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.
| Originalsprog | Engelsk |
|---|---|
| Tidsskrift | International Journal for Parasitology |
| Vol/bind | 40 |
| Udgave nummer | 13 |
| Sider (fra-til) | 1477-1481 |
| Antal sider | 5 |
| ISSN | 0020-7519 |
| DOI | |
| Status | Udgivet - 1 nov. 2010 |