Fragment-based drug design: combining philosophy with technology.
Fragment-based drug design began more than ten years ago and has been steadily gaining in popularity. This review discusses how fragments have been used to choose druggable targets, and what parameters need to be evaluated if a fragment hit is to be considered a suitable ligand for development. Examples of fragment-based screening from the recent literature are reviewed to highlight the various approaches used, along with the possible application of additional techniques to fragment screening against immobilized targets. Finally, mention is made of two different areas, multi-target drug discovery and selective tumor cell targeting, where fragment-based approaches may play an important role in the future.
Bartoli
Sandra
S
Chemistry Department, Menarini Ricerche SpA, Via Tito Speri 10, 00040 Pomezia, Roma, Italy.
Fincham
Christopher I
CI
Fattori
Daniela
D
D000818:Animals; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D013329:Structure-Activity Relationship; D013678:Technology, Pharmaceutical / Q000379:methods* / Q000639:trends*