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Published by: SMI Publishing, Ltd
Published: Jan. 23, 2006
Table of Contents
- Day 1
- 8.30 Registration & Coffee
- 9.00 Chairman's Opening Remarks
- Dr Lorenz Mayr, Executive Director, BioChemical Assay Development & Screening, Novartis.
- 9.10 THE HIGH THROUGHPUT MARKET
- What has been happening?
- Overview of High Throughput Screening (HTS) and
- Its impact on the pharmaceutical industry
- The importance of HTS
- The current opportunities and limitations
- The future of HTS - how will HTS progress over the next 5 years?
- Dr Mary Jo Wildey, Senior Research Fellow; Screening & Compound Logistics Center Team Lead, Johnson & Johnson PRI.
- 9.50 THE APPLICATION OF HTS IN DRUG DISCOVERY
- Making HTS deliver
- Keeping HTS efficient
- Tracking success downstream
- The benefits of HTS-based drug discovery
- Future challenges
- Dr David Keeling, Director, Lead Generation Biology, AstraZeneca.
- 10.30 Morning Coffee
- 10.50 HTS AS AN INTEGRAL PART OF THE EARLY DRUG DISCOVERY PROCESS
- The business of HTS
- Scaling HTS operations to meet organisational requirements
- Successful partnerships across the organisation for HTS success
- Alignment of HTS priorities with discovery goals
- HTS data deliverables that enable rapid progression of projects
- Investing in HTS related technologies that add value
- Dr Jefferson Paslay, Vice President, Screening Sciences, Wyeth Research.
- 11.30 HOW DOES HTS DELIVER VALUE IN LEAD GENERATION?
- The link between HTS, chemoinformatics and lead generation
- Optimising the use of HTS
- Ensuring quality and reproducibility in HTS
- Realising the value and investment of each section
- Developing a high quality hit list
- Setting the proper goals and metrics for HTS
- Dr Frank Brown, Senior Research Fellow, Johnson & Johnson PRI.
- 12.10 LEARNING FROM OUR MISTAKES
- Delivering starting points for successful lead development
- Corporate compound collections, an historic view
- Leadlike, druglike? Enriching corporate compound files
- Success through compound selection
- HTS and ADME
- How our processes drive physico-chemical properties
- Dr Dominique Besson, HTS Services Group Leader, Serono Pharmaceutical Research Institute.
- 12.50 Networking Lunch
- 2.20 HIGH THROUGHPUT SCREENING STRATEGIES FOR DISCOVERING ION CHANNEL DRUGS
- Ion channel HTS
- Types of ion channel high throughput screens
- Configuring fluorescence-based assays
- Methods for triggering ion channel activity in HTS
- Automated electrophysiology
- Types of ion channel high throughput screens
- Configuring fluorescence-based assays
- Methods for triggering ion channel activity in HTS
- Automated electrophysiology
- Dr Gregory Kaczorowski, Senior Director, Ion Channel Department, Merck Research Laboratories.
- 3.00 THE IMPACT OF NEW TECHNOLOGIES ON ELECTROPHYSIOLOGY-BASED SCREENING STRATEGIES FOR ION CHANNEL TARGETS
- Historical strategies
- Introduction of new electrophysiology-based technology
- Role of focused libraries
- Preliminary data
- Dr Andrew Southan, Head, Ion Channel Pharmacology, BioFocus Plc.
- 3.40 Afternoon Tea
- 4.00 IN SILICO SCREENING
- The emergence of screening methodologies
- Reviewing the techniques - ligand and target-based in silico screening
- Protein structure information as a prerequisite for high throughput docking
- Hit-list processing - combining potency and ADMET aspects
- Problems and success stories
- Dr Alexander Hillisch, Director, Medicinal Chemistry & Head, Computational Chemistry, Bayer HealthCare AG.
- 4.40 MICROFLUIDICS
- Global adoption in pharmaceutical screening
- The screening dilemma: more spending, more screening, more technologies have delivered relatively low success
- High throughput or high output? The landscape is changing
- Faster, high fidelity data is the new goal for screeners = less failures in the clinic
- 75% of top pharmaceutical companies have adopted microfluidics to assist the change in screening paradigm - why?
- Mr Jerome LeClercq, European Marketing Manager, Caliper Life Sciences.
- Mr Seth Cohen, Director, Application Sciences, Caliper Life Sciences.
- 5.20 Chairman’s Closing Remarks and Close of Day One
- 5.30 Networking Drinks Reception Sponsored by: Caliper Life Sciences
- Day 2
- 8.30 Registration & Coffee
- 9.00 Chairman's Opening Remarks
- Dr Lorenz Mayr, Executive Director, BioChemical Assay Development & Screening, Novartis.
- 9.10 SCREENING OF PROTEIN-PROTEIN INTERACTIONS VIA HIGH CONTENT BIOCHEMICAL ASSAY TECHNOLOGIES
- Interfering with protein-protein interactions - current challenges/limitations
- Generating new target-specific compound collections: The key requirements
- Impact of novel assay technologies on modern drug discovery with difficult targets
- Ultra-sensitive, multi-mode assay technologies for studying protein-protein interactions
- Success stories on protein-protein interactions from the Novartis Lead Discovery Center (LDC)
- Future directions of miniaturised multi-mode high content biochemical screening
- Dr Lorenz Mayr, Executive Director, BioChemical Assay Development & Screening, Novartis.
- 9.50 HOMOGENOUS ASSAYS FOR PROTEIN-PROTEIN INTERACTION
- Homogeneous protein-protein assays in lead isolation and optimisation
- Case studies for receptor-ligand and antibody-antigen interactions
- Comparison of different assay technologies
- Optimising assays to get the best hits
- How protein-protein assays influence hit to lead attrition
- Philip Newton, HTS Team Leader, Respiratory & Inflammation, Cambridge Antibody Technology.
- 10.30 Morning Coffee
- 11.00 KINASE INHIBITORS
- From hits to leads
- Kinase focussed library - design and value
- Screening and support of the drug discovery approach
- ADME screening
- The selectivity issue
- Dr Doris Hafenbradl, Director, Biochemical Screening, GPC Biotech AG.
- Dr Lars Neumann, Group Leader. Assay Development & Biochemical Screening, GPC Biotech AG.
- 11.40 A MINIATURISED KINASE PLATFORM
- Schering’s approach
- Challenges and benefits
- Impacts on assay development, HTS processes, data quality and compound profiling
- Dr Christian Bergsdorf, Research Fellow, Schering A G.
- 12.20 Networking Lunch
- 1.50 DATA ANALYSIS AND MINING TO FIND THE BEST LEADS
- Experiences from big pharma
- Analysing the data to get more from the assay results
- Using the activity models to drive further library design and synthesis
- Differentiating the compounds and attrition management using biological fingerprints to select candidates to proceed to preclinical and clinical testing
- Dr Jonathan Mason, Executive Director, Molecular Informatics, Structure & Design, Pfizer.
- 2.30 EXTRACTING INFORMATION FROM HIGH THROUGHPUT SCREENING DATA
- Considerations for the setup of data management and analysis processes
- Scientific data as a product: what makes them "good"?
- Converting complex data into useful information: data management and analysis strategies
- Maximising quality: designs, parameters, controls
- Maximising efficiency: automated processing and manual review of large-scale data sets
- Maximising information content: global analysis of potency and high content HTS data
- Mr Stephan Heyse, Project Leader Genedata Screener, Genedata .
- 3.10 Afternoon Tea
- 3.40 NEW TECHNOLOGIES
- A poisoned chalice?
- Possible goals of introducing new technologies in the HTS and early discovery environment
- Quantitative and qualitative benefits
- Identifying the risks and uncertainties
- How can we justify their costs?
- Some practical challenges to prepare for
- Dr Andrew Chadwick, Principal Consultant, Global Analytics & Life Sciences Consulting, PA Consulting Group.
- 4.20 HTS IN GENETIC TOXICOLOGY
- Is early specificity better than late sensitivity?
- The trouble with regulatory genetic toxicology
- Genetic toxicology screening methods
- Toxicogenomics and in silico screening
- Selected CASE studies in genotoxicity screening
- Next in HTS: micronucleus test and human cell biomarkers
- Dr Richard Walmsley, Director, Scientific, Gentronix Ltd.
- 5.00 Chairman’s Closing Remarks followed by Afternoon Tea
- Close of Conference
AbstractIn recent years pharmaceutical R&D productivity has been experiencing decline despite increased research and development spending. Consequently companies have come to rely on the latest screening methods and technologies available allowing researchers to effectively conduct hundreds of scientific experiments at once. Ten years ago high throughput screening was regarded as the potential saviour of drug discovery, but in reality HTS and uHTS have not lived up to their hype- why is this and what can still be achieved with the use of these assays?
SMi’s 4th Annual Conference, High Throughput Screening - The Application of HTS in current and Future Drug Discovery’ will provide attendees with the latest insight into this important application, covering market dynamics, improved technologies and thoughts for the future. Learn how to deal with critical bottlenecks and other issues reducing the efficiency of the drug discovery process through the use and application of better high throughput screening methods and tools. Further the conference will address how HTS-based lead generation can be made to deliver, the benefits of this application and where the industry will be in the next 5 years. Additional key issues to be addressed by leading experts in the industry include, opportunities for in silico screening, the screening of protein-protein interactions and data analysis and mining. A must attend event for those wishing to improve the drug discovery productivity!
Speakers at the 2006 event include:
- Dr Jefferson Paslay, Vice President, Screening Science, Wyeth
- Dr Jonathan Mason, Executive Director, Medicinal Informatics, Structure & Design, Pfizer
- Dr Lorenz Mayr, Executive Director, BioChemical Assay Development & Screening, Novartis
- Dr Gregory Kaczorowski, Senior Director, Ion Channel Department, Merck
- Dr David Keeling, Director, Lead Generation Biology, AstraZeneca
- Dr Mary Jo Wildey, Senior Research Fellow; Screening & Compound Logistics Centre Team Lead, Johnson & Johnson
- Dr Alexander Hillisch, Director, Medicinal Chemistry & Head, Computational Chemistry, Bayer Healthcare
- Dr Dominique Besson, HTS Services Group Leader, Serono
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