Spin-trapping agent α-phenyl N-tert-butylnitrone binds to trypsin and enhances heparin-induced inhibition of amidolytic activity and structural degradation of the enzyme
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文摘
The effects of heparin on trypsin have recently been demonstrated to involve inhibition of catalytic activity and degradation of the enzyme by means of an oxidative mechanism. The possibility that α-phenyl N-tert-butylnitrone protects heparin-induced radical formation on trypsin was investigated by measuring amidolytic activity and changes in the structure of trypsin in the presence of heparin with and without α-phenyl N-tert-butylnitrone. The results show that α-phenyl N-tert-butylnitrone does not only prevent, but it even significantly enhances effects of heparin on the enzyme. This is due to the unique property of α-phenyl N-tert-butylnitrone, independently of spin-trapping capacity, to modify the trypsin structure by binding irreversibly to the catalytic triad, at sites distinct from those to which heparin binds.

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