Selcia and Heptares Therapeutics Announce New Fragment Screening Collaboration
Partnership to utilise Selcia’s CEfragTM Capillary Electrophoresis Fragment Screening Technology
Ongar, UK and Welwyn Garden City, UK - April 18 2012: Selcia Limited today announced that it has entered into a new collaboration with Heptares Therapeutics Limited to discover fragment ligands that specifically bind to a Family B stabilised 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 CEfragTM drug discovery technology to confirm hits already obtained by Heptares and to screen its proprietary fragment library against the Heptares target.
Selcia’s CEfragTM platform utilises 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 stabilised GPCRs, CEfragTM 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 CEfragTM platform which has been made possible with Heptares’ StaR technology” said Simon Saxby, CEO of Selcia Limited. “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 CEfragTM 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.”
Selcia Limited is a leading worldwide provider of contract research services in integrated drug discovery, fragment based screening, medicinal chemistry and GMP certified 14-C custom radiolabelling services. Founded in 2005, Selcia operates from 3,000 m2 modern facilities with a GLP analytical laboratory, in Ongar, Essex, United Kingdom and Hopkinton, MA, USA.
Selcia’s Discovery division provides integrated drug discovery services to the pharmaceutical and biotechnology industries; these services include medicinal, organic and analytical chemistry, molecular modelling, in vitro biological & ADME/PK screening and fragment screening using its proprietary CEfragTM platform.
Selcia partners its CE fragment screening technology with pharmaceutical and biotechnology companies and has demonstrated the power of CEfragTM by identifying highly potent and drug-like novel ligands with the potential to address major unmet medical needs across a range of therapeutic areas and target classes.
Selcia’s Radiolabelling division is a leader in delivering pure radiolabelled compounds for preclinical and clinical ADME studies.
For further details about Selcia Limited and the CEfragTM technology please contact:
BD Director – Discovery
Phone: +44 1277 367000
About Heptares Therapeutics
Heptares discovers and develops new medicines targeting GPCRs (G-protein-coupled receptors), a super-family of drug targets linked to a wide range of human diseases. We have established R&D collaborations with Shire, Takeda, AstraZeneca, MedImmune and Novartis Option Fund, and have raised $40M in venture financing from MVM Life Science Partners, Clarus Ventures, Novartis Venture Fund and Takeda Ventures. Heptares is an industry pioneer in GPCR structure-based drug design and has built a unique capability for discovering novel molecules that modulate historically undruggable or challenging GPCRs. Our integrated discovery platform includes proprietary technologies for engineering stabilised GPCRs in their natural pharmacological conformations, identifying previously unknown chemistries for GPCR protein-drug interactions, and deploying advanced fragment-based approaches to GPCR target space for the first time. Using this approach, we are generating a broad pipeline of drug candidates for serious CNS and metabolic disorders, including Alzheimer’s disease, Parkinson’s disease, schizophrenia, autism, anxiety & depression, chronic insomnia, addiction and diabetes. For more information, please visit www.heptares.com .