Fragments: past, present and future

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In this article Mark Whittaker et al. review the origin of the fragment-based drug discovery approach, discuss how it is being applied and the prospects for future development. Futhermore, they illustrate this with examples from their own projects where they have found that information from fragments can inform the optimisation of hits identified by other means (e.g. HTS and/or virtual screening) and vice versa.

They further discuss that fragment information can also be applied to the discovery of ligands for targets that are not readily amenable to structural analysis by experimentation such as GPCRs, particularly through the application of computational modeling methods.

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