Heptares joins consortium applying cryo-electron microscopy to structure-based drug discovery

Cryo-EM can reveal the structure of complex molecular assemblies to near atomic level

Heptares Therapeutics is collaborating with Astex Pharmaceuticals, AstraZeneca, GlaxoSmithKline and UCB; the UK Medical Research Council’s Laboratory of Molecular Biology (MRC-LMB); the Nanoscience Centre of the University of Cambridge; and FEI Company, a manufacturer of high performance microscopes, to form the Cambridge-Pharmaceutical Cryo-EM Consortium, the first of its kind worldwide.

The consortium aims to evaluate the potential of an emerging analytical technique, cryo-electron microscopy (cryo-EM), for determining three-dimensional (3D) information about protein structures at the molecular level. Along with traditional methods for structure determination, such as X-ray crystallography and nuclear magnetic resonance spectroscopy, cryo-EM can reveal the structure of complex molecular assemblies to near atomic level.

Such detailed information is expected to improve understanding of the structure and function of proteins under investigation, and thereby advance the design of new drugs targeting specific proteins, such as G protein-coupled receptors.

Richard Henderson, a pioneer in the field of cryo-EM at MRC-LMB and a co-founder of Heptares, said: 'It is delightful to know that the development of cryo-EM, which many people have worked on for many years, has now reached mainstream structural biology. It is particularly satisfying that pharmaceutical companies are keen to evaluate the approach for drug development.'

Peter Fruhstorfer, Vice President and General Manager of FEI, added: 'Cryo-EM 3D models allow us to see and understand the workings of protein-based molecular machines that we could not analyse before because they were too large and complex or were resistant to the preparations required for other techniques.

'The technique was rapidly adopted by leading academic researchers and is now finding its way into early stage discovery and development in the pharmaceutical industry.'

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