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G-Protein Coupled Receptors are the largest single class of cell-surface receptors and are the site of action for a huge number of clinically relevant drugs, with more than 30% of the drugs currently on the market targeting GPCR function. There has been remarkable progress in the understanding of GPCRs and the role that they play in various pathological states and the therapeutic value of these discoveries should not be under-estimated. The pharmaceutical and biotech industries have been studying these receptors intensively in recent years in order to validate viable targets as a basis for drug development.

SMi’s Conference will provide you with the very latest developments in drug discovery and development, including specific case studies of GPCR-targeted drugs in various stages of development. The Conference aims to provide a forum where developments in this field, in terms of target identification and validation, drug design, assaying and molecular modelling can be discussed and evaluated.

A unique opportunity to learn from leading industry experts including:
· Dr Mark Pausch, Principal Research Scientist, Wyeth Neuroscience Discovery Research
· Dr Andrew Howard, Senior Investigator, Merck
· Kevin Beaumont, Director & Head of Discovery Pharmacokinetics, Dynamics & Metabolism, Pfizer
· Dr Graeme Wilkinson, Team Leader, AstraZeneca
· Dr Kent Bondensgaard, Research Scientist, Novo Nordisk
· Dr Charles Lunn, Research Fellow, Schering Plough Research Institute
· Dr Lijun Wu, Director, Molecular & Cellular Pharmacology, Millennium
· Dr Freddy Heitz, Scientist, Serono

Key benefits of attending:
DRUG DISCOVERY: gain an insight into the latest developments of GPCRs as targets for drug discovery
GPCR ASSAYs: learn about current trends and more predictive assays
INDENTIFYING NEW DRUGS: hear about the integration of new technologies for drug discovery
LIBRARY DESIGN: understand the importance of constructing cost-effective and efficient libraries
RECOGNITION OF PRIVILIGED SUBSTRUCTURES: identify new tools for the design of GPCR ligands

Conference programme

8:30 Registration and Coffee

9:00 Chairman's Opening Remarks

Professor John Davey

Professor John Davey, Professor / Chief Executive Officer, University of Warwick / Septegen

9:10 INTRODUCTION TO G-PROTEIN COUPLED RECEPTORS

Dr David Bailey

Dr David Bailey, Chief Executive Officer, Purely Proteins

The role of GPCRs in signal transduction

9:40 GPCR AS TARGETS FOR DRUG DISCOVERY

Dr Mark Pausch

Dr Mark Pausch, Principal Research Scientist, Wyeth Neuroscience Discovery Research

  • GPCRs as therapeutic targets
  • Development of novel screening methods to identify ligands for GPCRs
  • Activation of GPCRs
  • In vivo targeting design
  • Future prospects
  • 10:20 DETERMINING FUNCTION AND NEW DRUG TARGETS VIA SYSTEMATIC KNOCKOUTS OF ALL KNOWN GPCRS

    Dr Mark Moore

    Dr Mark Moore, Chief Scientific Officer, Deltagen

    Deltagen performs high-throughput gene knockouts in mice

    11:00 Morning Coffee

    11:20 PROGRESS IN IDENTIFYING NEW DRUGS AT GPCRS

    Dr Nigel Beeley

    Dr Nigel Beeley, Vice President & Chief Chemical Officer, Arena Pharmaceuticals

  • Targeting drugs in the therapeutic areas of neuroscience, cardiovascular, obesity and diabetes
  • Using functional genomics to associate GPCRs with different therapeutic end-points
  • Identifying modulators of GPCRs in a ligand-independent manner
  • Activating and enabling screening with orphan GPCRs
  • Tracking all data generated with our ‘in-house’ database
  • How chemistry interfaces with our drug discovery efforts
    A ‘case history’ using all the above
  • 12:00 SEPTECELLS

    Professor John Davey

    Professor John Davey, Professor / Chief Executive Officer, University of Warwick / Septegen

  • Using yeast to isolate individual GPCR signalling pathways
  • Coupling human GPCRs to the yeast signalling machinery
  • Providing an intrinsic control for GPCR activity
  • Uncovering the specificity of G-protein signalling
  • Deorphanisation of human GPCRs
  • Future devevelopments of SepteCells by Septegen
  • 12:40 Networking Lunch

    14:00 IDENTIFICATION OF NOVEL CLINICAL CANDIDATES

    Dr Olivier Valdenaire

    Dr Olivier Valdenaire, Chief Executive Officer, Axovan

  • Target selection process
  • Advantages of focusing on GPCR family
  • Design and screening of the proprietary GPCR-biased library
  • Lead optimisation and further development
  • GPCR-tailored cheminformatics
  • Concrete examples
  • 14:40 TURNING PEPTIDIC G-PROTEIN COUPLED RECEPTOR LIGANDS INTO DRUGS

    Kevin Beaumont

    Kevin Beaumont, Director & Head of Discovery Pharmacokinetics, Dynamics & Metabolism, Pfizer

  • Peptidic GPCR ligands are challenging to drug
  • Potency is achieved with hydrogen bonding, lipophilicity and molecular size
  • Physicochemistry determines oral bioavailability potential
  • The balance of potency and oral bioavailability is a challenge for peptidic GPCRs
  • This presentation will outline the challenge with personal experiences
  • 15:20 Afternoon Tea

    15:40 TOWARDS MORE PREDICTIVE GPCR ASSAYS

    Dr Graeme Wilkinson

    Dr Graeme Wilkinson, Team Leader, AstraZeneca

  • Promiscuity of GPCR-G-protein coupling
  • Agonist specific G-protein activation
  • G protein dependent changes in agonist potency
  • The design of G-protein specific assays
  • Increasing throughput while maintaining fidelity
  • 16:20 CURRENT TRENDS IN GPCR ASSAY AND SCREENING PLATFORMS

    Dr Andreas Scheel

    Dr Andreas Scheel, Head, Applied Assay Development, EVOTEC OAI

  • Binding functional assay systems
  • Trends in fluorescent technologies
  • GPCR focused libraries
  • Trends in internalization assay detection
  • Elimination of false positives/negatives
  • Case studies from uHTS and MTS campaigns
  • 17:00 Chairman's Closing Remarks and Close of Day One

    8:30 Re-registration and Coffee

    9:00 Chairman's Opening Remarks

    Dr Graeme Wilkinson

    Dr Graeme Wilkinson, Team Leader, AstraZeneca

    9:10 LIBRARY DESIGN

    Dr Jackie Macritchie

    Dr Jackie Macritchie, Section Head, BioFocus Dicovery

  • Advantages of focused libraries
  • Tools for the analysis of GPCRs binding environments
  • Approaches to the design of GPCR focused libraries
  • Case Study
  • 9:40 LIBRARIES FOR PEPTIDE-ACTIVATED GPCRS

    Dr John Saunders

    Dr John Saunders, Vice President, Research Chemistry, Neurocrine Biosciences

  • Importance of GPCR-PA
  • Chemistry property space occupied by GPCR-PA ligands
  • The use of BCUT in the design of a focused library
  • Results obtained with an initial designed set
  • Completion of the final library
  • 10:20 RECOGNITION OF PRIVILEGED SUBSTRUCTURES BY GPCRS

    Dr Kent Bodensgaard

    Dr Kent Bodensgaard, Research Scientist, Novo Nordisk

  • Privileged substructures
  • Sequence analysis of class A GPCRs
  • Conservation patterns within the ligand binding pocket
  • Modelling of privileged substructures-GPCR complexes
  • Ligand design based on privileged substructures
  • 11:00 Morning Coffee

    11:20 STRUCTURAL GENOMICS ON MEMBRANE PROTEINS: THE MEPNET APPROACH

    Dr Kenneth Lundstrom

    Dr Kenneth Lundstrom, Chief Scientific Officer, BioXtal

  • Selection of 100 GPCR targets based on ligand availability, drug target applicability and representation of GPCR subtypes and families
  • Subcloning of 100 GPCR targets into 3 expression vectors (E coli, Pichia pastoris and Semliki Forest virus)
  • Overexpression of targets in bacteria (inclusion bodies), yeast and mammalian cell membranes
  • Development of innovative methods for refolding/ solubilization, purification and crystallization in a high- throughput format
  • Expansion of target selection to 100 non-GPCRs including ion channels, transporters, pumps etc
  • 12:00 A GENERALIZED BORN SOLVATION MODEL WITH IMPLICIT MEMBRANE FOR TRANSMEMBRANE PROTEIN STRUCTURE MODELING

    Dr Christoph Schneider

    Dr Christoph Schneider, Scientific Specialist, Accelrys

  • The GBSA/IM method is applicable for minimization and MD simulations of peptides and proteins in a membrane- like environment without a supercomputer
  • The speed and accuracy of the method allows the study of molecular conformation, position and orientation relative to the membrane
  • The result of the validation studies are in agreement with the experimental data
  • 12:40 Networking Lunch

    13:40 FROM 3D STRUCTURE TO LEAD OPTIMIZATION

    Dr Oren Becker

    Dr Oren Becker, Chief Scientific Officer, Predix Pharmaceuticals

  • Structure of G-protein coupled receptors (GPCRs)
  • Modelling the 3D structure of GPCRs
  • 3D-based in silico screening for lead compounds
  • The interaction between lead compounds and the GPCR target
  • 3D-based integrated computational-experimental lead optimization
  • Examples from actual drug discovery programs
  • 14:20 OBESITY, GPCRS AND TARGET PRIORITISATION

    Dr Andrew Howard

    Dr Andrew Howard, Senior Investigator, Merck

  • Disease pathways
  • Potential targets
  • Strategy for prioritisation
  • Examples of GPCRs involved in obesity: detailed case studies
  • 15:00 Afternoon Tea

    15:20 ADENOSINE A3 RECEPTOR

    Dr Charles Lunn

    Dr Charles Lunn, Research Fellow, Schering Plough Research Institute

  • Adenosine biology as target for immune regulation
  • Involvement A3 receptor with TNFa production in mice
  • A3 receptor and histamine release in mice
  • Characterization of functional A3 receptor in human monocyte-derived dendritic cells
  • Potential for adenosine A3 receptor in other therapeutic areas
  • 16:00 MELANOCORTIN-4 RECEPTOR SMALL MOLECULE ANTAGONISTS

    Dr Lijun Wu

    Dr Lijun Wu, Director, Molecular & Cellular Pharmacology, Millennium

  • Role of melanocortins and their receptors in body weight regulation and energy homeostasis
  • Validation of melanocortin-4 receptor (MC4R) antagonists for treating cancer cachexia/wasting disorders
  • Discovery of MC4R small molecule antagonists
  • Characterization and SAR of representative series of MC4R antagonists
  • 16:40 GTPgS BINDING AND DRUG DISCOVERY

    Dr Freddy Heitz

    Dr Freddy Heitz, Scientist, Serono

    Need for a generic functional assay

    17:20 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, SMI 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.

    CPD Certificates

    We can provide a certificate for all our accredited events. To request a CPD certificate for a conference , workshop, master classes you have attended please email events@smi-online.co.uk

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