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• W4387037401 abstract "Covalent fragment approaches combine advantages of covalent binders and fragment-based drug discovery (FBDD) for target identification and validation. Although early applications focused mostly on cysteine labeling, the chemistries of available warheads that target other orthosteric and allosteric protein nucleophiles has recently been extended. The range of different warheads and labeling chemistries provide unique opportunities for screening and optimizing warheads necessary for targeting non-cysteine residues. In this review, we discuss these recently developed amino-acid-specific and promiscuous warheads, as well as emerging labeling chemistries, which includes novel transition metal catalyzed, photoactive, electroactive, and noncatalytic methodologies. We also highlight recent applications of covalent fragments for the development of molecular glues and proteolysis-targeting chimeras (PROTACs), and their utility in chemical proteomics-based target identification and validation." @default.
• W4387037401 created "2023-09-27" @default.
• W4387037401 creator A5011278193 @default.
• W4387037401 creator A5029796080 @default.
• W4387037401 creator A5045622531 @default.
• W4387037401 date "2023-09-01" @default.
• W4387037401 modified "2023-10-07" @default.
• W4387037401 title "Covalent fragment approaches targeting non-cysteine residues" @default.
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