Select Conferences |

Agenda

Day 1 - 20 February

09:00	Plenary Session Chaired by Steve Rees
09:05	The Industrialisation of Cell Based Screening Steve Rees, Director, Screening Compound Profiling, GlaxoSmithKline The Screening and Compound Profiling department occupies an open-plan facility designed according to the principles of Cellular Manufacturing and Lean Sigma. The design of this laboratory will be overviewed and specific challenges associated with the industrialisation of cell based assays will be discussed.
09:35	Towards a Comprehensive Understanding of Host Cell Function in Infection Nikolaus Machuy, Team Leader Screening Facility, Max Planck Institute for Infection Biology In order to identify factors affecting the infection process, an automated RNA interference platform enabling large-scale loss-of-function studies was set-up. A stable cell line was established expressing a cytoplasmic GFP fusion protein of the NFkB subunit p65 that translocated to the nucleus upon activation.
10:05	Coffee break and networking in exhibition hall
10:50	Automated Assay Development and Optimization Lorenz Mayr, Executive Director, Novartis Pharmaceutical AG Current bottlenecks in lead discovery are no longer in high-throughput screening, but rather in assay development and tool production. Our presentation describes fully automated assay development and optimization in 1536w plates upon the use of liquid handling robots and statistical design-of-experiment software.
11:20	Strategies to Reduce Late Stage Attrition Due to Mitochondrial Toxicity - Designing Novel Screening Methods Yvonne Will, Group Leader Biochemical/Cellular and Molecular Toxicology, Pfizer Drug Safety Research and Development Mitochondrial dysfunction is a major mechanism of drug-induced toxicity. A new HTS applicable screen measuring oxygen consumption in isolated mitochondria identifies early compounds to eliminate perturbing mitochondrial function within the drug discovery process which can reduce expensive late stage attrition.
11:50	NIH Chemical Genomics Center: Opening a New Door to Discovery Anton Simeonov, Group Leader, Bio-organic Chemistry and Assay Technologies, National Institute of Health The NIH Chemical Genomics Center, established under the NIH Roadmap initiative, uses the tools of small molecule discovery to develop chemical probes for the study of protein and cell functions.
12:20	Lunch and networking in exhibition hall
13:15	Poster Viewing
14:00	Track A - Novel Assay Technologies for the Discovery of GPCR Drugs Chaired by Sandra Siehler
14:05	Novel Fluorescent Techniques to Study the G12/13 Signaling Pathway of GPCRs: Molecular Insights and Impact on Drug Discovery Sandra Siehler, Research Investigator (II), Novartis Pharma AG A novel technique to measure G12/13 signaling of GPCRs using subcellular confocal imaging will be presented. The technique enables for the first time screening of GPCRs in a G12/13-related disease context.
14:35 .	Novel Applications of GPCR-G Protein Fusions in Pharmacology and Ligand Screening Graeme Milligan, Professor, University of Glasgow Pairs of inactive GPCR-G protein fusion proteins are used to develop a functional complementation strategy. This approach can identify hetero-dimer allosteric ligands that regulate the function of GPCRs to which they do not bind directly
15:05	Novel Functional Assay Approaches for GPCR Ligand Discovery Rochdi Bouhelal, Research Investigator, Novartis Current and novel approaches utilising functionnal assays in GPCR drug discovery at Novartis will be reviewed. In addition, a case study will be shown.
15:35	Coffee break and networking in exhibition hall
16:15	Integrating Cell-Impedance Technology to Characterize GPCR Modulators in Drug Discovery Oliver Nayler, Director, Head Molecular Biology, Actelion Pharmaceuticals Based on case studies, the application of cell-electrode impedance measurements as a label-free cell based assay to study cell signalling of the natural ligand or small molecular weight GPCR modulators in comparison with standard assays will be discussed.
16:45	Pharmacological Tools to Modulate GPCR Function: “Promises and Challenges for Drug Discovery and Lead Optimization” Evi Kostenis, Professor, Department of Molecular, Cellular and Pharmacobiology, Institute for Pharmaceutical Biology, University of Bonn A series of examples will be given clearly demonstrating that it is not advisable to rely on single assay technologies but rather on a repertoire of assays covering both G protein-dependent and –independent signals.
17:15	Using the 7TM BRET2 Assay for 7TM Receptor Compound Screening Anders Heding, Head of Molecular Screening, 7TM Pharma A/S The improved BRET2 beta-arrestin based assay has been implemented as the preferred assay at 7TM Pharma. The use of this assay compared to other assays will be discussed and examples from several screening campaigns described.
17:45	Advances in Bioluminescent Assays for G-Protein-Coupled Receptors Frank Fan, Group Leader, Promega Corporation Three bioluminscent GPCR assays will be described and compared : a luciferase reporter assay, a cAMP in vitro quantitation assay and a live cell cAMP assay.
18:15	Drinks reception compliments of Bioimage
14:20	Track B - Protein Kinases Chaired by Tim Hammonds
14:25	LANCE Ultra & SureFire - New Tools to Solve the Kinase Conundrum Krystyna Hohenauer, Screening Reagents Product Leader Europe, PerkinElmer Life and Analytical Sciences
14:55	Inhibitors of Protein Kinase D as Antitumour Agents Tim Hammonds, Head of Biochemistry and HTS, Cancer Research Technology Protein Kinase D enzymes are involved in the stimulation of cancer cell proliferation and protection from apoptosis. This presentation will describe the HTS of PKD at CRT and the subsequent development of low nanomolar PKD inhibitors through to preclinical studies.
15:25	Coffee break and networking in exhibition hall
16:10	Development & Validation of a Universal Assay for Metalloproteases: Applications to Protein Biochip Screening Technology Hakim Djaballah, Director, Memorial Sloan Kettering Cancer Center (MSKCC) Mammalian proteolytic enzymes regulate diverse biological processes such as cell death, proliferation, migration, invasion and protein turnover. In search of a strategy on how to screen for specific inhibitors of metalloproteinases, an FP assay using a novel probe has been developed, which is shown to bind to most metalloproteinases.
16:40	The Human MAP3 Kinase COT – A Case Study of Assay Development for High-throughput Screening and Hits Follow-up Characterization Yong Jia, Senior Scientist, Abbott Laboratories The development of various in vitro COT assays and the applications of each assay format for HTS, hits confirmation and analysis, and inhibitor mechanistic studies will be described to demonstrate the critical impact of in vitro assay development and validation on the drug discovery process.
17:10	High Content Screening of Protein Kinases using Microplate Cytometry Sarah Payne, Product Manager, TTP LabTech Limited Protein kinases represent the major target class for oncology research. Microplate cytometry is a proven cell-based technology for the elucidation of protein kinase activity and their role in the regulation of the cell cycle.
17:40	Evaluation of a Homogeneous Approach for the Identification of Kinase Inhibitors, Using b-Galactosidase (b-Gal) Enzyme Fragment Complementation (EFC) assay Pirthipal Singh, Associate Principal Scientist, AstraZeneca Pharmaceuticals A homogeneous binding approach, for the identification of kinase inhibitors, will be described. Inhibition potency data (IC50) will be compared with an assay, developed on the Biacore platform - based on the Surface Plasmon Resonance (SPR) approach.
18:15	Drinks Reception compliments of Bioimage

Day 2 - 21 February

08:30	Track A - Cell-Based Assays Chaired by Stig Linder
08:35	Cellular Screening Technologies for G Protein-Coupled Receptors Hans Pirard, European Technology Manager, PerkinElmer Life and Analytical Sciences Several of the latest advances in liquid handling, detection and reagent approaches to GPCR and high throughput cellular screening developed by PerkinElmer will be presented.
09:05	Methodologies for a High Throughput Cell Based Proliferation Assay System for Lead Compound Characterization and Oncology Drug Combination Studies Ronald Wegrzyn, Assistant Director, GlaxoSmithKline A novel system has been developed to characterize GSK's drug candidates extending from the screen implementation and validation, technology development including custom instrumentation and software as well as custom methodologies for the data flow/management with parameters for combination drug effects.
09:35	Screening for Apoptosis-Inducing Drugs: Biomarker Concept for Anticancer Drug Development Stig Linder, Professor of Experimental Oncology, Karolinska Institute The M30-Apoptosense assay quantifies accumulation of a caspase-cleaved protein specific for epithelial cells. The assay provides an integrated measure of apoptosis and can be used for screening 3-D cultures. The assay can be used as a blood biomarker assay in pre- clinical and clinical studies.
10:05	Pathway Screening with Protein Translocation Assays - Identification of Both Traditional and Previously Intractable Drug Targets Michael Brown, Head of Sales & Market Development (Europe), Thermo Fisher Scientific
10:35	Coffee break and networking in exhibition hall
11:20	Novel Sensitive, Homogeneous Assay for Antibody-Receptor Interactions Arnout Gerritsen, Senior Manager, Lead Identification, Genmab Therapeutic effects of antibodies can be influenced by specific antibody receptor interactions. Using a new cellular detection system we have developed a novel sensitive homogeneous assay which enables us to investigate the effect of antibodyreceptor complexes and facilitate selection of therapeutic antibody candidates.
11:50	Microsphere Mediated Sensing and Cellular Delivery Rosario Sanchez-Martin, Research Fellow, University of Edinburgh This presentation details the last adventures in the use of multifunctionalized microspheres to deliver "cell-impermeable" molecules such as drugs, sensors, proteins and oligonucleotides.
12:20	LanthaScreen™ GFP Cellular Kinase Assays: Biochemical Assays with Biological Relevance John Printen, Cell Signaling Business Segment Director, Invitrogen Screening with purified components means sacrificing the ability to interrogate a kinase of interest within the complex cellular milieu where it functions. TR-FRET assays have recently been developed to monitor phosphorylation of specific target proteins within the native cellular environment.
12:50	Lunch and networking in exhibition hall
13:50	Poster Viewing
14:50	Track A - Bioinformatics Chaired by Karol Kozak
14:55	Advanced Data Analysis for Hit and Lead Identification in Cell Based Assay Stephan Heyse, General Manager, Genedata Screener, Genedata This case study pinpoints the importance of a highly effective high-content screening and data analysis process and demonstrates its value by substantially enhancing the hit verification rate.
15:25	Screening Image Browser: Database and Tool for the Integration, Browsing and Analysis of Large Scale Image High-Content Screening Data Karol Kozak, IT-Specialist, Max Planck Institute of Molecular Cell Biology and Genetics High-Content Screening (HCS), applying automated microscopy, requires a system which is capable of storing and analyzing vast amounts of image and numeric data. We present bioinformatics solution as well as an image retrieval mechanism for browsing and analyzing screening information.
15:55	Coffee Break and Poster Award Ceremony
16:25	Power in Numbers: Low Resolution High Content Image Analysis Berend Snijder, PhD Student, Swiss Federal Institute of Technology Zurich A novel and flexible single cell scoring algorithm was applied in our efforts to map the human genes required for infection of a broad range of viruses. This algorithm and its application in HT screening will be discussed.
16:55	High Throughput Imaging with the Open Microscopy Environment Bernd Jagla, Research Scientist, Columbia University The data model and an example of how to integrate the data model and OME in an HTS environment will be presented. This will include the integration of automated image analysis and quality control workflows.
17:25	Close of conference
10:00	Track B - Label-Free Detection Chaired by John Comley
10:05	Rapid Kinetic-Based Screening of Fab Fragments for Lead Identification Marc Vanhove, Associate Director, Dyax S.A. An integrated approach to produce, purify and affinity-rank up to 200 soluble Fab fragments per week has been developed to allow the analysis of all unique isolates from a selection campaign, increasing the likelihood of identifying a potent and specific binder and reducing the need for time and labor intensive rounds of affinity maturation.
10:35	Coffee break and networking in exhibition hall
11:20	Electrical Impedance Measurement of Cell Adhesion and Cell-Mediated Cytotoxicity Anker Hansen, Principal Scientist, Novo Nordisk A/S Electrical impedance measurements is a real-time and label-free method for monitoring cells in vitro, e.g. adhesion, morphology and viability (death) and can be used for research and screening purposes.
11:50	Characterization of Therapeutic Antibodies Derived from a Novel Yeast Expression Platform Using Bio-Layer Interferometry (BLI) Leon Garcia-Martinez, Associate Director, Alder Biopharmaceuticals Monoclonal antibodies have emerged as an important drug class. They provide both great specificity with low side effects and very fast development times. New technologies in the identification and production of monoclonal antibodies for therapeutic applications will be reviewed.
12:20	Investigation of Drug Interactions with Cation Transporters Using a Solid Supported Membrane Francesco Tadini, Research Associate, University of Florence By employing a solid supported membrane the activity of electrogenic membrane proteins is detected directly by means of an electrical measurement. This method allows to investigate the interactions of compounds of pharmacological interest with ion pumps and transporters.
12:50	Lunch and networking in exhibition hall
13:50	Poster Viewing
14:50	Label-free Detection (continued)
14:55	Fragment-Based Lead Discovery by SPR Imaging of Chemical Microarrays Renate Sekul, VP R&D, Graffinity Pharmaceuticals GmbH Fragment-based lead discovery offers an alternative approach to high-throughput screening. Surface plasmon resonance (SPR) imaging of chemical libraries immobilized on chemical microarrays allows the detection of even weak interactions and is therefore particularly suited for fragment screening.
15:25	Grating-Based Resonance on Microtiter Plates Applied to Screening and Characterization of Small Molecule Ligands Julio Martin, Manager,Screening and Compound Profiling, GlaxoSmithKline SRU BINDTM is a label-free platform based on colorimetric resonance reflection. It quantitatively detects binding of various size molecules or cells. The system is amenable for the screening of a pilot compound library in DMSO, and the detection of cellular responses to external stimuli.
15:55	Coffee Break and poster award ceremony
16:25	A Physiological Approach to GPCR Screening Using a Label-Free Cell-based Platform Dave Laughton, Associate Principal Scientist, Lead Generation Biology, AstraZeneca Data will be presented on some examples of recombinant and endogenous GPCRs profiled on the CellKey™ platform. Additional studies will be described for an orphan GPCR and for some non-GPCR targets.
16:55	Rapid, Label-Free Screening and Affinity Ranking of Fragment Libraries Binding Selectively to Drug Targets Stefan Löfås, VP, Chief Scientific Officer, Biacore International SPR biosensors have now been validated for fragment screening and with a throughput of 1400 fragments/day/10 µg of protein they have been recognized as an important primary screening technique for use as the first step in a fragment screening campaign.
17:25	Close of conference