offers 90 orphan GPCR assays for GPCR drug discovery.  
After the three parties identify some of the ligands for these orphan GPCRs, certain receptors will progress into high-throughput compound screens, which could be performed either by MRCT or GSK, to identify lead molecules for possible drug discovery and development efforts.  
In general, though, as GSK has had significant success at pairing orphan GPCRs with ligands, it will provide the GPCR ligand banks, laboratory equipment and laboratory space. DiscoveRx, for its part, is providing access to stable cell lines expressing orphan GPCRs formatted in the PathHunter β-Arrestin assay. And MRCT is in place to provide scientific staff members who can perform project activities and identify academic collaborators to characterize ligand-matched GPCRs.  
As Dr. Pyare Khanna, CEO of DiscoveRx noted with the release of the PathHunter β-Arrestin assay just over three years ago, "[This assay] is another revolutionary offering from DiscoveRx which further confirms our commitment to provide novel, chemiluminescent assays for both biochemical and cell-based drug discovery research and screening. This product was developed in response to a market demand for a non-imaging, HTS technology for studying virtually any GPCR. With a product portfolio that includes Beta-Arrestin technology, HitHunter cAMP assays, HitHunter IP3 assays, Calcium NW and Coelenterazine reagents, DiscoveRx is the only GPCR assay provider that offers best-in-class screening solutions for every major type of GPCR target."
In other recent PathHunter β-Arrestin assay news, DiscoveRx announced just a week after the global access deal with GSK that it had signed a co-marketing agreement that allows BioFocus to perform screening on behalf of BioFocus' customers using DiscoveRx PathHunter β-Arrestin GPCR screening assay, HitHunter cAMP assays and associated cell lines.
Code: E110915



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