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TUESDAY , MAY 13
7:30am – 5:45pm
Registration Open
1:55pm Chairperson’s Remarks
Ryan McGuinness, MDS Analytical Technologies
2:00 Application
of Epic System in Cell-Based Assays
Hong Xin, Ph.D.,
Senior Scientist, Lead Generation, Johnson & Johnson Pharmaceutical R&D
The Epic system is a high-throughput, label-free assay system
that uses optical waveguide technology to detect changes in local refraction
index. These changes correspond to a binding event for biochemical assays and
mass redistribution in cell-based assays. The system allows us to assay GPCRs
using native cell lines with an endogenous level of receptor expression,
regardless of the G-protein coupling mechanism. Because the same assay platform
may be used for all GPCR targets, we anticipate a rapid assay development time,
the elimination of label-dependent interference, and results that are more
predictive of a compound’s physiological activity. This system also enables
screening of challenging targets, such as Gi-coupled GPCRs. This presentation
would discuss the application of Epic system in functional cell-based GPCR
assays for lead generation, and compound profiling.
2:30 Evaluation
of Cellular Impedance Assays for Assessing Complex GPCR Pharmacology in
Drug Discovery
Matthew F. Peters, Ph.D., Principle Scientist, Lead Generation
Department, AstraZeneca
GPCR ligands with subtle structural differences can activate
different signaling pathways via the same receptor. This ligand-specific
signaling is not widely exploited in drug discovery perhaps due to the
difficulty of assessing SAR vs. multiple pathways. Cellular
dielectric spectroscopy (CDS) is an emerging technology that can
distinguish Gs, Gi/o and Gq signal transduction in a whole-cell
label-free format, enabling one to monitor activation pathways by
different ligands within the same assay condition. We show that
GPCR agonists, antagonists, inverse agonists and allosteric modulators
can be quantified by CDS with precision suitable for drug discovery SAR
studies. Furthermore, agonist ligands for one GPCR reveal
Gs-dominant coupling in HEK cells versus Gi-dominant coupling in CHO
cells. Other ligands showed inverse agonism against Gi coupling
only, consistent with either ligand-specific trafficking or
pathway-specific constitutive activity. These findings support
broad use of CDS for SAR studies including ligand-specific signalling.
3:00 Novel
Applications of the CellKey System for Assaying Compound Activity
Against GPCR and Chemotaxis Related Targets
Rod DeLeon, Scientist IV,
Department of Translational Sciences, Boehringer Ingelheim
Pharmaceuticals, Inc.
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3:30 Technology
Watch
The CellKeyTM System, a Label-Free Cell Based Assay
Platform: Generating Biorelevant Data in all Phases of Drug
Discovery
Ryan McGuinness, Senior Application Scientist - CellKey™ System,
MDS Analytical Technologies
Label free cell based assay technologies are advancing at a
rapid rate and promise to enhance compound screening efforts by
providing novel readouts in simplified formats. Using impedance technology,
the system CellKey™ System generates functional data which reflect
integrated cellular responses to compound treatment in a kinetic and
noninvasive manner. By not requiring labels or
artificial mediators of any sort, the CellKey™ System monitors the
activity of native response pathways, thus producing more
biorelevant data. In this presentation we will provide an
overview of this important label-free technology and discuss its
applications to the full spectrum of drug discovery tasks, including
target identification and validation, compound screening, and lead
optimization. Through its unique features and strengths, the
CellKey™ System has the potential to identify higher quality
validated compounds earlier in the drug discovery process.
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Sponsored by
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3:45 Networking
Refreshment Break in the Exhibit Hall
Plenary
Keynote
4:30
Pharmaceutical Research: From Productivity to
Sustainability
Charles T. Gombar,
Ph.D., Vice President, R&D Strategy & Business Improvement, Wyeth Research
The global
pharmaceutical industry is facing new and unprecedented challenges that may
alter the framework for how companies operate.
For pharmaceutical companies to sustain research and development
investments at traditional levels new products must succeed commercially, yet
the evolution of the pharmaceutical environment is making commercial success
increasingly difficult. Regulatory
hurdles have never been higher, reimbursement is difficult to secure, and
pressure from generic competition is eroding markets.
In this session, Charles Gombar, Ph.D., Vice President, R&D Strategy and
Business Improvement, Wyeth Research, will present a perspective on the current
industry challenges, and a panel of experts representing these major
stakeholders will discuss the issues and potential solutions.
5:00 Panel
Discussion: Facing the Challenges in the Pharmaceutical Industry
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How
Pharmaceutical Companies Need to Evolve to Succeed
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Meeting the
Challenges in Licensing, Reimbursement, and Generic Competition
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Regulatory
Issues and Insights
Panelists:
Charles T. Gombar,
Ph.D., Vice President, R&D Strategy & Business Improvement, Wyeth Research
Susan S Allen, MD,MPH, Regulatory and Compliance Consultant, Regulatory and
Compliance Consultants, LLC
William D. Matthews, Ph.D., Vice President of R&D Management Operations,
Johnson and Johnson
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5:30pm End of Day
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