University of Dundee

CLS First to install Biacore 4000 SPR System enabling fast, reliable and cost-effective screening of fragment libraries

15 Jun 2010

CLS First to install Biacore 4000 SPR System enabling fast, reliable and cost-effective screening of fragment libraries

The College of Life Sciences at the University of Dundee announced today that it has become the first facility worldwide to take delivery of Biacore(tm) 4000. Biacore 4000 is a powerful solution for large-scale, label-free molecular interaction analysis in drug discovery, from early screening to characterization. The University of Dundee and spin-out company Kinetic Discovery Ltd will be using the system to focus on developing biophysical fragment based screening methodologies for efficient drug discovery.

Dr Iva Navratilova, Independent Investigator at the College of Life Sciences’ Division of Biological Chemistry and Drug Discovery and founder of Kinetic Discovery, commented: "We are developing biosensor based screening methods that enable us to characterise the kinetics and thermodynamics of molecular interactions. The unprecedented combination of high sample capacity and sensitivity provided by Biacore 4000 means we can now carry out highly accurate screening of our fragment library in only a couple of days, rather than the weeks it would have otherwise taken."

Dr. Navratilova also plans to use Biacore 4000 to continue her work on developing biosensor SPR methods for screening native membrane proteins such as GPCRs, an important class of drug targets. SPR is used to characterise complex kinetic interactions of GPCRs with their natural ligands or low molecular weight inhibitors. The system is designed forlarge-scale parallel interaction analyses, with the capability to analyze up to 4800 interactions in 24hrs, ideal for running biophysical screening campaigns on selected compound libraries.

Structural methods used for fragment screening present several technical challenges, including consumption of large amounts of target protein, and a requirement for high sample concentrations due to the low (typically micromolar to millimolar) affinities exhibited by fragments, which leads to solubility/non-specific binding issues. SPR-based strategies can be designed to overcome many of these issues, providing an efficient, informative complement to structural methods. The kinetic information obtained can then be used to support further compound optimisation efforts.

"We're very excited to be the first facility to install a Biacore 4000 instrument", said Prof. Andrew Hopkins, Chair of Medicinal Informatics and SULSA Research Professor of Translational Biology, at CLS and CEO of Kinetic Discovery: "We believe this reinforces our position as a world leader in the field of SPR based fragment screening, and we look forward to seeing the many benefits the purchase will make to our research efforts."

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