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• W2091920457 abstract "Although rare, small molecules that covalently bind one non-enzyme protein could have important applications—for instance, as imaging and therapeutic agents. A newly designed ligand that selectively binds to transthyretin and reacts chemoselectively with a lysine provides enhanced efficacy over a noncovalent analog in inhibiting amyloid fibril formation. A small molecule that could bind selectively to and then react chemoselectively with a non-enzyme protein in a complex biological fluid, such as blood, could have numerous practical applications. Herein, we report a family of designed stilbenes that selectively and covalently modify the prominent plasma protein transthyretin in preference to more than 4,000 other human plasma proteins. They react chemoselectively with only one of eight lysine ε-amino groups within transthyretin. The crystal structure confirms the expected binding orientation of the stilbene substructure and the anticipated conjugating amide bond. These covalent transthyretin kinetic stabilizers exhibit superior amyloid inhibition potency compared to their noncovalent counterparts, and they prevent cytotoxicity associated with amyloidogenesis. Though there are a few prodrugs that, upon metabolic activation, react with a cysteine residue inactivating a specific non-enzyme, we are unaware of designed small molecules that react with one lysine ε-amine within a specific non-enzyme protein in a complex biological fluid." @default.
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• W2091920457 date "2009-12-20" @default.
• W2091920457 modified "2023-10-17" @default.
• W2091920457 title "Chemoselective small molecules that covalently modify one lysine in a non-enzyme protein in plasma" @default.
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• W2091920457 doi "https://doi.org/10.1038/nchembio.281" @default.
• W2091920457 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3107129" @default.
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