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Advances in High-Throughput Screening
21 January - 22 January 2004
Advances in High-Throughput Screening
AIMS & OBJECTIVES OF THE CONFERENCE

With increasing industry pressure to produce pharmaceuticals faster and faster, high-throughput technologies are critical to the drug discovery process. The challenge of identifying bioactive compounds in as shorter time as is possible is met by ever advancing screening technologies. The evidence suggests that simply expanding conventional HTS is not sufficient to meet the drug discovery needs of today. However, how does a company select the most appropriate technology for their needs? How are these technologies validated? How can HTS systems be integrated into the business? The purchase and implementation of HTS systems is highly costly. This Conference will take a look at how to get the best return possible on this investment by adopting the right strategies and selecting the right technologies for your business.

A unique opportunity to learn from leading industry experts including:
  • Dr Lorenz Mayr, Technology Programme Head, Lead Discovery Center, Novartis
  • Dr Giuseppe Ciaramella, Assistant Director & Head, Hit Discovery Group, Pfizer
  • Dr Martin Valler, Group Leader, HTS, Boehringer-Ingelheim
  • Dr Jin Li, Director, Chemical Computing, AstraZeneca
  • Dr Dominique Besson, Global Head, HTS Services, Serono
  • Dr Jörg Hüser, Director, HTS Technologies, Bayer Healthcare
  • Dr Everard Pap, Head, Assay Technologies, HTS, Aventis
  • Dr Ulf Boemer, Head, Technology Development, HTS Infrastructure, Schering
  • Dr Jeffrey Weidner, Head, Screen Operations, Eli Lilly

Benefits of Attending:
  • HIGH-THROUGHPUT SCREENING (HTS) & THE PHARMACEUTICAL INDUSTRY: Discover how the industry develops its selection criteria for new HTS technologies
  • TECHNOLOGY PLATFORMS: Evaluate current methods being used for HTS, including in silico, fluorescence, microfluidics and miniaturisation techniques
  • PURCHASE & IMPLEMENTATION OF HTS SYSTEMS: Can these costly systems be justified? How can they be integrated within the company?
  • NEW TECHNOLOGIES AND THE FUTURE OF HTS: Learn about the up and coming practices to improve lead generation
  • KEY INDUSTRY PERSONNEL: Meet the leaders in the field and learn from their experience
  • Conference agenda

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    8:30

    Registration & Coffee

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    9:00

    Chairperson's Opening Remarks

    Dr Paul England

    Dr Paul England, Chief Executive Officer, ProXara Biotechnology

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    9:10

    HIGH-THROUGHPUT SCREENING (HTS) AT THE CROSSROADS

    Dr Lorenz Mayr

    Dr Lorenz Mayr, Technology Programme, Lead Discovery Center Head, Novartis

  • Importance of HTS in the early stages of drug discovery
  • Limitations of current HTS processes and technologies
  • Industrialisation of the HTS lead discovery process
  • Impact of genomics, miniaturisation and new readout technologies
  • Future role of HTS for industrial drug discovery
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    9:40

    HTS AND THE PHARMACEUTICAL INDUSTRY

    Laurie Taylor

    Laurie Taylor, Director, Lead Discovery, Pharmacology Services, MDS Pharma Services

  • Twenty years of ‘more, smaller, faster, cheaper’ HTS and what we have learned
  • Science driven HTS and selection of target-appropriate assay methods: balancing HTS cost, throughput and performance
  • Meeting investor/shareholder/internal expectations of aggressive timelines, milestone delivery and cost containment
  • Recognising which lead discovery activities needlessly divert corporate focus and critical resources away from proprietary differentiators
  • Managing through fluctuating HTS staffing needs, downtime and changing internal priorities
  • Developing selection criteria for new HTS technology acquisition: HTS goals, costs, profit vs capital investment, depreciation and obsolescence
  • HTS outsourcing makes good business sense…case histories
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    10:20

    INTEGRATING HTS TECHNOLOGIES INTO THE SCREENING LABORATORY

    Dr Dominique Besson

    Dr Dominique Besson, Global Head, HTS Services, Serono

  • Number of HTS laboratories
  • The key link in the chain that comprises the new industrialised drug discovery paradigm
  • Integration of HTS within the company
  • Sharing data amongst groups and sites
  • Changes expected within the HTS laboratories
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    11:00

    Morning Coffee

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    11:20

    TRANSLATING ACADEMIC RESEARCH

    Dr Barbara Saxty

    Dr Barbara Saxty, Senior Scientist, Medical Research Council Technology

  • Tapping the wealth of knowledge within MRC units
  • Meeting industry HTS requirements
  • Bridging the gulf: The Assay Development Group
  • Developing ‘intelligent’ screening strategies
  • Case studies
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    12:00

    CURRENT HTS TECHNOLOGIES

    Gareth Williams

    Gareth Williams, Screening Scientist, Pfizer

  • Integration of the EvoScreen platform into Pfizer, Sandwich
  • Benefits and pitfalls of low volume screening
  • Cell based screening using ratiometric readouts on the Evotec system
  • Cell based screening using high content imaging readouts on the Evotec system
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    12:40

    Networking Lunch

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    13:40

    NEXT WAVE HTS TECHNOLOGIES

    Dr Everard Pap

    Dr Everard Pap, Head, Assay Technologies, HTS, Aventis

  • Addressing new business-goals of screening laboratories
  • Successful screening in 50 nanoliter volumes using high density arrays
  • Microfluidics set new quality standards in HTS
  • Secondary screening: filtering the good, the bad and the ugly
  • The relevance of binding assays in compound filtering
  • Surface plasmon resonance: a new technology platform in drug discovery
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    14:20

    HIGH CONTENT SCREENING (HCS)

    Dr Paul England

    Dr Paul England, Chief Executive Officer, ProXara Biotechnology

  • HCS as an approach for easing bottlenecks in target validation and lead optimisation
  • HCS as a primary screening tool
  • Creative use of HCS technology increases the validation and screening of difficult targets
  • The application of HCS technology for screening signalling pathways
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    15:00

    MOVING FROM HTS TO uHTS

    Dr Jörg Hüser

    Dr Jörg Hüser, Director, HTS Technologies, Bayer Healthcare

  • Traditional scaling up assay throughput using laboratory robotics and new assay technologies facilitated demand
  • Fundamental changes to sustain uHTS throughput to >100,000 assays everyday
  • UHTS as a manufacturing process
  • Strategies and steps taken to build uHTS facilities
  • The integration of manufacturing principles, HTS biology and IT infrastructure
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    15:40

    Afternoon Tea

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    16:00

    IN SILICO HTS

    Dr Jin Li

    Dr Jin Li, Director, Chemical Computing, AstraZeneca

  • Overview of in silico techniques
  • Structure-based virtual screening: opportunities, experience and challenges
  • Ligand-based virtual screening
  • Improving virtual screening
    • Better pre-filtering, docking and post-processing
    • Integration of different virtual screening techniques
    • Improved processes
  • Focused approach to lead generation: combining virtual screening and HTS
  • Improving sources of leads: compound collection enhancement
  • Future perspectives: scientific issues, high performance computing and virtual libraries
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    16:40

    IN SILICO DRUG PROFILING

    Dr Andrew Lemon

    Dr Andrew Lemon, Chemistry Products Manager, IDBS

  • A platform for a novel, systemic approach to drug design
  • Models with application in virtual screening and property prediction, complimenting the knowledge of research
  • Extracting the true value of QSAR models in drug discovery
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    17:20

    FLUORESCENCE DETECTION TECHNOLOGIES FOR HTS

    Dr Martin Valler

    Dr Martin Valler, Group Leader, HTS, Boehringer-Ingelheim

  • Importance of homogenous fluorescence methods as tools for HTS technologies
  • Recently developed techniques and their applications
  • Matching optimised fluorophores to specific high-throughput screening in drug discovery
  • Scope and limitations
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    18:00

    Chairperson’s Closing Remarks and Close of Day One

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    8:30

    Re-registration & Coffee

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    9:00

    Chairperson's Opening Remarks

    Laurie Taylor

    Laurie Taylor, Director, Lead Discovery, Pharmacology Services, MDS Pharma Services

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    9:10

    IMPROVING SCREENING DATA ANALYSIS

    Swen Reimann

    Swen Reimann, Business Development Manager, Genedata

  • Large-scale quality assessment, detection and correction of repetitive patterns
  • Efficient analysis of 1000s of dose response curves with robust fitting methods
  • Comprehensive biological and chemical profiling across assays
  • Increasing hit and lead quality with thr cutting edge Genedata™ software system
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    9:40

    HIGH-THROUGHPUT PRIMARY AND SECONDARY SCREENING WITH ONE DETECTION METHOD

    Dr Sherri Millis

    Dr Sherri Millis, Group Leader, Drug Discovery Systems, Research & Development, Pierce Biotechnology

  • Fluoresence-based screening of kinases, phosphatases or proteases
  • Streamlined identification and confirmation of hit compounds
  • Elimination of background from fluorescent and coloured compounds
  • Customised approach to choosing the ideal target substrate
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    10:20

    MICROFLUIDICS WITHIN HTS

    Dr Hugh McManus

    Dr Hugh McManus, Vice President/Sales & Marketing, Nanostream

  • Miicrofluidics: problems and promises
  • Technology to product: bridging the gap
  • An application in high-throughput separations
  • Customer-driven changes to an existing product
  • Applications in chemistry and biochemistry
  • Manufacturing microfluidic systems – economic or costly?
  • The development of a high-throughput separation system: HPLC with speed
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    11:00

    Morning Coffee

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    11:20

    PRACTICAL CONSIDERATIONS FOR AN ASSAY MINIATURIZATION STRATEGY

    Dr Jeffrey Weidner

    Dr Jeffrey Weidner, Head, Screen Operations, Eli Lilly

  • Motivations for miniaturisation
  • Miniaturization issues
  • Trends and techniques
  • Evaluation of miniaturization approaches
  • Consequences of miniaturization
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    12:00

    SPEEDSCREEN

    Dr Hartmut Zehender

    Dr Hartmut Zehender, Laboratory Head, Novartis

  • Proteins with unknown function from genomics and proteins lacking functional assays: do we need to exclude them from HTS?
  • Affinity-based, label-free HTS with MS readout to determine binder molecules from compound libraries
  • Hit validation
  • Example from SpeedScreen campaigns
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    12:40

    Networking Lunch

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    13:40

    RAPID SCREENING OF KNOWN AND ORPHAN GPCR S

    Dr William Thomsen

    Dr William Thomsen, Research Fellow , Arena Pharmaceuticals

  • Drugs acting at GPCRs (G-protein coupled receptors) account for 30% of all the drugs currently on the market
  • CART can be used to activate orphan and known GPCRs so that ligand-independent screens can be rapidly designed and utiized
  • CART allows screening for inverse agonists and agonists simultaneously
  • The Melanophore platform provides a rapid, robust, and general purpose screen for all GPCRs
  • Arena’s GPCR genechip and functional genomics program enables rapid prioritization of GPCRs for screening
  • Several case studies of the success of the CART technology and use of the melanophore screening platform will be presented
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    14:20

    DATA MANAGEMENT IN HTS

    John Helfrich

    John Helfrich, Program Manager, Drug Discovery & Development Group, NuGenesis Technologies

  • Increase in throughputs from 10,000>100,000 per day
  • Current data management practices
  • Data processing, correlation and communication: the decision to proceed
  • Optimal data management platforms
  • SDMS
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    15:00

    IMPROVING YOUR HIT-TO-LEAD PROCESS

    Dr Giuseppe Ciaramella

    Dr Giuseppe Ciaramella, Assistant Director & Head, Hit Discovery Group, Pfizer

  • Importance of alignment with up- and downstream interfaces to HTS
  • Productivity increase in lead discovery
  • Bringing high-throughput methodologies and processes at the forefront of the drug discovery process
  • Efficient selection of lead molecules from the usually high numbers of HTS hits
  • Providing data on key preclinical properties early in the discovery process
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    15:40

    Afternoon Tea

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    16:00

    HIGH-THROUGHPUT FUNCTIONAL GENOMICS FOR TARGET DISCOVERY AND DEVELOPMENT

    Michael Kazinski

    Michael Kazinski, Head, Robotics & Screening, Xantos Biomedicine

  • Proving that DNA, RNA or protein molecule is directly involved in a disease process and thus a suitable target for the development of new therapeutic interventions
  • Target families: GPCRs, kinases and new secreted factors
  • Target validation as the new bottleneck in pharmaceutical discovery
  • Cost effective and efficient modes of target detection
  • Assigning biological functions to genes- innovative HTS approach
  • Future technological advances
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    16:40

    NEW TECHNOLOGIES AND THE FUTURE OF HIGH-THROUGHPUT SCREENING

    Dr Ulf Boemer

    Dr Ulf Boemer, Head, Technology Development, HTS Infrastructure, Schering

  • The future of HTS as determined by various inputs such as company culture and strategies
  • Technologies, diversity and flexibility
  • The drug discovery process as a single entity
  • Modern screener must be capable of operating from multiple perspectives, fluent in biochemistry, data management, instrumentation and process engineering
  • Emerging technologies
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    17:20

    SUPERQUENCHING POLYMER TECHNOLOGY FOR ASSAY TECHNOLOGY OF PROTEIN-PROTEIN INTERACTIONS, KINASES, PROTEASES AND DNA TARGETS

    Dr Duncan McBranch

    Dr Duncan McBranch, Founder & Chief Operating Officer, QTL Biosystems

  • Homogenous platform with amplified sensitivity
  • Propriety patented technology using superquenching polymer technology
  • First commercialised for proteases (BACE, caspase 3, 7, Gamma Secretase) and Kinases (PKA and Phosphates)
  • Distinguished features are:
  • Accelerated development of targets
  • Universal platform
  • No antibodies required
  • No wash steps
  • Mix and read format
  • Robust and adaptable to existing instruments and HTS
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    18:00

    Chairperson’s Closing Remarks and Close of Conference

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