Integration of fragment screening and library design

Gregg Siegal, Eiso AB, Jan Schultz
2007 Drug Discovery Today  
With more than 10 years of practical experience and theoretical analysis, fragment-based drug discovery (FBDD) has entered the mainstream of the pharmaceutical and biotech industries. An array of biophysical techniques has been used to detect the weak interaction between a fragment and the target. Each technique presents its own requirements regarding the fragment collection and the target; therefore, in order to optimize the potential of FBDD, the nature of the target should be a driving
more » ... for simultaneous development of both the library and the screening technology. A roadmap is now available to guide fragment-to-lead evolution when structural information is available. The next challenge is to apply FBDD to targets for which high-resolution structural information is not available.
doi:10.1016/j.drudis.2007.08.005 pmid:18061882 fatcat:y6hf5zo46fb5bnptlcbwprab2q