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Heptares Joins Pharma Consortium Applying State of the Art Cryo-Electron Microscopy to Advance Structure Based Drug Discovery
Date:4/4/2016

LONDON, April 4, 2016 /PRNewswire/ --

Heptares Therapeutics ("Heptares"), the wholly-owned subsidiary of Sosei Group Corporation (TSE Mothers Index: 4565), announces it has partnered with four pharmaceutical companies (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, the 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. Detailed information, such as this, 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, pioneer in the field of cryo-EM at MRC-LMB and a co-founder of Heptares, states, "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."

"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," states Peter Fruhstorfer, vice president and general manager of the Life Sciences business, FEI. "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."

Fiona Marshall, Chief Scientific Officer and co-founder of Heptares, said: "The rapid developments in the cryo-EM field are revolutionising our ability to get detailed structures of membrane protein complexes. Cryo-EM has now reached a stage where it can begin to impact structure-based drug design, and Heptares is committed to be at the forefront of these developments."

About Heptares Therapeutics 
Heptares is a clinical-stage company creating transformative medicines targeting G protein-coupled receptors (GPCRs), a superfamily of 375 receptors linked to a wide range of human diseases. Heptares' proprietary StaR® technology and structure-based drug design (SBDD) capabilities enable us to engineer and develop drugs for highly validated, yet historically undruggable or challenging, GPCRs. Using this approach, we are building an exciting pipeline of new medicines (small molecules and biologics) with the potential to transform the treatment of Alzheimer's disease, schizophrenia, migraine, addiction, metabolic disease and other indications.

We have advanced our lead assets - the first-in-class selective muscarinic M1 receptor agonists - from the earliest stages of discovery into clinical development for treating cognitive impairment/dementia in Alzheimer's disease and schizophrenia. Preliminary clinical results confirm the exquisite selectivity of these compounds for the M1 receptor over other subtypes in human subjects, reinforcing preclinical findings. Other proprietary and partnered candidates across multiple indications are progressing towards the clinic.

We have also entered partnerships for our novel candidates and technologies with leading pharmaceutical and biotechnology companies, including AstraZeneca, MedImmune, MorphoSys, Pfizer and Teva.

Heptares is a wholly owned subsidiary of Sosei Group Corporation. For more information, please visit http://www.heptares.com and http://www.sosei.com.

HEPTARES is a registered trademark in the EU, Switzerland, US and Japan;  

StaR® is a registered trademark in the EU and Japan.

About Sosei 
Sosei is a biopharmaceutical company originating from Japan but with global presence. Sosei's primary business model is based on identifying novel and/or differentiated product assets or technology platforms and, through supporting these in preclinical and clinical development and establishing commercial partnerships, advancing new medicines to patients worldwide. For more information about Sosei, please visit http://www.sosei.com.


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