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GPCRs: From thermostabilisation to X-ray structures and Drug discovery

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The technique of conformational thermostabilisation applied to G protein-coupled receptors (GPCRs) was developed in the group of Dr Chris Tate at the LMB . Heptares Therapeutics was set up in 2007 to utilise this technology for structure based drug design. StaR (Stabilised receptor) proteins are used for biophysical techniques such as surface plasmon resonance and the generation of X-ray structures. We have selected GPCR drug targets that were previously intractable to conventional drug discovery approaches. Chemical starting points are identified by fragment screening and virtual screening and optimised to drug candidates using structure based design approaches. Computational strategies to analysing GPCR protein structure features relevant to drug design such as lipophylic hotspots and water networks will be discussed. A number of case studies will be described including the identification of highly selective M1 agonists for Alzheimer’s disease, adenosine A2a antagonists for Parkinson’s disease and orexin antagonists for sleep disorders. Most recently we obtained the first structure 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 receptors.

This talk is part of the MRC LMB Seminar list series.

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