Heptares and Leadxpro Enter Collaboration on Powerful New Approaches to GPCR Structure Determination for Drug Discovery

Jun 29, 2016, 04:00 ET from Heptares Therapeutics

LONDON and VILLIGEN, Switzerland, June 29, 2016 /PRNewswire/ --

Heptares Therapeutics ("Heptares"), the wholly-owned subsidiary of Sosei Group Corporation (TSE Mothers Index: 4565), and leadXpro AG ("leadXpro"), a new spin off from the Paul Scherrer Institute (PSI), announce a collaboration to employ powerful new approaches for the determination of high-resolution X-ray structures of G protein-coupled receptors (GPCRs) to discover new drug lead compounds.

GPCRs form one of the most important classes of drug targets, and Heptares is the world leader in the use of structure-based methods for GPCR drug discovery. leadXpro has deep expertise in biophysical and structure-based methods including serial crystallography and cryo-electron microscopy (cryo-EM), and applies these new techniques to the discovery and optimisation of innovative lead compounds targeting membrane proteins, such as GPCRs, ion channels and transporters.

In the collaboration, Heptares will use its proprietary platform to generate conformationally stabilised GPCRs (StaR® proteins), which facilitate the formation of protein crystals. The teams will evaluate novel analytical methods for crystals that fail traditional X-ray crystallography techniques, using leadXpro's expertise in high-powered X-ray technology at Swiss Light Source and free-electron laser technology at SwissFEL. This combination of technologies has the potential to accelerate the delivery of structural information for drug discovery efforts.

Michael Hennig, Chief Executive Officer of leadXpro said: "We are excited Heptares has chosen to collaborate with us and to apply leadXpro's unique technological capabilities to complement its StaR® protein and structure-based drug design platform. Serial crystallography with synchrotron and free electron laser technologies push the frontier of membrane protein crystallography. Advantages include enhanced X-ray data collection at room temperature and the ability to generate more than 100-fold redundancy of data, while the ultimate brilliance of the free electron laser enables work with much smaller crystals to produce better resolved 3D structures. In this way we can unlock those membrane proteins that are currently intractable for structure-based drug discovery."

Fiona Marshall, Heptares' Chief Scientific Officer, said: "We are delighted to enter this new collaboration with leadXpro and excited to see if these cutting-edge technologies can generate new insights for structure-based drug discovery with GPCR crystals that prove challenging to standard X-ray crystallography. Serial crystallography and free electron laser technology are powerful new techniques that could open many new opportunities for drug discovery when applied to StaR® proteins. This collaboration is a further demonstration of our commitment to remain at the forefront of GPCR structure based drug discovery."

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, cancer immune-oncology, migraine, addiction, metabolic disease and other indications. We have partnerships for our novel candidates and technologies with leading pharmaceutical and biotechnology companies, including Allergan, AstraZeneca, Kymab, 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 leadXpro AG 

leadXpro is a lead discovery company focusing on membrane protein drug targets. We are committed to the application of biophysical and structure-based methods for the discovery and optimization of next generation lead compounds. leadXpro's technology platform enables structural determination of membrane proteins where classical crystallographic techniques fail, unlocking structure-based drug discovery for challenging targets. We capitalize on the knowledge regarding membrane protein structural biology and facilities of the Paul Scherrer Institute (PSI) with premium access to the synchrotron Swiss Light Source (SLS) and the Free Electron Laser (SwissFEL). Core expertise beyond X-ray include single particle cryo-electron microscopy (cryo-EM) and electron diffraction (ED). For more information, please visit http://www.leadxpro.com  

leadXpro is a registered trademark in the EU, Switzerland, US and Canada.

SOURCE Heptares Therapeutics