While still a relatively new approach, fragment-based drug discovery (FBDD) has been so successful for identifying ligands for protein targets that it is already widely regarded as representing a sea-change in drug discovery techniques. The strategy involves identifying small, low-affinity ligands (‘fragments') and combining or expanding these to produce larger, higher-affinity ligands.
The major advantage of FBDD over more traditional high-throughput screening is that FBDD provides a more rapid and effective means of identifying ligands for a protein target. It samples chemical space more efficiently than traditional approaches and therefore requires far fewer compounds to be tested to identify suitable ‘hits' as starting points for development. Fragment-based screening provides more ‘developable' compounds than traditional drug discovery approaches, which optimise a high affinity ‘hit'. Most importantly, fragment methods produce lead candidates with physicochemical properties (described by Lipinski's ‘rule of five') that are likely to result in orally bioavailable compounds.
This inaugural Fragment-Based Drug Design Down Under workshop will reflect the rapidly growing interest in FBDD in Australia, with participants from many centres around the country. We are also pleased to welcome three international leaders in this field as keynote speakers.