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Dynamic, template-assisted strategies in fragment-based drug discovery

M. Schmidt, J. Rademann – 2009

Fragment-based methods for drug discovery are increasingly popular because they provide drug leads with greater ligand efficiency than conventional high-throughput screening. However, established methods for fragment detection do not address the central question in fragment-based ligand discovery: how can a primary ligand be optimally extended by a secondary fragment? Dynamic screening methods solve this issue by using a protein target as a template for ligand assembly, thus yielding high-affinity binders from low-affinity fragments. This review summarizes recent work on dynamic screening methodology, which resulted in the development of several high-affinity binders for various targets. Strengths and limitations of the published approaches are discussed and possible contributions of dynamic screening methodology to the drug discovery process are highlighted.

Titel
Dynamic, template-assisted strategies in fragment-based drug discovery
Verfasser
M. Schmidt, J. Rademann
Datum
2009
Kennung
10.1016/j.tibtech.2009.06.001
Zitierweise
Trends in Biotechnol. 2009, 27, 512-521
Art
Text
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