Following the Lead from Nature with Covalent Inhibitors

Chimia
Roman Lagoutte, Nicolas Winssinger

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.

Citations

Dec 18, 2018·Organic & Biomolecular Chemistry·Takahiro MasuyaKenji Watanabe
May 18, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Jacek KędziaTomasz Janecki
Jun 24, 2020·Nature Chemical Biology·Yosuke IsobeDaniel K Nomura
Dec 5, 2020·Future Medicinal Chemistry·Elena De Vita
Feb 5, 2021·Science Advances·Fandi SutantoAlexander Dömling
Apr 1, 2021·Cell Chemical Biology·Hannah Kiely-CollinsGonçalo J L Bernardes
Jun 25, 2021·Chemical Science·Robert J MayerArmin R Ofial
Dec 17, 2019·Journal of the American Chemical Society·John K EatonStuart L Schreiber
Aug 27, 2019·Journal of the American Chemical Society·Xirui HuThomas J Maimone

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