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
Hauptverfasser: Tat'yanenko, L.V, Dobrokhotova, O.V, Kotel'nikova, R.A, Poletayeva, D.A, Mishchenko, D.V, Pikhteleva, I. Yu, Bogdanov, G.N, Romanova, V.S, Kotel'nikov, A.I
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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.
ISSN:0091-150X