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Fragment-based drug design (FBDD) can be considered as the most successful structure-based drug design (SBDD) approach. It includes: (i) identification of low molecular weight fragments as hits, followed by (ii) determination of their binding mode using biophysical methods, such as X-ray crystallography or NMR spectroscopy, just to name a few, and then by (iii) optimization, through evolving or combining (linking) fragments. X-ray protein crystallography is one of the most sensitive biophysical methods used for screening, as it provides detailed structural information of the protein-fragment complexes at the atomic level.

FBDD has evolved significantly over the past 20 years and is now recognized as a good alternative to traditional methods of hit identification and high-throughput screening (HTS). The usefulness in drug discovery of fragment-based approaches is documented by over 30 clinical drug candidates and importantly a few FDA-approved drugs in oncology. The progresses in FBDD approaches are illustrated in this lecture along with success stories of FBDD in drug discovery.

The event starts at 12: 00