Transforming fragments into candidates: small becomes big in medicinal chemistry

Stephen Carney

Again, medicinal chemistry features highly in our "Most downloaded" spot. This time we feature the extremely hot topic of fragment-based drug discovery, from some of the most influential experts, based in the Netherlands and the UK

Fragment-based drug discovery (FBDD) represents a logical and efficient approach to lead discovery and optimisation. It can draw on structural, biophysical and biochemical data, incorporating a wide range of inputs, from precise mode-of-binding information on specific fragments to wider-ranging pharmacophoric screening surveys using traditional HTS approaches. It is truly an enabling technology for the imaginative medicinal chemist. In this review, we analyse a representative set of 23 published FBDD studies that describe how low molecular weight fragments are being identified and efficiently transformed into higher molecular weight drug candidates. FBDD is now becoming warmly endorsed by industry as well as academia and the focus on small interacting molecules is making a big scientific impact.

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Medicinal Chemistry


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