2017
DOI: 10.3389/fnmol.2017.00092
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Abstract: The broad-spectrum anthelmintic drug ivermectin (IVM) activates and stabilizes an open-channel conformation of invertebrate chloride-selective glutamate receptors (GluClRs), thereby causing a continuous inflow of chloride ions and sustained membrane hyperpolarization. These effects suppress nervous impulses and vital physiological processes in parasitic nematodes. The GluClRs are pentamers. Homopentameric receptors assembled from the Caenorhabditis elegans (C. elegans) GluClα (GLC-1) subunit can inherently res… Show more

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Cited by 5 publications
(5 citation statements)
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References 155 publications
(208 reference statements)
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“…contortus , such as TM3-G36’ [30] and TM1-P230 [31], and in the α subunit of C . elegans , such as TM1-L279 and TM1-F276 [32, 33]. The glutamate binding site and TM3 domain are also sites that harbour mutations in wild ML-resistant strains of C .…”
Section: Introductionmentioning
confidence: 99%
“…contortus , such as TM3-G36’ [30] and TM1-P230 [31], and in the α subunit of C . elegans , such as TM1-L279 and TM1-F276 [32, 33]. The glutamate binding site and TM3 domain are also sites that harbour mutations in wild ML-resistant strains of C .…”
Section: Introductionmentioning
confidence: 99%
“…This hypothesis is consistent with the results from the non-Ala substitutions which revealed aromaticity was needed for the residue at position 284. Aromaticity here is conserved across equivalent residues in other GABA A R subunits and in most pLGICs ( Figure 3 ), and mutation to Ala of this residue in GluCl (F276A) and GlyR (Y233A) yields non-functional receptors, while substitution to another aromatic does not [ 20 , 21 ]. Thus, these π–π and/or CH–π interactions with the Cys-loop Pro are likely conserved and critical for receptor function in the whole pLGIC family.…”
Section: Discussionmentioning
confidence: 99%
“…Однако авермектины безопасны для млекопитающих, так как не могут преодолеть гематоэнцефалический барьер и достичь ГАМК А -чув-ствительные Cl-каналы в центральной нервной системе (105). Как известно, GluCl-каналы и GABA A -рецепторы входят в семейство Cys-петлевых рецепторов, включающее также глициновые, никотиновые и серотониновые (5-HT3) ионотропные рецепторы (101,106,107), с которыми авермектины и мильбемицины также взаимодействуют, проявляя, однако, меньшую аффинность. Обнаружено также взаимодействие ивермектина с рецептором P2X4 (108).…”
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