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- W3175604071 abstract "Reversible covalent kinase inhibitors (RCKIs) are a class of novel kinase inhibitors attracting increasing attention because they simultaneously show the selectivity of covalent kinase inhibitors, yet avoid permanent protein-modification-induced adverse effects. Over the last decade, RCKIs have been reported to target different kinases, including atypical kinases. Currently, three RCKIs are undergoing clinical trials to treat specific diseases, for example, Pemphigus, an autoimmune disorder. In this perspective, first, RCKIs are systematically summarized, including characteristics of electrophilic groups, chemical scaffolds, nucleophilic residues, and binding modes. Second, we provide insights into privileged electrophiles, the distribution of nucleophiles and hence effective design strategies for RCKIs. Finally, we provide a brief perspective on future design strategies for RCKIs, including those that target proteins other than kinases." @default.
- W3175604071 created "2021-07-05" @default.
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- W3175604071 date "2021-06-22" @default.
- W3175604071 modified "2023-10-17" @default.
- W3175604071 title "Advance in Reversible Covalent Kinase Inhibitors" @default.
- W3175604071 doi "https://doi.org/10.48550/arxiv.2106.11698" @default.
- W3175604071 hasPublicationYear "2021" @default.
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