Fragment-based lead discovery complements high-throughput screening and computer-aided drug design for the discovery of small-molecule inhibitors of protein-protein interactions. Fragments are molecules with molecular masses ca 280 Da or smaller, and are generally screened using structural or biophysical approaches. Several methods of fragment-based screening are feasible for any soluble protein that can be expressed and purified; specific techniques also have size limitations and/or require multiple milligrams of protein. This chapter describes some of the most common fragment-discovery methods, including surface plasmon resonance, nuclear magnetic resonance, differential scanning fluorimetry, and X-ray crystallography.
CITATION STYLE
Pfaff, S. J., Chimenti, M. S., Kelly, M. J. S., & Arkin, M. R. (2015). Biophysical methods for identifying fragment-based inhibitors of protein-protein interactions. Methods in Molecular Biology (Clifton, N.J.), 1278, 587–613. https://doi.org/10.1007/978-1-4939-2425-7_39
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