Linked Life Data

11920914

Source:http://linkedlifedata.com/resource/pubmed/id/11920914

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:dateCreated
2002-3-28
pubmed:abstractText
The rates of inhibition of mouse acetylcholinesterase (AChE; EC 3.1.1.7) by paraoxon, haloxon, DDVP and enantiomers of neutral alkyl methylphosphonyl thioates and cationic alkyl methylphosphonyl thiocholines were measured in the presence and absence of AChE peripheral site inhibitors: gallamine, d-tubocurarine, propidium, atropine and derivatives of coumarin. All ligands, except the coumarins, at submillimolar concentrations enhanced the rates of inhibition by neutral organophosphates, whereas inhibition rates by cationic organophosphates were decreased. When peripheral site ligand concentrations extended to millimolar concentrations the extent of the enhancement decreased, creating a well-shaped activation profile. Analysis of inhibition by DDVP revealed that peripheral site inhibitors increase the second-order reaction rates by increasing maximal rates of phosphorylation. These observations suggest that peripheral site ligands are capable of allosterically affecting the conformation of residues in the choline binding site of AChE, thus optimizing the position of the leaving group of uncharged organophosphates during the inhibition reaction.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
0260-437X
pubmed:author
pubmed:copyrightInfo
Copyright 2001 John Wiley & Sons, Ltd.
pubmed:issnType
Print
pubmed:volume
21 Suppl 1
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
S13-4
pubmed:dateRevised
2004-11-18
pubmed:meshHeading
pubmed:year
2001
pubmed:articleTitle
Peripheral site ligands accelerate inhibition of acetylcholinesterase by neutral organophosphates.
pubmed:affiliation
Department of Pharmacology, University of California at San Diego, La Jolla, CA 92093-0636, USA. zradic@ucsd.edu
pubmed:publicationType
Journal Article