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- W2998589099 abstract "This chapter highlights recent advances in ligand-directed labeling and covalent drug design for specific reaction with targeted proteins in a multimolecular biological context. It focuses on their application for in vivo labeling of endogenous proteins in animal models. Targeted covalent inhibitors (TCIs) are compounds that form a specific covalent bond with a target protein and irreversibly suppress its biological function. Michael acceptors are a representative class of warheads in the modern design of TCIs. Along with Michael acceptors, haloacetamides are another important class of warheads for covalent protein modification. Selective covalent modification of endogenous proteins with reactive small molecules has emerged as an indispensable chemical tool in biological research and drug discovery. In the development of TCIs, high target specificity is critically important for increasing the chance of success in clinical trials and to avoid the risk of unwanted side effects." @default.
- W2998589099 created "2020-01-10" @default.
- W2998589099 creator A5058166028 @default.
- W2998589099 creator A5067014553 @default.
- W2998589099 date "2019-12-27" @default.
- W2998589099 modified "2023-10-05" @default.
- W2998589099 title "<scp> <i>In Vivo</i> </scp> Targeting of Endogenous Proteins with Reactive Small Molecules" @default.
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- W2998589099 doi "https://doi.org/10.1002/9783527344406.ch10" @default.
- W2998589099 hasPublicationYear "2019" @default.
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