PISCATAWAY, N.J. & RESEARCH TRIANGLE PARK, N.C.--(BW HealthWire)--Aug. 29, 2001--
Transfluor(TM) Technology and the LEADseeker(TM) Cell Analysis
System Bring Together Two Advanced G Protein-Coupled Receptor
Drug Discovery Platforms
Norak Biosciences, Inc. and Amersham Pharmacia Biotech, Inc. today announced the signing of a collaborative agreement to initially enable a limited number of pharmaceutical companies with a combination of two important new G protein-coupled receptor (GPCR) drug discovery technologies.
Both technologies are only now becoming commercially available.
GPCRs are cell surface targets to which drugs that cause changes in intracellular function bind. As a class, GPCRs are historically the single richest receptor target for drug discovery, involved in nearly 60 percent of all prescription drugs on the market today. Medications that treat conditions regulated by GPCRs cover most therapeutic areas and represent billions in annual sales worldwide. However, the potential for GPCR-based drugs remains largely untapped due to the fact that only about 200 of these important drug targets are functionally known. It is estimated that a further 1,000 GPCRs are ``orphans'' (functionally unknown), and most major pharmaceutical companies today have active GPCR drug discovery programs.
Norak's Transfluor(TM) technology is a patented, universal GPCR drug discovery technology designed to be the most direct and accurate method for screening potential drug candidates against GPCR targets, whether known or orphan. Amersham Pharmacia Biotech's LEADseeker(TM) Cell Analysis System is the first automated, laser-based confocal fluorescence imager for high throughput screening of live, whole cell assays. The combination of these two technologies has the potential to substantially accelerate known and orphan GPCR drug discovery by combining the predictive accuracy and quantitative data normally acquired from multiple primary and secondary screens into one primary screening exercise. These combined technologies will allow researchers to observe the direct effect of a drug candidate on live cells.
``Both Transfluor and the LEADseeker cell analysis system are breakthroughs in drug discovery technology,'' commented Dr. Roger D Blevins, President and CEO of Norak. ``Combining them will create a very powerful, state-of-the-art, high throughput screening engine that will accelerate GPCR drug discovery with great savings in time and money for the pharmaceutical industry,'' added Neil Cook, VP drug discovery at Amersham Pharmacia Biotech.
Transfluor was licensed by Norak from technology developed at Duke University in 1999 and represents the combined research into GPCR signaling pathways over several decades by Norak's scientific founders, Drs. Marc Caron, Robert Lefkowitz, and Larry Barak. The LEADseeker Cell Analysis System is Amersham Pharmacia Biotech's next generation, state-of-the-art imaging system and is based on technology developed at Praelux, acquired in 2000.
Norak Biosciences, Inc., headquartered in Research Triangle Park, NC, is a private biotechnology company. Norak is utilizing its proprietary Transfluor technology to become a world leader in the discovery and development of drugs that regulate G protein- coupled receptors. For more information about Norak Biosciences, Inc., please visit the Company's website at norakbio.com.
(edit) From Norak website -
Transfluor™… The Company has an exclusive license from Duke University to develop and commercialize a patented platform technology enabling the direct measurement of GPCR activation and subsequent receptor regulation. In contrast to the present methods of analyzing GPCR function, the power of the new technology is in its simplicity and general applicability to all GPCRs. A common feature of this receptor class is their diminished ability to signal after prolonged or repeated stimulation by ligand. This phenomenon of receptor “desensitization” depends upon the rapid interaction of two intracellular proteins, namely G protein-coupled receptor kinase (GRK) and arrestin, with the activated receptor. As the main research focus of Norak’s scientific founders for more than two decades, Drs. Marc Caron, Robert Lefkowitz and Larry Barak at Duke University have defined the process of GPCR desensitization and developed a method to monitor the process. This method is the basis of the Transfluor™ technology that enables detection of receptor activation and desensitization in real time by monitoring the movement of fluorescent arrestin protein inside a single living cell. The movement of fluorescence is easily detected and the process can be automated and quantitated with existing computerized imaging systems. The methodology discriminates between agonists, partial agonists, antagonists, inverse agonists and allosteric modulators, provides valuable information about relative potency and receptor affinity, and can be used to discover compounds that modulate GRK or arrestin. Utilizing cell lines expressing human, animal or plant GPCRs of interest, the Transfluor™ technology provides a platform for screening chemical libraries.
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