Beta-Lactams and Beta-lactones as activity-based probes in chemical biology

Med. Chem. Commun., 2011, DOI: 10.1039/C2MD00275B, published on 04.01.2012


Med. Chem. Commun., online article


Activity-based protein profiling (ABPP) employs small molecule probes to profile their dedicated targets in complex proteomes. Unlike traditional proteomics which is limited on protein abundance, probes that selectively target the active site of certain proteins are a benign measure of protein activity and provide tools for functional analysis. ABPP probes have largely replaced isotope labelled probes and have demonstrated broad spectrum utility ranging from identification and characterization of disease associated enzymes to drug development. Privileged structures with balanced reactivity are prime candidates for the design of activity-based probes. beta-Lactams and beta -lactones display such privileged structures and have demonstrated unprecedented value as probes. This review provides an overview on beta -lactam and beta -lactone probes and recent advances in their applications in chemical biology.

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