London, 23 March 2015. MRC Technology (MRCT) and Cyclofluidic Ltd have announced the successful completion of their collaboration to identify and optimise drug-like molecules with activity against hepsin, a serine protease known to be overexpressed in prostate, breast, kidney, and ovarian cancers and an important target in the fight against cancer.
Cyclofluidic used their proprietary CyclOps™ platform to optimise a micromolar hit to an advanced tool molecule with nanomolar activity against hepsin and >6000-fold selectivity against the counter target uPA, an enzyme with structural similarities to hepsin. These molecules are now being studied by an MRCT academic collaborator at the University of Helsinki’s Translational Cancer Biology Research Program and Institute of Biomedicine in more complex biological assays, to validate the target and form the basis of a drug development programme.
The Cyclofluidic CyclOps™ platform is an innovative technology platform which directly integrates molecule synthesis with biochemical screening. The platform uses an integrated machine learning algorithm to select molecules meeting the required criteria and to allow 24/7 unattended operation. The team has shown that use of the platform reduces timelines for hit to lead optimisation by 50%, from a year to less than 6 months, allowing molecules to progress into pre-clinical studies faster.
Dr Andy Merritt, Associate Director, Chemistry at MRC Technology said: “The Cyclofluidic platform delivered results with great efficiency and the collaboration worked with exemplary effectiveness. We are pleased that this small molecule project has advanced science in the treatment of cancer. Our drug development and commercial expertise enable us to progress and translate scientific discoveries into treatments and technologies that benefit the public.”
Elizabeth Farrant, Chief Business Officer of Cyclofluidic said: “This has been a key collaboration for us to showcase our platform on an important project with one of the world’s foremost medical research charities. We are very proud to have made an early impact on a key area of research with the potential to improve human health.”