Effect of nitroxyalkyl derivatives of fullerenylproline on the activity of [Ca.sup.3+]-atpase of sarcoplasmic reticulum
The effect of nitroxyalkyl derivatives of fullerenylproline methyl ester on the enzymatic activity of [Ca.sup.2+]-ATPase of sarcoplasmic reticulum (SR) has been studied. It is shown that hybrid derivatives of [C.sub.60] fullerene are capable of inhibiting the activity of [Ca.sup.2+]-ATPase of SR. Th...
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Veröffentlicht in: | Pharmaceutical chemistry journal 2011-09, Vol.45 (6), p.329 |
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Sprache: | eng |
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Zusammenfassung: | The effect of nitroxyalkyl derivatives of fullerenylproline methyl ester on the enzymatic activity of [Ca.sup.2+]-ATPase of sarcoplasmic reticulum (SR) has been studied. It is shown that hybrid derivatives of [C.sub.60] fullerene are capable of inhibiting the activity of [Ca.sup.2+]-ATPase of SR. The mononitrate inhibits the hydrolytic activity of the enzyme with [K.sub.i]=1.92 x 10 6 M; active [Ca.sup.2+] transport, with [K.sub.i] = 3.79 x 10 6 M. The dinitrate inhibits ATP hydrolysis with [K.sub.i] = 2.38 x 10 8 M; [Ca.sup.2+] transport, with [K.sub.i] = 3.08 x 10 8 M. Fullerenylproline methyl ester does not affect the enzymatic activity of [Ca.sup.2+]-ATPase. Based on these data it is possible to predict the possible fields of application for hybrid fullerene derivatives as potential drugs. Key words: [Ca.sup.2+]-[Mg.sup.2+]-ATPase of sarcoplasmic reticulum, phosphodiesterase of cyclic guanosine monophosphate, fullerenylproline nitrates. |
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ISSN: | 0091-150X |