Abstract
The effect of galanthamine, tacrine, and oxazyl on phosphorylation of acetylcholinesterase of human erythrocytes by armin and GD-42 (o-ethyl-S-β-ethylthioethyl ester of methylthiophosphinic acid) was studied. In the presence of galanthamine the organophosphorus inhibitors were shown to interact only with the binding site of the enzyme whose anionic region was not occupied by the reversible inhibitor. Tacrine and oxazyl lower the reactivity of the free enzyme and reduce the rate of its phosphorylation.
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Literature Cited
A. P. Brestkin and D. L. Pevzner, Biokhimiya,36, 81 (1971).
R. N. Glebov, G. M. Dolganov, and G. N. Kryzhanovskii, Dokl. Akad. Nauk SSSR,218, 1464 (1974).
G. M. Grigor'eva, Biokhimiya,29, 716 (1964).
G. M. Grigor'eva, Biokhimiya,30, 415 (1965).
V. D. Tonkopii and E. B. Padinker, Byull. Éksp. Biol. Med., No. 4, 100 (1975).
V. D. Tonkopii, V. B. Prozorovskii, and I. M. Suslova, Byull. Ékxp. Biol. Med., No. 8, 947 (1976).
V. A. Yakovlev, Kinetics of Enzymic Catalysis [in Russian], Moscow (1965).
V. A. Yakovlev and R. S. Agabekyan, Molekul. Biol.,2, 859 (1968).
D. E. Koshland, Zh. Vses. Khim. Ova.16, 158 (1971).
H. Lullmann, F. K. Ohnesorge, H. D. Tonner, et al., Biochem. Pharmacol.,20, 2579 (1971).
G. Mooser and D. S. Sigman, Croat. Chem. Acta,47, 265 (1975).
B. D. Roufogalis and E. E. Quist, Molec. Pharmacol.,8, 41 (1972).
G. M. Steinberg and M. L. Mednick, J. Med. Chem.,18, 1056 (1975).
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Tonkopii, V.D., Ardab'eva, T.V. Effect of reversible inhibitors on reactivity of functional sites of the active center of acetylcholinesterase. Bull Exp Biol Med 86, 1331–1334 (1978). https://doi.org/10.1007/BF00800450
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DOI: https://doi.org/10.1007/BF00800450