Dr. Anthony Aglione, Associate Principle Scientist at Hoffmann-La Roche will present at GTCbio’s 3rd Assay Development & Screening Technologies Conference on June 5-6, 2008 in San Francisco, CA. Dr. Aglione will present on conducting a High Throughput Screening Campaign to identify allosteric modulators of a GPCR using FLIPR.

Recent interests geared at identifying potential drug candidates that interact with a GPCR’s allosteric site have altered high throughput screening (HTS) approaches which have traditionally looked at a compounds ability to interact with a GPCR’s orthosteric ligand binding site. One experimental approach is to first expose the GPCR of interest to potential allosteric drug candidates, followed by exposure to an EC10 concentration of the natural orthosteric agonist ligand. In this scenario it is possible to identify “enhancing” compounds that may either increase the potency (leftward shift of an agonist dose response curve) or efficacy (magnitude of the functional signal) of the natural ligand. A known GPCR that is implicated in feeding behavior was cloned into CHOK1 cells for use in a FLIPR calcium flux-based HTS campaign. Evaluation of our full compound library was successful in identifying selective positive allosteric modulators with a range of activities. Assay specifics such as Z’ prime, hit rate and agonist response will be discussed.

GTCbio's 3rd Assay Development and Screening Technologies conference will provide attendees with critical information to utilize in the discovery and development of assays, while keeping them informed about the latest screening technologies for both high-throughput screening and high-content screening. Topics being covered include cell based assays, high throughput screening, high content screening, in vitro assays and screening, novel assay and screening technologies, and target validation.