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• W3212303670 endingPage "100433" @default.
• W3212303670 startingPage "100433" @default.
• W3212303670 abstract "Irreversible Bruton's tyrosine kinase (BTK) inhibitor drugs are designed to bind covalently to a free-thiol cysteine in the BTK protein active site. However, these reactive drugs bind to off-target proteins as well. In this study, seven BTK-inhibitor drugs containing acrylamide warheads were incubated with human serum albumin (HSA) and analyzed using an LC-MS/MS peptide mapping approach to determine the amino acid sites of drug covalent binding. Significant adduction at the free-thiol cysteine of HSA was only observed for two of the drugs. However, significant adduction was observed for at least four lysine residues. This is just a small percentage of the 59 total lysine residues in HSA. These four lysine residues are likely partially buried, accessible to the drugs, and exist at least partially in a neutral state. The levels of adduction observed in the in-vitro experimental conditions are only indicative of a relative propensity for adduction with the individual lysine residues of HSA, and are not in-vivo predictions. Widespread off-target lysine binding could impact clearance and bioavailability for irreversible inhibitor drugs. However, the extent of the impact on clearance may be limited in comparison to conjugation with glutathione." @default.
• W3212303670 created "2021-11-22" @default.
• W3212303670 creator A5005925664 @default.
• W3212303670 creator A5009432510 @default.
• W3212303670 date "2022-02-01" @default.
• W3212303670 modified "2023-10-03" @default.
• W3212303670 title "BTK-inhibitor drug covalent binding to lysine in human serum albumin using LC-MS/MS" @default.
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• W3212303670 doi "https://doi.org/10.1016/j.dmpk.2021.100433" @default.
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