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Streamlining Drug Discovery with High throughput Screening
18 June - 19 June 2001
Streamlining Drug Discovery with High throughput Screening
The perceived needs of the pharmaceutical industry have changed with time, which in turn has prompted key changes within the industry, in terms of its business strategies and its scientific approaches to drug discovery and development. Indeed, many of the large pharma companies currently face pipeline gaps and must resort to major improvisations as mainstay products go off patent.

For large-scale experimental endeavours to be tractable, a technological shift away from the present-day laboratory is essential. New technology in miniaturisation and automation with the aim of ultra-High Throughput Screening (uHTS) is necessary for the quantum leap in experimental processing power.

Astoundingly, the total world-wide market for HTS products and services was $1.46 billion in the late 90’s and is thought to show a resounding increase in revenues, growing at a compound annual growth rate of 22.5%, well into the 21st century.

With this knowledge in mind our challenge at SAE Media Group was to produce a unique event exploring the advances in high throughput screening. Covering the plethora of new offerings, including novel assays, new formats, new technologies and new instruments, senior level pharmaceutical executives will deliver timely and pertinent presentations within this escalating field.

Conference agenda

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8:30

Registration and Coffee

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9:00

Chairman's Opening Remarks

Dr Silja Petersen-Mahrt

Dr Silja Petersen-Mahrt, , Associate Director, HTS Centre, AstraZeneca

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9:10

HIT TO LEAD PROCESS IN DRUG DISCOVERY

Dr Mervi Vasänge

Dr Mervi Vasänge, Section Manager Biochemistry, Division Biovitrum, Pharmacia

  • To increase the speed of the drug discovery process it is crucial with efficient selection of lead molecules from the usually high numbers of HTS hits
  • This includes providing data on key preclinical properties early in the discovery process
  • The aim is to minimise failures due to unfavourable pharmacokinetics, toxicity or pharmaceutical properties
  • In addition limited SAR work needs to be carried out in order to ensure the pharmacological suitability of the template
  • Examples of the process in projects for phosphatase and GPCR targets
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    9:40

    MINIATURISED CELLULAR ASSAYS FOR HTS

    Dr Peter Tomme

    Dr Peter Tomme, Director, Research and Development, Galapagos Genomics

  • The biological factor in assay development
  • Single pathway or pathway-based assay format
  • Choosing the right detection methodology. Keeping a clear view: importance of image analysis in the decision process
  • Advantages and limitations of an arrayed approach versus pooled screening
  • Current status at Galapagos: examples
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    10:20

    SO WHAT ARE THE BENEFITS OF MINIATURISATION?

    Dr Peter Grandsard

    Dr Peter Grandsard, Associate Director, Research, Information and Automation Techologies, Amgen

  • Miniaturisation at Amgen: business drivers and cost analysis
  • Results from the Amgen - Caliper Technology Access Program
  • Other miniaturisation initiatives at Amgen in the areas of small molecule screening, DNA nalysis, and liquid dosing
  • When is small small enough?
  • Interfacing miniaturised systems with industrial (large) automation
  • Amgen’s wish list
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    11:00

    Morning Coffee

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    11:20

    THE LUMINEX LABMAPTM SYSTEM

    Lehka Patel

    Lehka Patel, Senior Scientist, RWJ Pharmaceutical Research Institute

  • Homogenous (no wash) assay format
  • Non-radioactive
  • Multiplexed assay format
  • Enhanced sensitivity
  • Potential for miniaturisation
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    12:00

    MICROFLUIDICS AND DRUG DISCOVERY

    Dr Hugh McManus

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

  • Microfluidics: problems and promises
  • Developing modular components
  • Applications in chemistry and biochemistry
  • Integrated devices
  • Manufacturing microfluidic systems
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    12:40

    Networking Lunch

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    14:00

    IN-SILICO HIGH THROUGHPUT SCREENING – SHOCK OF THE NEW?

    Dr Lewis Whitehead

    Dr Lewis Whitehead, Computational Chemist, Novartis

  • Pros and cons of ‘wet’ HTS
  • Reviewing in-silico techniques and measuring their impact
  • Experiences in the virtual world
  • The future and potential
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    14:40

    QUANTIFICATION OF GAP JUNCTION FORMATION USING HIGH CONTENT SCREENING SYSTEM

    Dr Zhuyin (Julie) Li

    Dr Zhuyin (Julie) Li, Head of Assay Development, Aventis

  • High Content Screening (HCS) is a new approach for easing the bottlenecks that have formed at target validation, library screening and lead optimisation in the drug discovery pipeline
  • Provision of temporal and spatial information about target function and drug activity at sub-cellular resolution
  • Creatively utilising HCS technology could provide a previously unavailable opportunity to validate and screen some difficult targets
  • Case study: the application of HCS technology in quantifying gap junction formation
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    15:20

    Afternoon Tea

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    15:40

    HIGH-THROUGHPUT PROCESS DEVELOPMENT

    Dr Alan Smith

    Dr Alan Smith, Technology Manager, Pharma and Fine Chemicals, Avantium Technologies

  • Accelerated chemistry benefits greatly from a fully integrated approach
  • Pragmatic s/w tools are becoming available which make this possible when combined with advanced robotics and accessories in a modular fashion
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    16:20

    MAKING THE TRANSITION FROM E-COMMERCE TO E-RESEARCH

    Mark Robillard

    Mark Robillard, Senior Vice President, EMAX Solutions, a SciQuest Company

  • Understand how to achieve optimum levels of research supply chain performance
  • Analyse what technologies can be deployed to optimise the research supply chain
  • Determine the necessary points of integration-within and outside the organisation
  • Recognise the bottlenecks and how to handle them
  • Identify the benchmarks that measure success or failure
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    17:00

    Chairman's Closing Remarks and Close of Day One

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    17:10

    Networking Drinks Reception

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    8:30

    Re-registration and Coffee

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    9:00

    Chairman's Opening Remarks

    Dr John Harris

    Dr John Harris, Technical Director, BioFocus

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    9:10

    ASSAY INNOVATIONS: THE KEY TO OPTIMAL HTS

    Dr Paul England

    Dr Paul England, Senior Scientific Fellow, Aurora Biosciences

  • Streamlining assay development: reducing time to market, increasing efficiency
  • Key considerations: · Knowledge of the biological target · Knowledge of the technical requirements for HTS · Improving quality of reagents and ensuring consistency · Miniaturisation issues
  • Results of highly miniaturised ultra-high throughput assays
  • Trends and enabling technologies
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    9:40

    IN SILICO TECHNOLOGIES FOR DRUG DISCOVERY

    Dr Jin Li

    Dr Jin Li, Director, Chemical Computing, AstraZeneca

  • Drug discovery has become an information-intensive business, even more so in the post genomic era
  • Rapid and reliable distillation of information is of key importance for making quality decisions in compound acquisition, HTS experiments, structure determination and lead exploration
  • In silico screening technologies based on advanced computational algorithms and large scale high performance computing offer many possibilities and potential advantages
  • Examples of recent in silico screening applications will be discussed
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    10:20

    AN UNIQUE AND INTEGRATED MICROARRAY PLATFORM FOR HIGH-THROUGHPUT SCREENING

    Dr Mary Jane Cunningham

    Dr Mary Jane Cunningham, Project Manager, Genometrix

  • Focused gene and protein expression microarrays for screening combinatorial chemistry libraries and optimising lead candidates
  • Gene expression profiles from cell treatments with known pharmaceutical compounds
  • High-throughput genotyping platform that aids in addressing adverse drug effects by screening clinical samples
  • Comparison of N-acetyltransferase genotypes and phenotypes of a diverse population
  • State-of-the art software that allows easy management of large gene expression and genotyping data sets as well as complex statistical and bioinformatic analysis
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    11:00

    Morning Coffee

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    11:20

    AEQUOSCREEN LIGHTS UP HTS

    Michel Detheux

    Michel Detheux, Group Leader Core Technologies, Euroscreen

  • Homogenous cell-based HTS assay
  • Agonists and antagonists screening of GPCRs
  • Screening of orphan GPCRs
  • New measurement devices for 384 well plates
  • Broad potential for other applications
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    12:00

    THE ACUMEN EXPLORER

    DrAdrian Dawkes

    DrAdrian Dawkes, Biosciences Manager, Acumen - A Division of The Technology Partnership

  • Multi-parameter object analysis
  • User defined algorithms
  • Simultaneous multiple wavelength detection capability
  • Live cell receptor binding / function / morphology assays
  • On bead kinase & phosphatase assays
  • Analysis by population with user controllable data collection levels to ensure statistical significance
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    12:40

    Networking Lunch

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    14:00

    HAS THE CHEMICAL INPUT TO HTS BEEN OVERLOOKED?

    Dr David Langley

    Dr David Langley, , GlaxoSmithKline

  • HTS as a driver for building an extensive screening collection
  • What are the options for samples to screen?
  • Relative merits and drawbacks of different sample types
  • How can we improve our collections?
  • Exploiting external sources of compounds and libraries
  • Making best use of internal and external resources
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    14:40

    FROM FUNCTIONAL PROTEOMICS TO DRUG TARGET DISCOVERY: HYBRIGENICS’ CUTTING-EDGE PROTEIN INTERACTION TECHNOLOGY

    Prof Donny Strosberg

    Prof Donny Strosberg, CEO, Hybrigenics

  • Protein-protein interactions are deciphered with unprecedented low rates of false positives and false negatives
  • Interactions are uniquely scored for their reliability (PBS®) and interacting domains are identified (SID®)
  • Functional pathways are reconstituted and resulting protein interaction maps are displayed through a user-friendly navigation and analysis bioinformatics platform: PIMRider®
  • Furthermore, the company’s SID® technology helps validating new therapeutic targets and results in the isolation of SID compounds, i.e. models for drug lead compounds that can be used as: · Dominant negative mutant production for in vivo proof of principle assays · Development of high-throughput screening assays · First step for drug modelling
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    15:20

    Afternoon Tea

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    15:40

    GENOMICS AND PROTEOMICS TOOLS IN DRUG DISCOVERY AND SCREENING

    Dr Scott Hunicke-Smith

    Dr Scott Hunicke-Smith, President and CEO, GeneMachines

  • Genomics tools (sequencing and gene expression) will become bigger parts of drug discovery
  • Microarraying is a rapidly maturing technology
  • Protein expression analysis requires diverse approaches
  • Examples of GeneMachines’ tools and their use in drug discovery
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    16:20

    HIGH-THROUGHTPUT SCREENING WITH INTEGRATED MICROFLUIDIC DEVICES

    Dr William Radany

    Dr William Radany, Vice President, Drug Discovery Programs, Caliper Technologies

  • Lab on a chip
  • Microfluids
  • HTS
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    17:00

    Chairman's Closing Remarks and Close of Conference

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    WHAT IS CPD?

    CPD stands for Continuing Professional Development’. It is essentially a philosophy, which maintains that in order to be effective, learning should be organised and structured. The most common definition is:

    ‘A commitment to structured skills and knowledge enhancement for Personal or Professional competence’

    CPD is a common requirement of individual membership with professional bodies and Institutes. Increasingly, employers also expect their staff to undertake regular CPD activities.

    Undertaken over a period of time, CPD ensures that educational qualifications do not become obsolete, and allows for best practice and professional standards to be upheld.

    CPD can be undertaken through a variety of learning activities including instructor led training courses, seminars and conferences, e:learning modules or structured reading.

    CPD AND PROFESSIONAL INSTITUTES

    There are approximately 470 institutes in the UK across all industry sectors, with a collective membership of circa 4 million professionals, and they all expect their members to undertake CPD.

    For some institutes undertaking CPD is mandatory e.g. accountancy and law, and linked to a licence to practice, for others it’s obligatory. By ensuring that their members undertake CPD, the professional bodies seek to ensure that professional standards, legislative awareness and ethical practices are maintained.

    CPD Schemes often run over the period of a year and the institutes generally provide online tools for their members to record and reflect on their CPD activities.

    TYPICAL CPD SCHEMES AND RECORDING OF CPD (CPD points and hours)

    Professional bodies and Institutes CPD schemes are either structured as ‘Input’ or ‘Output’ based.

    ‘Input’ based schemes list a precise number of CPD hours that individuals must achieve within a given time period. These schemes can also use different ‘currencies’ such as points, merits, units or credits, where an individual must accumulate the number required. These currencies are usually based on time i.e. 1 CPD point = 1 hour of learning.

    ‘Output’ based schemes are learner centred. They require individuals to set learning goals that align to professional competencies, or personal development objectives. These schemes also list different ways to achieve the learning goals e.g. training courses, seminars or e:learning, which enables an individual to complete their CPD through their preferred mode of learning.

    The majority of Input and Output based schemes actively encourage individuals to seek appropriate CPD activities independently.

    As a formal provider of CPD certified activities, SAE Media Group can provide an indication of the learning benefit gained and the typical completion. However, it is ultimately the responsibility of the delegate to evaluate their learning, and record it correctly in line with their professional body’s or employers requirements.

    GLOBAL CPD

    Increasingly, international and emerging markets are ‘professionalising’ their workforces and looking to the UK to benchmark educational standards. The undertaking of CPD is now increasingly expected of any individual employed within today’s global marketplace.

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