Released on: April 18, 2008, 9:46 am

Press Release Author: dario/GTCbio

Industry: Biotech

Press Release Summary: Dr. Aglione will present on conducting a High Throughput
Screening Campaign to identify allosteric modulators of a GPCR Using FLIPR.

Press Release Body: MONROVIA, CA - 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.
For more information visit www.gtcbio.com.



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