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Issue 4, 2012
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β-Lactams and β-lactones as activity-based probes in chemical biology

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Abstract

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. β-Lactams and β-lactones display such privileged structures and have demonstrated unprecedented value as probes. This review provides an overview on β-lactam and β-lactone probes and recent advances in their applications in chemical biology.

Graphical abstract: β-Lactams and β-lactones as activity-based probes in chemical biology

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Publication details

The article was received on 31 Oct 2011, accepted on 22 Dec 2011 and first published on 04 Jan 2012


Article type: Review Article
DOI: 10.1039/C2MD00275B
Citation: Med. Chem. Commun., 2012,3, 408-417
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    β-Lactams and β-lactones as activity-based probes in chemical biology

    T. Böttcher and S. A. Sieber, Med. Chem. Commun., 2012, 3, 408
    DOI: 10.1039/C2MD00275B

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