AUTHOR=van der Zouwen Antonie J. , Witte Martin D. TITLE=Modular Approaches to Synthesize Activity- and Affinity-Based Chemical Probes JOURNAL=Frontiers in Chemistry VOLUME=9 YEAR=2021 URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2021.644811 DOI=10.3389/fchem.2021.644811 ISSN=2296-2646 ABSTRACT=

Combinatorial and modular methods to synthesize small molecule modulators of protein activity have proven to be powerful tools in the development of new drug-like molecules. Over the past decade, these methodologies have been adapted toward utilization in the development of activity- and affinity-based chemical probes, as well as in chemoproteomic profiling. In this review, we will discuss how methods like multicomponent reactions, DNA-encoded libraries, phage displays, and others provide new ways to rapidly screen novel chemical probes against proteins of interest.