link to BBSRC
 

Structure-Based Drug Discovery
A course for medicinal chemists and discovery biologists

Course Details (details to be reviewed in February 2008)

Monday

Monday Evening :

  • Arrival

Tuesday

Tuesday am :

  • Lecture on the drug discovery context
  • Lecture - Introduction to Protein Structure (including graphics workshop)
  • Lecture - with workshop demonstrations
    • Overview of Protein - Ligand interactions
    • Thermodynamics / Physical Chemistry
    • Computational Methods

Tuesday pm :

  • Lectures on Determining structures and probing interactions
    • Protein production
    • X-Ray
    • NMR
    • ITC
    • SPR
    • Mass Spec
    • Future perspectives
    Interspersed with tours of experimental facilities with demonstrations

Tuesday Evening :

  • Roundtable discussion of first day

Wednesday

Wednesday am :

  • Virtual screening lecture plus graphics workshop
  • Lecture on fragment screening
  • Modelling and design lecture plus workshop

Wednesday pm :

  • Case history projects

Thursday

Thursday am :

  • Case History projects
  • Case History presentations
  • Lunch & Departure

So - what do we mean by a Case History :

  • Attendees are briefed by example on a couple of case histories
    • succinct summary of disease and target
    • strategy adopted to find hit / lead series
    • emphasis on how structure used to inform chemistry
    • brief summary of clinical trials etc
  • Attendees work in teams (2-3 depending on numbers)
  • Each team chooses from a list of possible topics. Examples include :
    • influenze - relenza & tamiflu
    • Factor Xa
    • PPAR
    • p38 kinase
    • PDEIV
    • Hsp90
    • Bcl-xl
  • Use web resources / literature to develop story
  • Produce a powerpoint presentation (10 minutes) summary
  • All presentations will be made available to all delegates

There will be no assessment on the course

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Last Updated: November 30, 2007 | Tim Kirk

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