Dr Peter Simpson, Director of the N8 Research Partnership, has stated that a new automation approach in drug discovery will be “helpful”, though not transformative by itself, in an article by Katharine Sanderson published in May 2015’s edition of Nature Reviews Drug Discovery.
The article ‘March of the Synthesis Machines’, examines what impact will advances in automated chemical synthesis have for medicinal chemists – in light of the development of an automated set-up developed at the University of Illinois to run a wide range of palladium-catalyzed carbon-coupling reactions.
Dr Simpson stated that he sees such automation as an adjunct, which has the potential to help address validated targets which do not currently have chemical leads. It can partly address the top priority chemistry task in drug discovery, which is to find truly innovative small molecules as probe molecules to validate new targets. These probes may be made using more sophisticated chemistry synthesis approaches; and the article notes that the Illinois work represents a welcome redirection of focus away from automation to deliver a plethora of compound scaffolds already over-represented in screening libraries, onto methods for diverse ‘natural-product-like’ molecules.
However, new chemistry probes are likely to be impactful when married to new insights into biological pathways. To maximise the impact of new chemistry, a concerted, interdisciplinary approach to target identification and validation would be enabling, in finding better targets to try these new synthetic approaches on.
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