The fragment-approach: An update

Fragment-based drug discovery as a source of preliminary hits has become a significant alternative to conventional drug discovery. A large variety of elegant biophysical validation methods such as NMR, X-ray crystallography, mass spectrometry or a combination of these, are used to fully investigate the typically weak binding interactions between fragments and the target of interest. This review discusses the pros and cons of the aforementioned methods, and gives an overview of the most recent reviews and advances in the various techniques, outlining also how clinical candidates have been developed using these technologies.

Section editor:Hugo Kubinyi – University of Heidelberg, Heidelberg, Germany