| Title : [The mechanism of anticholinesterase action of acetylene organophosphorus inhibitors] - Brestkin_1992_Bioorg.Khim_18_1067 |
| Author(s) : Brestkin AP , Zhukovskii Iu G , Moralev SN , Rozengart VI , Sochilina EE , Iagodina OV , Vikhreva LA , Godovikov NN , Kabachnik MI |
| Ref : Bioorganicheskaia Khimiia , 18 :1067 , 1992 |
| Abstract : Introduction of the triple bond in the leaving group of the organophosphorus inhibitor molecule gives a sharp raise of the inhibitor activity but does not change principal characteristics of the cholinesterase inhibition mechanism. The reactivation experiments suggest that inactivation of cholinesterases by these compounds occurs due to phosphorylating of the serine hydroxyl by the corresponding phosphoric acid. A close similarity was shown between acetylenic and saturated organophosphorus inhibitors in altering ka upon change of pH and tetraalkylammonium ions action. It is demonstrated that S-alkynyl esters of thioacetic acid are slowly hydrolyzed by acetylcholinesterase and cholinesterase without irreversible inhibition of the enzymes. |
| ESTHER : Brestkin_1992_Bioorg.Khim_18_1067 |
| PubMedSearch : Brestkin_1992_Bioorg.Khim_18_1067 |
| PubMedID: 1445434 |
Brestkin AP, Zhukovskii Iu G, Moralev SN, Rozengart VI, Sochilina EE, Iagodina OV, Vikhreva LA, Godovikov NN, Kabachnik MI (1992)
[The mechanism of anticholinesterase action of acetylene organophosphorus inhibitors]
Bioorganicheskaia Khimiia
18 :1067
Brestkin AP, Zhukovskii Iu G, Moralev SN, Rozengart VI, Sochilina EE, Iagodina OV, Vikhreva LA, Godovikov NN, Kabachnik MI (1992)
Bioorganicheskaia Khimiia
18 :1067