Cambridge, UK, September 3rd 2010 — Prosarix announces successful completed of EEDA funded program on the development of chiral SAR panels for drug discovery.
Pharmaceutical companies develop biologically active lead compounds using a variety of methods e.g. “rational” approaches (fragment-based discovery, computer-based design) or screening large collections of molecules (HTS – high throughput screening). From an identified “hit”, large numbers of structurally-related compounds are synthesised in order to optimise both the drug-like properties of the molecule and to define the maximum scope of protectable IP.
A recent trend by companies working in this structure activity relationship (SAR) stage of drug discovery is to utilise more complex molecular structures, which typically possess chirality, i.e. the compound can exist in two or more stereospecific forms. As a consequence single isomers are now preferred as building blocks for use during construction of SAR compound series, even at the primary screening stage, since one isomer often results in a different biological effect to its enantiomer.
In October 2009 Prosarix received a Research and Devlopment grant from EEDA (East of England Development Agency) in order to investigate the use of Prosarix’s state-of-the-art computational platform coupled with biocatalytic chemistry methods to specifically design and synthesise a series of single isomer building blocks that will be used to constitute panels for use by medicinal chemists.
Following the analysis and design stages, method development for a number of panels has now been successfully completed. Based on this, Prosarix has raised further financing and production has now started on the EnzaCore™ SAR Explorer Panels, which will be available soon.