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Lookup NU author(s): Dr Mathew Martin, Professor Jane Endicott, Professor Martin NobleORCiD, Dr Natalie TatumORCiD
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© 2023Fragment-based drug discovery (FBDD) has brought several drugs to the clinic, notably to target proteins once considered to be challenging, or even undruggable. Screening in FBDD relies upon observing and/or measuring weak (millimolar-scale) binding events using biophysical techniques or crystallographic fragment screening. This latter structural approach provides no information about binding affinity but can reveal binding mode and atomic detail on protein-fragment interactions to accelerate hit-to-lead development. In recent years, high-throughput platforms have been developed at synchrotron facilities to screen thousands of fragment-soaked crystals. However, using accessible manual techniques it is possible to run informative, smaller-scale screens within an academic lab setting. This chapter describes general protocols for home laboratory-scale fragment screening, from fragment soaking through to structure solution and, where appropriate, signposts to background, protocols or alternatives elsewhere.
Author(s): Martin MP, Endicott JA, Noble MEM, Tatum NJ
Publication type: Book Chapter
Publication status: Published
Book Title: Methods in Enzymology
Year: 2023
Volume: 690
Pages: 211-234
Print publication date: 17/10/2023
Online publication date: 11/07/2023
Acceptance date: 02/04/2023
Series Title: Methods in Enzymology
Publisher: Academic Press Inc.
Place Published: San Diego
URL: https://doi.org/10.1016/bs.mie.2023.06.021
DOI: 10.1016/bs.mie.2023.06.021
