A big and new trend more specific to small molecule drug discovery, is fragment-based drug design (FBDD),” said Molly (a senior scientist at (Sunesis). It has gained increasing popularity among the pharmaceutical and biotech companies because of its ability to access large chemical space using small amounts of compounds—it’s a new paradigm for drug discovery and it has the advantages over conventional bioassay-based, high-throughput screening in that low-affinity fragments with novel structures can be identified as starting points for hit-to-lead chemistry.
Based on this research, the group claims, there is a clear correlation between the size of the molecule and the success of its development. Compounds that are too large tend to be too complex to succeed and suffer high rates of attrition in development. something interesting and. With use of a number of biophysical techniques as screening tools including high-throughput x-ray crystallography (the advantage of giving the best picture of how the fragment sits in the target) and when paired with NMR allows you to create a structure-based lead.
With different companies approaching this new route in different ways like :
- high-throughput x-ray crystallography
- NMR-fragment screening
- fluorescence polarization assay and many other interesting ways like Protien-Protein interactions etc., this field I think have important role to play. Though the approach is still in its nascent stage, hope something to happen in the near future….