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DiscoveRx Interview

Posted: 19 April 2011 |

“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 chemiluminescent screening methodology for GPCRs that was compatible with existing high throughput equipment. Early GPCR screening campaigns relied on labour intensive and radioactive techniques such as binding assays, before researchers moved towards more functional assays that relied on artificially influencing the coupling of the GPCR to combine with low cost detection reagents and high throughput fluorescent plate readers to increase throughput. “DiscoveRx’s HitHunter® cAMP technology platform became a viable and superior alternative to laborious radiolabelled binding and force coupled calcium screening,” Kuchibhatla explains.

“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 chemiluminescent screening methodology for GPCRs that was compatible with existing high throughput equipment. Early GPCR screening campaigns relied on labour intensive and radioactive techniques such as binding assays, before researchers moved towards more functional assays that relied on artificially influencing the coupling of the GPCR to combine with low cost detection reagents and high throughput fluorescent plate readers to increase throughput. “DiscoveRx’s HitHunter® cAMP technology platform became a viable and superior alternative to laborious radiolabelled binding and force coupled calcium screening,” Kuchibhatla explains.

So why is GPCR analysis important for drug discovery? Kuchibhatla clarifies: “G proteincoupled receptors (GPCRs) are the largest and most druggable class of cell surface receptors that account for more than 50 per cent of all drug discovery programs. Since the mid 1980’s, there has been a focused effort to understand them, yet there are still known and orphan GPCR targets that aren’t well understood. They continue to be studied by drug discovery researchers as successful GPCR screening campaigns are likely to yield promising drug candidates.”

DiscoveRx subsequently launched the next generation PathHunter® β-Arrestin platform, which took advantage of actual GPCR biology which transformed the industry as the combination of PathHunter® and HitHunter® cAMP gave researchers two independent signalling options for screening. “To expedite the drug discovery process, we provided multiple formats by which technology could be accessed,” Kuchibhatla says. “More recently, we launched another PathHunter® platform for monitoring GPCR internalisation. The vision of the DiscoveRx organisation is that for every known or orphan GPCR, we will have at least an assay format and sometimes multiple assay formats. This commitment to provide a comprehensive portfolio will truly enable the drug discovery community as it continues to race towards identifying the next blockbuster drug.”

DiscoveRx’s PathHunter® and HitHunter® GPCR assays are 1- 2 step addition protocols that are simple, robust, gain-of-signal chemi – luminescent detection assays. Apart from ease of adoption, the assays are compatible with standard laboratory equipment. DiscoveRx offers over 400 assays and their commitment to providing multiple options to end-users has led them to develop two or more pathway formats for each and every known GPCR. “The ability to interrogate the effects of a compound on multiple pathways for a single target is revolutionary and holds the promise of uncovering more about compound activity. This can provide greater compound knowledge allowing for more specific and more potent drug compounds with fewer less desirable side effects,” Kuchibhatla contends.

GPCRs are activated through both G-protein dependent and G-protein independent pathways, opening discovery of a novel class of compounds that are biased towards one pathway. Having an option to screen a target in multiple pathway formats allows the drug discovery community to discover new compounds for old targets or to de-orphanise GPCRs that are therapeutically relevant and validated as a drug target.

“We continue to launch cutting edge platforms,” Kuchibhatla acknowledges. “In the future, our second messenger, β-arrestin recruitment and GPCR internalisation assays will be followed by GPCR hetero- and homodimerisation assays as well as platforms that will allow researchers to study their own proprietary GPCR or mutant GPCR of interest.’’

Visit www.discoverx.com/gpcrs for a complete overview of DiscoveRx’s innovations in the field of GPCR biology

About the Author

Ms. Sailaja Kuchibhatla is Senior Vice President of Marketing and Business Development responsible for activities that include creating and managing new business opportunities and initiatives for the drug discovery research market. Ms. Kuchibhatla began her career at Clontech in 1989 in the research and development organization. After six years of varied and increasing responsibility within R&D at Clontech, she moved into Marketing, followed by her most recent appointment as VP of Business Development. As a key member of the marketing and business development group for the last 10 years, Ms. Kuchibhatla handled various responsibilities, including leading the marketing team and licensing of key technologies for Clontech in the last five years. She was a member of the Senior Leadership team at BD Biosciences/Clontech and a member of the Technology Strategy and Business Development team at BD Biosciences. She holds MS and BS degrees in Biological Sciences. interview:Layout 1 5/4/11 09:15 Page 1

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