Comparative analysis of sensitivity of cholinesterases of different origin to bis-onium reversible inhibitors |
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Authors: | S N Moralev E V Rozengart |
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Institution: | (1) Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, St. Petersburg, Russia |
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Abstract: | Analytical review of the literature data on interaction constant of cholinesterases from different animal (vertebrates and squids) with 45 bis-onium reversible inhibitors forming homologous series with regularly varied structure has been carried out. Values of the competitive, uncompetitive and generalized inhibitor constants are compared. Interspecies and intraspecies differences in sensitivity of ChE are revealed. Results of conformational analysis of the investigated ligand molecules are presented. The data on population of individual conformations are compared with the data on anticholinesterase potency. Conclusions are made on the action mechanism of the investigated compounds and predominant place of their sorption. The presented data are considered from the point of view of comparative biochemistry and in the light of current information about the active center structure of cholinesterases. |
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Keywords: | comparative study cholinesterase active center reversible inhibitors inhibitor specificity |
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