LifeArc’s scientists have been working on a fresh approach to drug discovery, using a parallel high-throughput application to significantly improve fragment-based screening.

This will potentially enable researchers into antibacterial therapeutics to prioritise and select new targets more effectively. Antibacterial drug discovery is a field with many unique challenges, some of which can be addressed through more reliable target selection. Our team’s novel workflow combines informatics, using the wealth of data coming from consortia investigating structural genomics, with experimental approaches, to enable researchers to carry out evidence-based prioritisation of targets from large sets.

LifeArc scientists developed a proof of concept, applying this technique to a set of antibacterial targets comprising 146 essential genes. Of these targets, 51 were selected and 38 delivered results that allowed the team to rank them by ligandability. The data obtained against these de-risked targets resulted in rapid progression into structurally enabled drug discovery projects, demonstrating the practical value of the fragment-based target screening workflow.

The team’s article on this research, entitled “Fragment-based target screening as an empirical approach to prioritising targets: a case study on antibacterials” featured in the November 2020 issue of Drug Discovery Today. The theme of this issue was “High throughput screening; current biochemical and cell-based approaches”. The article offers both a way ahead for improving future antibacterial drug discovery and a practical case for the increasing importance of informatics as a diagnostic tool. As a particularly promising development in this field, our case study featured as the lead article.

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