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- W4283168912 abstract "Thiosulfinates in situ formed by “pharmacological pair” C115H methionine γ-lyase/S-(allyl/alkyl)-l-cysteine sulfoxides possess cytotoxic activity against various malignant cell lines. To investigate in vivo antitumor activity of thiosulfinates generated directly at the surface of tumor cells, a chemical conjugate between Clostridium novyi C115H methionine γ-lyase (C115H MGL) and isoflavone daidzein was prepared. The binding of conjugate (C115H-Dz) to various breast cancer cell lines was demonstrated, as well as its cytotoxicity in the presence of S-(allyl/alkyl)-l-cysteine sulfoxides. The most promising among thiosulfinates was dipropyl thiosulfinate (IC50 < 0.53 μM). The pharmacokinetic parameters of C115H MGL and C115H-Dz were obtained. Plasma half-lives of the enzyme and conjugated enzyme were 4.4 and 7.2 h, respectively. In vivo antitumor effect of pharmacological pairs on SKBR-3 xenografts was demonstrated. Treatment of tumor-bearing mice with a pair of C115H-Dz/propiin inhibited tumor growth by 85%." @default.
- W4283168912 created "2022-06-21" @default.
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- W4283168912 date "2022-10-01" @default.
- W4283168912 modified "2023-10-18" @default.
- W4283168912 title "Daidzein-directed methionine γ-lyase in enzyme prodrug therapy against breast cancer" @default.
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- W4283168912 doi "https://doi.org/10.1016/j.biochi.2022.05.007" @default.
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