Comparative Analysis of Sensitivity of Cholinesterases of Different Origin to Bis-Onium Reversible Inhibitors

被引:0
|
作者
Moralev, S. N. [1 ]
Rozengart, E. V. [1 ]
机构
[1] Russian Acad Sci, IM Sechenov Evolutionary Physiol & Biochem Inst, St Petersburg 196140, Russia
关键词
comparative study; cholinesterase; active center; reversible inhibitors; inhibitor specificity;
D O I
10.1134/S0022093008040029
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
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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页码:414 / 429
页数:16
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