Chapter 5: Principles and Applications of Fragment-based Drug Discovery for Chemical Probes
Published:16 Aug 2018
M. Moustakim and P. E. Brennan, in Chemical and Biological Synthesis: Enabling Approaches for Understanding Biology, ed. N. J. Westwood and A. Nelson, The Royal Society of Chemistry, 2018, ch. 5, pp. 114-137.
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Chemical probes are useful tool molecules that allow for interrogation of a given target biomolecule, such as an enzyme or ion channel. Ultimately these tools can be used to ask fundamental questions about the biology surrounding a target and provide early target validation in the drug-discovery process. Fragment-based drug discovery (FBDD) is gaining popularity in the field of chemical probe development owing, in part, to its time- and resource-efficient nature for identifying an initial hit molecule. The following is a collection of reports of the development of chemical probes using a FBDD approach, which highlight its utility in addressing a broad variety of targets.