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This workshop will provide an overview of potential solutions to the problems currently faced in protein-protein interaction drug discovery programmes, with a focus on some specific proven technologies. In the discussions, we also aim to cover some actual examples with the lessons learned.  Recent evidence has demonstrated that specific interactions between proteins are integral to all cellular signalling processes.  Misplaced signalling events and mutant proteins lead changes in key protein-protein interactions, and have been shown to play fundamental roles in a range of disease processes. The ability to specifically disrupt or modulate these interactions in discrete subcellular locations, presents a new opportunity to target cellular signalling components involved in disease associated pathways. By
only disrupting the protein complex involved in the disease state, potential side effects often found with inhibitors targeting
enzyme, receptor or channel functions may be avoided.  Due to the nature of the interactions, identifying small molecule disrupters that are functional in a cellular environment has proved difficult. There are however, an increasing number of novel technologies being developed to address these problems.

Workshop programme

8:30 Registration & Coffee

9:00 Chairman's Opening Remarks

Simon MacKenzie

Simon MacKenzie, Head of Laboratories, Scottish Biomedical

9:10 ADVANCES IN PROTEIN AND ANTIBODY STRUCTURAL MODELLING

  • Use of a rich rotamer library and a Unary Quadratic Optimisation algorithm to address protein sidechain predictions in homology modelling

  • Specific techniques for homology modelling of antibody structures; knowledge-based domain-specific libraries and canonical methods; loop grafting to produce chimeric templates

  • Validation examples

  • Susan Boyd

    Susan Boyd, , Chemical Computing Group

    Steve Maginn

    Steve Maginn, Director, Scientific Services, Chemical Computing Group

    10:00 ADDRESSING PROTEIN-PROTEIN INTERACTIONS FOR GPCR, KINASE & NHR DRUG TARGETS USING A COMPLEMENTATION-BASED TECHNOLOGY SUITABLE FOR CELL-BASED HIGH THROUGHPUT SCREENING

    Keith Olson

    Keith Olson, Vice President R&D, DiscoveRx

  • The use of enzyme-based complementation
    assays versus conventional methods
  • Protein-protein interactions, directly addressing
    cellular events at the target protein of interest
  • GPCR targets, directly measuring receptor activity
  • NHR targets, a focus on nuclear translocation
    and binding to co-regulator proteins
  • Receptor tyrosine kinases, using the protein
    interaction between the active RTK and SH2-
    domain containing proteins
  • 10:50 Morning Coffee

    11:20 TARGET VALIDATION TO SMALL MOLECULE BLOCKER IDENTIFICATION: NOVEL APPROACHES TO PROTEIN-PROTEIN INTERACTION DRUG DISCOVERY

    Simon MacKenzie

    Simon MacKenzie, Head of Laboratories, Scottish Biomedical

  • Assessment of protein-protein interaction
    target validation approaches
  • Assay development first steps, is the target
    interaction druggable?
  • Defining successful assay strategies
  • Comparing cell free and cell based approaches
  • Hit confirmation and deconvolution
  • 12:10 DISCUSSIONS, QUESTIONS AND PROBLEMS FROM THE AUDITORIUM

    12:30 Close of Workshop

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    Copthorne Tara Hotel

    Scarsdale Place
    Kensington
    London W8 5SR
    United Kingdom

    Copthorne Tara Hotel

    The Copthorne Tara Hotel London Kensington is an elegant contemporary four-star hotel in prestigious Kensington, located just a two minutes walk from High Street Kensington underground station, making exploring easy. The hotel offers well-appointed and comfortable guest rooms combining Standard, Superior and Club accommodation. Club rooms offer iconic views over the city and include Club Lounge access for complimentary breakfast and refreshments. Guests can sample the authentic Singaporean, Malaysian and Chinese cuisine at Bugis Street, traditional pub fare at the Brasserie Restaurant & Bar or relax with a delicious drink at West8 Cocktail Lounge & Bar.

    The Copthorne Tara Hotel boasts 745 square meters of flexible meeting space, consisting of the Shannon Suite and the Liffey Suite, ideal for hosting conferences, weddings and social events. Facilities include access to the business centre 24 hours a day, fully equipped fitness room, gift shop, theatre desk and Bureau de Change. With ample onsite parking outside the London congestion charge zone and excellent transport links via Heathrow Airport, the hotel is the perfect location for business or leisure stays. The hotel is within close proximity to the shops of High Street Kensington, Knightsbridge and Westfield London, Olympia Conference Centre, Royal Albert Hall, Kensington Palace and Hyde Park.

     

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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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