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Volumn 19, Issue 1, 2011, Pages 588-594

Peripheral site ligand-oxime conjugates: A novel concept towards reactivation of nerve agent-inhibited human acetylcholinesterase

Author keywords

Acetylcholinesterase; Nerve agent; Oxime; Peripheral site; Reactivation

Indexed keywords

1 (4 PYRIDINIUMALDOXIME) 2 (((2 CHLOROETHOXY) 2 ETHOXY)ETHOXY)ETHANE; 1 (4 PYRIDINIUMALDOXIME) 2 ((2 CHLOROETHOXY) 2 ETHOXY)ETHANE; 1 (4 PYRIDINIUMALDOXIME) 2 (2 CHLOROETHOXY)ETHANE; ACETYLCHOLINESTERASE; LIGAND; OXIME; PYRIDINIUM DERIVATIVE; UNCLASSIFIED DRUG;

EID: 78650720518     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2010.10.059     Document Type: Article
Times cited : (42)

References (41)
  • 28
    • 78650724174 scopus 로고    scopus 로고
    • All biological tests described in this manuscript were performed in triplicate
    • All biological tests described in this manuscript were performed in triplicate.
  • 29
    • 78650721924 scopus 로고    scopus 로고
    • The results of reactivation at other concentrations are depicted in Figure S3 in Supplementary data
    • The results of reactivation at other concentrations are depicted in Figure S3 in Supplementary data.
  • 30
    • 78650725244 scopus 로고    scopus 로고
    • note
    • Interestingly, when sarin-inhibited electric eel AChE was used instead of human AChE, reactivation by HI-6 was poor, whereas the conjugates 1a-c performed comparably as with human AChE, thus dominating HI-6. Graphs of inhibition/reactivation experiments using electric eel AChE are given in Figure S4 in Supplementary data.
  • 31
    • 78650733162 scopus 로고    scopus 로고
    • note
    • More reactivation experiments with varying inhibitors were carried out by Dr. F. Worek (IPT, Germany). The results of these experiments are given in the supporting information (Fig. S5). These results show the same trends (enhanced reactivation of the total construct compared to the parent compounds), but the percentage reactivation is generally somewhat lower. These differences can be attributed to the use of a slightly different method employing erythrocyte hAChE (ghosts).
  • 40
    • 78650744746 scopus 로고    scopus 로고
    • The inhibition curve of propidium iodide is given in Figure S1 in Supplementary data
    • The inhibition curve of propidium iodide is given in Figure S1 in Supplementary data.
  • 41
    • 33947630408 scopus 로고    scopus 로고
    • The idea for conjugation of a peripheral site ligand and a reactivating oxime as a dual site binding reactivator was recently mentioned in the literature. P. Taylor, Z. Kovarik, E. Reiner, and Z. Radić Toxicology 233 2007 70
    • (2007) Toxicology , vol.233 , pp. 70
    • Taylor, P.1    Kovarik, Z.2    Reiner, E.3    Radić, Z.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.