Selcia Limited has announced that it has entered into a new collaboration with Heptares Therapeutics Limited to discover fragment ligands that specifically bind to a Family B stabilized GPCR (StaR®) drug target purified by Heptares.
This follows the successful conclusion of an initial proof-of-concept study using a Family A StaR®.
Selcia will initially develop a screening assay and then apply its novel CEfrag™ drug discovery technology to confirm hits already obtained by Heptares and to screen its proprietary fragment library against the Heptares target.
Selcia’s CEfrag™ platform utilizes capillary electrophoresis technology to identify fragment compounds that selectively bind to drug targets.
All reagents are in solution and no tethering of the protein is required, enabling near physiological ligand/target interactions to be observed with a low false positive rate.
As well as stabilized GPCRs, CEfrag™ can be used to detect fragment/target interactions across a wide range of other target classes including “challenging” targets such as protein-protein interactions.
“We are delighted that Heptares has selected Selcia to carry out the screening of this new GPCR drug target using Selcia’s CEfrag™ platform which has been made possible with Heptares’ StaR technology” said Simon Saxby, CEO of Selcia Limited.
Saxby continued, “We are looking forward to identifying novel fragment compounds against this new target and to continuing our collaboration with the scientists at Heptares.”
Dr Miles Congreve, Head of Chemistry at Heptares Therapeutics, commented, “As Selcia’s CEfrag™ fragment screening platform does not require tethering of the drug target this makes it a very powerful technology to screen drug targets like GPCRs and in particular to StaRs®. This screening technology could be a valuable additional tool as part of a comprehensive structure-based drug discovery capability. We therefore look forward to working with Selcia and building upon our already successful relationship.”