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SUMMARY:GPCRs: From thermostabilisation to X-ray structures and Drug disco
 very - Fiona Marshall\, Heptares Therapeutics
DTSTART:20131212T161500Z
DTEND:20131212T180000Z
UID:TALK46163@talks.cam.ac.uk
CONTACT:Scientific Meetings Co-ordinator
DESCRIPTION:The technique of conformational thermostabilisation applied to
  G protein-coupled receptors (GPCRs) was developed in the group of Dr Chri
 s Tate at the LMB.  Heptares Therapeutics was set up in 2007 to utilise th
 is technology for structure based drug design. StaR (Stabilised receptor) 
 proteins are used for biophysical techniques such as surface plasmon reson
 ance and the generation of X-ray structures. We have selected GPCR drug ta
 rgets that were previously intractable to conventional drug discovery appr
 oaches. Chemical starting points are identified by fragment screening and 
 virtual screening and optimised to drug candidates using structure based d
 esign approaches. Computational strategies to analysing GPCR protein struc
 ture features relevant to drug design such as lipophylic hotspots and wate
 r networks will be discussed. A number of case studies will be described i
 ncluding the identification of highly selective M1 agonists for Alzheimer
 ’s disease\, adenosine A2a antagonists for Parkinson’s disease and ore
 xin antagonists for sleep disorders. Most recently we obtained the first s
 tructure of a Class B GPCR\, the CRF1 receptor\, and this is being used as
  a template to identify small molecule drugs for this family of peptide re
 ceptors. 
LOCATION:Max Perutz Lecture Theatre\, Medical Research Council (MRC) (MRC 
 Laboratory of Molecular Biol
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