4.7 Article

The avermectin/milbemycin receptors of parasitic nematodes

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出版社

ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.pestbp.2021.105010

关键词

Nematode; Ivermectin; Glutamate; Anthelmintic; Macrocyclic lactones

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  1. Loire Valley Institute for Advanced Studies

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Glutamate-gated chloride channels are crucial targets for ivermectin and related compounds in parasitic nematodes. Due to variations in gene family members, it is challenging to extrapolate from Caenorhabditis elegans to parasites. Recent advances in localisation data are helping to understand the mode of action of the drugs and the possible combinations of subunits that form their targets in vivo.
Glutamate-gated chloride channels are the most important target of ivermectin and related compounds in parasitic nematodes. A small family of genes encode subunits of these channels, allowing the assembly of multiple channel subtypes; the subunit composition of most of the native receptors is unknown. The members of the gene family vary between species, making extrapolation from C. elegans to parasites difficult. Expression of recombinant receptors in Xenopus oocytes can identify subunits that have the ability to co-assemble into novel channels, but localisation data, ideally at the single-cell level, is required to confirm that these subunits are expressed in the same cells and tissues. Fortunately, recent advances in this area are starting to make this information available; this information is adding to our understanding of how the drugs act and of the possible subunit combinations that create their targets in vivo.

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