A glycine residue essential for high ivermectin sensitivity in Cys-loop ion channel receptors

Lynagh, Timothy and Lynch, Joseph W. (2010) A glycine residue essential for high ivermectin sensitivity in Cys-loop ion channel receptors. International Journal for Parasitology, 40 13: 1477-1481. doi:10.1016/j.ijpara.2010.07.010


Author Lynagh, Timothy
Lynch, Joseph W.
Title A glycine residue essential for high ivermectin sensitivity in Cys-loop ion channel receptors
Journal name International Journal for Parasitology   Check publisher's open access policy
ISSN 0020-7519
1879-0135
Publication date 2010-11
Sub-type Article (original research)
DOI 10.1016/j.ijpara.2010.07.010
Volume 40
Issue 13
Start page 1477
End page 1481
Total pages 5
Place of publication Kidlington, Oxford, United Kingdom
Publisher Elsevier
Collection year 2011
Language eng
Abstract Ivermectin exerts its anthelmintic effect by activating nematode Cys-loop glutamate-gated receptors. Here we show that a glycine residue at a specific transmembrane domain location is essential for high ivermectin sensitivity in both glycine- and glutamate-gated Cys-loop receptors. We also show that ivermectin sensitivity can be conferred on an ivermectin-insensitive receptor by introducing a glycine at this position. Furthermore, comparison of amino acid sequences of ivermectin-sensitive and -resistant receptors reveals that the presence of a glycine reliably predicts ivermectin sensitivity. By providing a means of identifying ivermectin-sensitive receptors, this finding should help in characterising ivermectin-resistance mechanisms and identifying new anthelmintic targets. © 2010 Australian Society for Parasitology Inc.
Keyword Glycine receptor
Glutamate receptor
Chloride channel
Anthelmintic
Macrocyclic lactone
Nematode
Binding site
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2011 Collection
Queensland Brain Institute Publications
 
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Citation counts: TR Web of Science Citation Count  Cited 32 times in Thomson Reuters Web of Science Article | Citations
Scopus Citation Count Cited 32 times in Scopus Article | Citations
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Created: Sun, 28 Nov 2010, 00:04:56 EST