2022
DOI: 10.1021/acschembio.2c00083
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Chemo-Selective Cys–Pen Disulfide for Proximity-Induced Cysteine Cross-Linking

Abstract: Disulfide-rich architectures are valuable pharmacological tools or therapeutics. Besides, a ligand-induced conjugate strategy offers potential advantages in potency, selectivity, and duration of action for novel covalent drugs. Combining the plentiful disulfide-rich architecture library and ligand-induced conjugate via thiol–disulfide interchange would supply great benefits for developing site specific covalent inhibitors. Cysteine–cysteine (Cys–Cys) disulfide bonds are intrinsically unstable in endogenous red… Show more

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