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Agenda
Day One - September 10
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8:00am |
Registration |
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Target-Based Biology and Validation
Session Chair: Eben Massari, Principal Scientist, Kalypsys |
| 9:05am |
Use of Novel High-content Assays to Identify New Treatments for Huntington’s Disease
Stefan Jaeger, Evotec
This presentation will illustrate the immense power of High-Content Assays within a CNS drug discovery project. Also, in times when "systems biology" is a new buzzword, the benefits and challenges of phenotypic assays for drug discovery will be discussed. |
| 9:35am |
Keynote Address - GPCR Dynamics in Membranes: Ligand Channeling and Receptor Mixing
Thomas Sakmar, Professor, Rockefeller University
Hydrophobic 7-transmembrane receptor ligands may use a specific pathway through the membrane bilayer interior to enter the receptor active site. The primary ligand entry site in rhodopsin, a model Type I GPCR, is located between TM helices 5 and 6. FRET experiments show three orders of magnitude changes in ligand binding kinetics depending on the side chains in the entry pathway. MD simulations suggest high energy barriers for ligand entry and exit. Additional simulations show how receptors associate spontaneously in bilayers to form higher-order structures. |
| 10:20am |
Coffee and Networking in Exhibit Hall |
| 11:05am |
Hsp90 Inhibition for Cancer Therapy
Rob Howes, Senior Team Leader, Vernalis |
| 11:35am |
A Cell-based Assay for IκBα Stabilization Using a Two-color Dual Luciferase-based Sensor
Eric Davis, Metabolism Branch, National Cancer Institute |
| 12:05pm |
Lunch and Poster Viewing |
| 1:35pm |
Other Screening Technologies
Session Chair: Thomas Sakmar, Professor, Rockefellar University |
| 1:40pm |
Interrogating Diverse Target Families by Homogenous Immunodetection of Nucleotides
Robert Lowery, President and CEO, Bell Brook Labs |
| 2:10pm |
Development of an ADME and Drug-drug interactions Knowledge Database for the Acceleration of Drug Discovery and Development
Francois Petitet, CSO, Aureus Pharma
The take home messages from this presentation will include a highly structured database which describes biological protocols in detail, the extraction of high quality datasets with precise filters, as well as the accurate design of predictive models. |
| 2:40pm |
A Phenotypic-Based Approach for Identification of off Target Effects and Mechanism of Drug Action
Yama Abassi, Director, ACEA Biosciences
We describe a simple drug profiling approach in mammalian cells using impedance technology. Signature activity patterns for anti-mitotics, GPCR modulators, nuclear receptors agonists, protein synthesis inhibitors, DNA damaging agents and actin disrupting agents were obtained. Using these signature patterns we have identified the molecular target for an experimental compound and have identified off-target effect for an FDA approved compound as well as an experimental compound. |
| 3:10pm |
Coffee and Networking in Exhibit Hall |
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3:55pm |
Light Induced Depolarization of Cells: An Emerging Tool for HTS of Voltage-gated Ion Channels
Bela Kelety, Director R&D, IonGate Biosciences |
| 4:25pm |
Optimizing Transiently Transfected HEK-293 Cells Expressing α7-V201-5HT3 Chimeras for the QPatch
Ali Yehia, Applications Scientist, Sophion Bioscience |
| 4:55pm |
Drinks Reception
(Sponsorship opportunity still available, please contact Ian.Slade@selectbiosciences.com)
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Day Two - September 11
| 9:00am |
GPCR Screening
Session Chair: Carsten Haber, Scientist, IonGate Biosciences |
| 9:05am |
Addressing the Challenges to GPCR Screening
Annette Gilchrist, CSO, Caden Biosciences
Deciphering the hits that come from screens targeting GPCRs is challenging due to the lack of effective tools. This problem has been compound by the recognition of allosteric modulators and inverse agonists as important therapeutic classes. Most GPCRs couple to multiple G-proteins, and elucidating functional selectivity can be difficult in functional assays. There remain a number of intractable targets within this large receptor family. |
| 9:35am |
Keynote Address - Ultra High-Throughput Screening of G Protein-Coupled Receptors Using Kalysps Technologies
Eben Massari, Principal Scientist, Kalypsys
Kalypsys' mission is to leverage its suite of proprietary ultra high-throughput (uHTS) technologies to create a highly efficient and sustainable drug discovery pipeline. In this presentation, they discuss efforts to use uHTS technologies to miniaturize and implement cAMP, calcium mobilization and protein-protein interaction assays to identify GPCR ligands. |
| 10:20am |
Coffee and Networking in Exhibit Hall |
| 11:05am |
The CellKey™ System: A Biorelevant Cell Based Assay Platform and its Application for Secondary Screening of GPCRs
Debra Gallant, Applications Scientist, MDS Sciex
This presentation illustrates the universal ability of the CellKey™ System to measure multiple endogenous cell surface receptor families, including GPCRs, in a single assay with minimal assay development. Generation of information–rich data coupled with ease of use can streamline your workflow from assay development to informed decision. |
| 11:35pm |
New Platforms
Session Chair: Enal Razvi, Industry Analyst |
| 11:40am |
A Novel, Label Free Analysis Tool for Screening Transporter Proteins
Carsten Haber, Scientist, IonGate Biosciences
IonGate Biosciences’ label-free Surface Electrogenic Event Reader or SURFE2R is a newly developed, high-throughput analysis instrument which directly captures electrogenic transfer currents of biological transporters. Sensor elements containing the transporter protein on solid supported membrane vesicles are activated via rapid substrate solution exchange, delivering fast and repeatable transfer currents in the range of pico- to nanoAmps. The key applications are in ADME, the characterization of transporter targets and research for inhibitors. |
| 12:10pm |
Lunch and Poster Viewing |
| 1:40pm |
High Content Live-Cell Analysis at High Throughput Utilizing The New Genetix Imager
Nicol Watson, Research Scientist, Genetix Ltd. |
| 2:10pm |
Automated Patch Clamp for High-quality, Versatile Ion Channel Screening
Cecilia Farre, Senior Scientist, Nanion Technology |
| 2:40pm |
Coffee and Networking in Exhibit Hall |
| 3:25pm |
Flash Luminescence in HTS
Andrea Rossignoli, Senior Scientist, Axxam |
| 3:55pm |
Close of Conference |
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