Heptares provides Gpcr expertise to new European drug discovery consortium

Consortium supported with over €20 million funding from EU Innovative Medicines Initiative and big pharma

04-Dec-2012 - United Kingdom

Heptares Therapeutics is joining a group of European academic and industry researchers known as the ‘K4DD’ (‘kinetics for Drug Discovery’) Consortium to investigate binding kinetics or ‘kinotypic’ properties of drug-receptor complexes. The five-year program will focus on important drug target classes, such as protein kinases, proteases and GPCRs – with the goal of demonstrating the value of kinotypic information to early drug discovery and to establish kinotype analysis as a routine part of the lead compound optimisation process.      

Heptares will provide stabilised GPCRs (StaRs®) to the consortium, as well as access to expertise and to its broader GPCR discovery platform. In return, Heptares will receive grant funding from the EU, which will enable the Company to develop further its expertise and capabilities in this area.

The K4DD Consortium has been established based on the theory that, to date, drug discovery has focused on drug-receptor binding affinity and selectivity. However, finding new molecules that have high binding affinity and selectivity has not radically increased the chances of those molecules getting to market. New evidence suggests that ‘target residence time’ or the time a drug remains bound to its target may be as important as affinity or selectivity for its clinical effects.

The Consortium has been set up as part of the European Union’s Innovative Medicines Initiative, and is funded with over €20 million from the EU and contributions from members of EFPIA (European Federation of Pharmaceutical Industries and Associations). The Consortium, which will be coordinated by Bayer Healthcare and Leiden University, will include 20 partners with expertise in structure elucidation, bioanalytical technologies, computational drug design and pharmacology from leading academic institutions, biotech companies and pharmaceutical companies across Europe.

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