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Curr Opin Chem Biol. 2011 Aug;15(4):469-74. doi: 10.1016/j.cbpa.2011.02.020. Epub 2011 Mar 14.

Ligand specificity, privileged substructures and protein druggability from fragment-based screening.

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Laboratoire des Sciences Analytiques-UMR CNRS 5180, Université de Lyon, Université Claude Bernard-Lyon 1, Bât. ESCPE Lyon, Domaine scientifique de la Doua, 69622 Villeurbanne cedex, France.


Fragment-based screening has now become an established method for the generation of lead molecules against therapeutic targets. Fragment molecules are simple, low molecular-weight compounds with few chemical functionalities. These characteristics lead to high hit rates for fragment screening as compared to the more classical High-Throughput Screening of drug-like molecules and raise the question of the specificity of fragment molecules. This review analyzes recent outcomes of fragment screenings published in the literature, showing that the specificity of the fragments can be related to their structures and physico-chemical properties. We also discuss both the concept of privileged fragment scaffolds and the role of fragment-based screening in predicting protein druggability, highlighted by recent publications in the field.

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