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Following the Lead from Nature with Covalent Inhibitors

Published in Chimia. 2017, vol. 71, no. 10, p. 703-711
Abstract Covalent inhibitors are re-emerging as pharmacologically interesting entities with several candidates having received recent approval for therapeutic intervention. Nature has embraced this strategy and many natural products possess mildly electrophilic moieties able to covalently engage a target protein. This review surveys recent case studies for the identification of the target proteins of natural products. While sesquiterpene lactones represent a vast repertoire of covalent inhibitors, they can also be found in other classes of natural products, with sometimes unusual mechanisms to unmask the electrophilic moieties. These examples ought to be inspiring for the development of new biochemical probes and tomorrow's first-in-class drugs.
Keywords Covalent inhibitorsMode of actionNatural productsProtein modificationTarget identification
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Research group Groupe Winssinger
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LAGOUTTE, Roman, WINSSINGER, Nicolas. Following the Lead from Nature with Covalent Inhibitors. In: Chimia, 2017, vol. 71, n° 10, p. 703-711. doi: 10.2533/chimia.2017.703 https://archive-ouverte.unige.ch/unige:101651

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Deposited on : 2018-01-24

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