Partners aim to take lead in fragment screening

By Wai Lang Chu

- Last updated on GMT

Related tags: X-ray

An $8.8m collaboration between two pharma companies and a leading
university has resulted in a project that uses fragment-based
crystallography and in silico fragment screening for lead

The collaboration aims to develop fragment-based screening technologies, additionally developing and validating an experimental and computational approach to determine binding of low-molecular weight compounds and molecular probes. Through its BioChance programme the German Federal Ministry of Education and Research (BMBF) has awarded Proteros Biostructures and BioSolveIT a three-year development grant. In selecting these companies the German Government aims to gain a perspective of industry requirements paring this off with an academic viewpoint represented by the University of Marburg. Both companies will work in partnership with the research group of Prof. Dr. Gerhard Klebe at the University of Marburg. The eventuality in fusing these points of view is; 'to bridge the gap between the research lab and the marketplace, stimulating prosperity through innovation.' "Today, fragment-based technologies are among the hottest topics in this industry​," says Dr. Christian Lemmen, CEO of BioSolveIT. "The FragScreen project will allow us to further improve and capitalise on our technological basis and to provide the pharma industry with the most advanced applications available. We are very pleased to be able to further extend our lead in this field​," he added. The market for fragment-based drug discovery approaches has enjoyed a period of growth and success worldwide with many organisations eager to capitalise on its efficient pre-screening and X-ray structure analysis process. FBS is well suited to take advantage of the improvements in automation, software and brighter X-ray sources that have become available in recent years. Fragment Based Screening has become the method for searching novel leads in the drug discovery process, the goal of which is to rapidly convert the identified leads into clinical candidates. Binding at active sites is determined using X-ray crystallography to detect difference density in the active site. Using high-throughput crystallographic methods, a large number of fragments can be assessed in a relatively short time; typically 10-100 compounds can be scanned in a day. The method is also sensitive, detecting fragments with a relatively low affinity of 100 µM-10 mM. "We too observe significant interest in the market for fragment-based drug discovery approaches​," said Dr. Torsten Neuefeind, CEO of Proteros Biostructures. "Success strongly depends on a highly efficient and industrialised pre-screening and x-ray structure analysis process, which supports the structure-guided growing of the small fragment compounds​." Germany have been recognised as one of the most active countries in the life sciences policy field with three different policy measures that specifically address this sector. Biotechnology is seen as one of the key technologies for the coming decade and the German government has made a concerted effort in basic research and diffusion of results in this emerging technology area. The 'BioChance' programme provides support for high-risk projects in applied research carried out by young biotechnology firms, preferably in collaboration with universities and/or research institutions. The primary aim of the scheme is to strengthen research in biotechnology and to promote the application of the results of such research. For this purpose, grants are disbursed to successful applicants to subsidise the costs of the research, which should be pre-competitive yet aiming to lead to the development of new commercial products. The average grant has been calculated at just under $1.6m.

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