To develop covalent inhibitors with high potency and low off-target effects, combinatorial approaches that search for candidates from large libraries are desired. Here, sulfur(VI) fluoride exchange (SuFEx) in vitro selection is established for the evolution of covalent aptamers from trillions of SuFEx-modified oligonucleotides. Through this technique, covalent aptamers with optimally balanced selectivity and reactivity are identified.
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References
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This is a summary of: Qin, Z. et al. Discovering covalent inhibitors of protein–protein interactions from trillions of sulfur(VI) fluoride exchange-modified oligonucleotides. Nat. Chem. https://doi.org/10.1038/s41557-023-01304-z (2023).
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In vitro selection of covalent aptamers with sulfur(VI) fluoride exchange chemistry. Nat. Chem. 15, 1662–1663 (2023). https://doi.org/10.1038/s41557-023-01376-x
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DOI: https://doi.org/10.1038/s41557-023-01376-x