Fragment-based drug discovery (FBDD) is a powerful approach that involves the screening of small, low molecular-weight compounds (fragments) to identify potential drug leads[1]. FBDD has gained popularity in the pharmaceutical industry as a way to reduce attrition rates and provide leads for previously intractable biological targets[2].
The FBDD approach typically involves identifying starting points, which are small molecules or fragments that are about half the size of typical drugs. These fragments are then expanded or linked together to generate larger molecules with higher binding affinities[3]. The use of fragments allows for a more efficient screening process and can increase the probability of identifying a binding event[1].
FBDD has several advantages over traditional high-throughput screening methods, including a higher hit rate, the ability to target previously intractable targets, and a reduced risk of generating non-drug-like compounds[4]. FBDD has been used to discover several successful drugs, including vemurafenib and venetoclax[5].
Overall, FBDD is a promising approach to drug discovery that can provide a more efficient and effective way to identify potential drug leads. Its success in identifying several successful drugs highlights its potential as a valuable tool in the pharmaceutical industry.
Sources:
https://drughunter.com/resource/an-introduction-to-fragment-based-drug-discovery-fbdd/
https://www.nature.com/articles/nchem.217
https://pubmed.ncbi.nlm.nih.gov/21695633/