Modular Approaches to Synthesize Activity- and Affinity-Based Chemical Probes

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.

Keywords: DNA-templated; SuFEx; activity-based probe; affinity-based probe; chemical probe design; iminoboronate chemistry; protein profiling.