دورية أكاديمية
Molecular and Functional Characterization of GABA Receptor Subunits GRD and LCCH3 from Human Louse Pediculus Humanus Humanus ; Molecular and Functional Characterization of GABA Receptor Subunits GRD and LCCH3 from Human Louse Pediculus Humanus Humanus: Characterization of GRD and LCCH3 from Human Louse
| العنوان: | Molecular and Functional Characterization of GABA Receptor Subunits GRD and LCCH3 from Human Louse Pediculus Humanus Humanus ; Molecular and Functional Characterization of GABA Receptor Subunits GRD and LCCH3 from Human Louse Pediculus Humanus Humanus: Characterization of GRD and LCCH3 from Human Louse |
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| المؤلفون: | Hashim, Omar, Charvet, Claude L., Toubaté, Berthine, Ahmed, Aimun A.E., Lamassiaude, Nicolas, Neveu, Cédric, Dimier-Poisson, Isabelle, Debierre-Grockiego, Françoise, Dupuy, Catherine |
| المساهمون: | Infectiologie et Santé Publique (UMR ISP), Université de Tours (UT)-Institut National de Recherche pour l’Agriculture, l’Alimentation et l’Environnement (INRAE), University of Gezira, Al-Baha University, Omdurman Islamic University, Campus France (Agence Française pour la Promotion de l'Enseignement Supérieur, l'Accueil et la Mobilité Internationale, 934152H), Federation de Recherche en Infectiologie of the Region Centre Val-de-Loire, Ministry of Higher Education-Sudan and the University of Gezira-Sudan, the Université of Tours, INRAE, American Society for Pharmacology and Experimental Therapeutics |
| المصدر: | ISSN: 0026-895X ; Molecular Pharmacology ; https://hal.inrae.fr/hal-03738563Test ; Molecular Pharmacology, 2022, 102 (2), pp.116-127. ⟨10.1124/molpharm.122.000499⟩ ; https://molpharm.aspetjournals.org/content/102/2/116Test. |
| بيانات النشر: | HAL CCSD American Society for Pharmacology and Experimental Therapeutics |
| سنة النشر: | 2022 |
| المجموعة: | Université François-Rabelais de Tours: HAL |
| مصطلحات موضوعية: | GABA receptors, insecticides, cloning, expression profiling, MESH: Animals, MESH: Drosophila / metabolism, MESH: Humans, MESH: Insecticides* / pharmacology, MESH: Lice Infestations, MESH: Pediculus* / genetics, MESH: Pediculus* / metabolism, MESH: Phthiraptera* / metabolism, MESH: Receptors, GABA, MESH: gamma-Aminobutyric Acid, [SDV]Life Sciences [q-bio] |
| الوصف: | International audience ; Human louse Pediculus humanus is a cosmopolitan obligatory blood-feeding ectoparasite causing pediculosis and transmitting many bacterial pathogens. Control of infestation is difficult due to the developed resistance to insecticides that mainly target GABA (γ-aminobutyric acid) receptors. Previous work showed that Pediculus humanus humanus (Phh) GABA receptor subunit resistance to dieldrin (RDL) is the target of lotilaner, a synthetic molecule of the isoxazoline chemical class. To enhance our understanding of how insecticides act on GABA receptors, two other GABA receptor subunits were cloned and characterized: three variants of Phh-grd (glycine-like receptor of Drosophila) and one variant of Phh-lcch3 (ligand-gated chloride channel homolog 3). Relative mRNA expression levels of Phh-rdl, Phh-grd, and Phh-lcch3 revealed that they were expressed throughout the developmental stages (eggs, larvae, adults) and in the different parts of adult lice (head, thorax, and abdomen). When expressed individually in the Xenopus oocyte heterologous expression system, Phh-GRD1, Phh-GRD2, Phh-GRD3, and Phh-LCCH3 were unable to reconstitute functional channels, whereas the subunit combinations Phh-GRD1/Phh-LCCH3, Phh-GRD1/Phh-RDL, and Phh-LCCH3/Phh-RDL responded to GABA in a concentration-dependent manner. The three heteromeric receptors were similarly sensitive to the antagonistic effect of picrotoxin and fipronil, whereas Phh-GRD1/Phh-RDL and Phh-LCCH3/Phh-RDL were respectively about 2.5-fold and 5-fold more sensitive to ivermectin than Phh-GRD1/Phh-LCCH3. Moreover, the heteropentameric receptor constituted by Phh-GRD1/Phh-LCCH3 was found to be permeable and highly sensitive to the extracellular sodium concentration. These findings provided valuable additions to our knowledge of the complex nature of GABA receptors in human louse that could help in understanding the resistance pattern to commonly used pediculicides. SIGNIFICANCE STATEMENT: Human louse is an ectoparasite that causes pediculosis and ... |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| العلاقة: | info:eu-repo/semantics/altIdentifier/pmid/35858760; hal-03738563; https://hal.inrae.fr/hal-03738563Test; https://hal.inrae.fr/hal-03738563/documentTest; https://hal.inrae.fr/hal-03738563/file/2022_Hashim_Mol-Pharmacol_vol-102_p-116-27.pdfTest; PUBMED: 35858760 |
| DOI: | 10.1124/molpharm.122.000499 |
| الإتاحة: | https://doi.org/10.1124/molpharm.122.000499Test https://hal.inrae.fr/hal-03738563Test https://hal.inrae.fr/hal-03738563/documentTest https://hal.inrae.fr/hal-03738563/file/2022_Hashim_Mol-Pharmacol_vol-102_p-116-27.pdfTest |
| حقوق: | http://creativecommons.org/licenses/by-ncTest/ ; info:eu-repo/semantics/OpenAccess |
| رقم الانضمام: | edsbas.8127B931 |
| قاعدة البيانات: | BASE |
| DOI: | 10.1124/molpharm.122.000499 |
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