[The effect of ionic strength on reversible inhibition of catalytic activity of acetylcholinesterase by thione phosphonates].
The effect of ionic strength was used to analyze the mechanism of reversible acetylcholinesterase inhibition by three alkoxymethylthionphosphonates. The most considerable realization of the hydrophobic interaction with the surroundings of the enzyme esteratic site was marked for n-butyl derivative (compound I). The replacement of piperidine by morpholine (compound II) resulted in a decrease of the anticholinesterase activity by an order due to enhancement of the inhibitor hydrophilicity. An increase of MgCl2 concentration promotes an enhancement of the uncompetitive component contribution for compound III contrast to compound II. Hydrophobicity of the phosphoryl part of the compound I molecule is balanced under hydrophobic interaction of the heterocyclic "cationic head" with the enzyme anionic site. The break of this equilibrium intensifies the allosteric regulation, on the one hand, and lowers the inhibitor efficiency, on the other hand.
Vaĭburg
G M
GM
Dalimov
D N
DN
Gafurov
M B
MB
Abduvakhabov
A A
AA
Rozengart
E V
EV
D000110:Acetylcholinesterase / Q000378:metabolism*; D002384:Catalysis; D055598:Chemical Phenomena; D002621:Chemistry; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D004912:Erythrocytes / Q000201:enzymology; D006801:Humans; D007202:Indicators and Reagents; D015636:Magnesium Chloride; D009946:Organothiophosphorus Compounds / Q000494:pharmacology*; D009994:Osmolar Concentration; D011189:Potassium Chloride; D012965:Sodium Chloride
D002800:Cholinesterase Inhibitors; D007202:Indicators and Reagents; D009946:Organothiophosphorus Compounds; D015636:Magnesium Chloride; D012965:Sodium Chloride; D011189:Potassium Chloride; D000110:Acetylcholinesterase
Vliianie ionnoĭ sily na obratimoe tormozhenie kataliticheskoĭ aktivnosti atsetilkholinésterazy tionfosfonatami.