Article
Multidisciplinary Sciences
Shivani Choudhary, Melanie Abongwa, Sudhanva S. Kashyap, Saurabh Verma, Gunnar R. Mair, Daniel Kulke, Richard J. Martin, Alan P. Robertson
Summary: In this study, a GluCls subunit from Brugia malayi was cloned and its pharmacological properties were investigated. The results showed that the receptor was regulated by the natural ligand L-glutamate and ivermectin, and had dual effects when exposed to nodulisporic acid. Furthermore, the unique pharmacological characteristics of this GluCls subunit could explain the variation in drug sensitivities observed in different nematode parasites.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2022)
Article
Medicine, Research & Experimental
Mark D. Kaji, Jennifer D. Noonan, Timothy G. Geary, Robin N. Beech
Summary: The study revealed that MOX inhibits wild-type C. elegans GLC-2 receptors approximately 10 times more potently than IVM, with greater maximal inhibition of glutamate activation. Mutations in amino acid residues can alter the actions of IVM and MOX, highlighting differences in their receptor-level pharmacology.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Microbiology
Germanus S. Bah, Sebastian Schneckener, Steffen R. Hahnel, Nicolas H. Bayang, Helena Fieseler, Gabriele M. Schmuck, Ralph Krebber, Anouk Sarr, Carsten Terjung, Henrietta F. Ngangyung, David D. Ekale, Youssouf M. Mfopit, Lucien Rufener, John Graham-Brown, Vincent N. Tanya, Martin Glenschek-Sieberth, Daniel Kulke, Benjamin L. Makepeace
Summary: Onchocerciasis, caused by the parasitic worm Onchocerca volvulus, is a devastating neglected tropical disease affecting sub-Saharan Africa with an overall impact of >1.3 million years lived with disability. Emodepside, originally a veterinary wormer, has shown significant efficacy against adult worms in cattle, supporting its ongoing clinical development for the treatment of human onchocerciasis by targeting adult filariae.
Article
Genetics & Heredity
Damien M. O'Halloran
Summary: Glutamate-gated chloride channels are a protein family that are activated by glutamate and serve as targets for antiparasitic drugs. Analysis of a database of predicted glutamate-gated chloride subunit genes from various nematode species revealed patterns of gene count and sequence diversity.
G3-GENES GENOMES GENETICS
(2022)
Article
Agronomy
Yue Gao, Kyungjae Andrew Yoon, Jong Hyeok Lee, Ju Hyeon Kim, Si Hyeock Lee
Summary: The study revealed that Western flower thrips resistance to emamectin benzoate is highly specific, mainly due to the overexpression of cytochrome P450 monooxygenase (CYP) genes and mutations and overexpression of glutamate-gated chloride channel (GluCl) genes.
PEST MANAGEMENT SCIENCE
(2022)
Article
Medicine, General & Internal
Kai-Feng Shen, Xiao-Lin Yang, Guo-Long Liu, Gang Zhu, Zhong-Ke Wang, Xian-Jun Shi, Ting-Ting Wang, Zhi-Feng Wu, Sheng-Qing Lv, Shi-Yong Liu, Hui Yang, Chun-Qing Zhang
Summary: The study revealed that ClC-mediated current was increased in the hippocampal neurons of chronic TLE mice. Application of chloride channel blockers NPPB and DIDS reduced the current and increased inhibitory synaptic transmission in TLE mice. These drugs also decreased seizure frequency and the average power of ictal high-frequency oscillations in TLE mice.
Article
Biochemistry & Molecular Biology
Noelia Rodriguez Araujo, Guillermina Hernando, Jeremias Corradi, Cecilia Bouzat
Summary: This study reveals the potential compounds regulating the function of MOD-1 and demonstrates its role in worm locomotion, suggesting MOD-1 as a potential target for anthelmintic therapy.
JOURNAL OF BIOLOGICAL CHEMISTRY
(2022)
Review
Neurosciences
Byoung Ju Lee, Che Ho Yang, Seung Yeon Lee, Suk-Ho Lee, Yujin Kim, Won-Kyung Ho
Summary: The coupling distance between VGCCs and synaptic vesicles determines the VGCC dependence of spontaneous release at synapses, with tightly coupled synapses showing significant VGCC contribution while loosely coupled synapses have minimal VGCC involvement.
PROGRESS IN NEUROBIOLOGY
(2022)
Article
Agriculture, Multidisciplinary
Benjie Li, Ying Yan, Guangkai Yao, Ling Zhang, Fei Lin, Hanhong Xu
Summary: A series of novel pyrazoloquinazolines were synthesized, and pyrazoloquinazoline 5a was found to have high insecticidal activity against the diamondback moth without cross-resistance to fipronil. Electrophysiological experiments suggested that 5a acts on the GABAR and GluCl. The potency of 5a on PxGluCl was 15-fold higher than fipronil, explaining the lack of cross-resistance. Downregulation of PxGluCl transcription significantly enhanced the insecticidal activity of 5a on the diamondback moth.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Xi Sun, Wenjuan Hua, Kunkun Wang, Jiajia Song, Bin Zhu, Xiwu Gao, Pei Liang
Summary: The frequent use of insecticides has caused insecticide resistance, which poses a threat to global agricultural production. This study identified a novel mutation in the glutamate-gated chloride channel of the diamondback moth, which is responsible for its resistance to the insecticide abamectin. These findings provide insights into the mechanisms of abamectin resistance and lay the groundwork for the development of new molecular detection methods.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Cell Biology
Lingyong Li, Shao-Rui Chen, Meng-Hua Zhou, Li Wang, De-Pei Li, Hong Chen, Garam Lee, Vasanthi Jayaraman, Hui-Lin Pan
Summary: The study reveals that nerve injury potentiates postsynaptic CP-AMPARs in the spinal dorsal horn via alpha 2 delta-1, which interacts with GluA1 and GluA2 to regulate the subunit composition and synaptic expression of AMPARs. Inhibition of alpha 2 delta-1 restores the intracellular assembly and synaptic dominance of heteromeric GluA1/GluA2 receptors, highlighting alpha 2 delta-1 as a key regulator of AMPAR function.
Article
Biology
Jodi T. Thomas, Blake L. Spady, Philip L. Munday, Sue-Ann Watson
Summary: This study found that GABA(A) receptors and other ligand-gated chloride channels play a significant role in CO2-induced behavioral changes in cephalopods. The pharmacological evidence suggests altered functioning of these receptors underlies some behavioral changes in marine invertebrates exposed to elevated CO2 levels.
JOURNAL OF EXPERIMENTAL BIOLOGY
(2021)
Article
Pharmacology & Pharmacy
Nicolas Lamassiaude, Elise Courtot, Angelique Corset, Claude L. Charvet, Cedric Neveu
Summary: This study identified and characterized highly conserved GluCl subunits from different nematode species, revealing the pivotal role of GLC-2 subunit in the composition of heteromeric GluCls and discovering a novel GluCl subtype combining GLC-2/GLC-3 subunits. The findings provide new insights into GluCl diversity and potential drug targets for the development of next generation anthelmintic compounds.
BRITISH JOURNAL OF PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Xian-Zheng Wang, Jia-Sheng Chen, Wei Wang, Duo-Bang Niu, Hui-Zi Wu, Subba Reddy Palli, Hai-Qun Cao, Cheng-Wang Sheng
Summary: This study investigated the molecular targets of emamectin benzoate (EB) in controlling fall armyworm (FAW). The glutamate-gated chloride channel (GluCl) was identified as a potential target. The expression level of SfGluCl was found to be higher in the head and nerve cord of FAW, as well as in eggs. Knockdown of SfGluCl significantly reduced mortality caused by EB treatment.
PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
(2023)
Review
Neurosciences
Peter Kovermann, Miriam Engels, Frank Mueller, Christoph Fahlke
Summary: Excitatory amino acid transporters (EAATs) play a crucial role in optimizing the temporal resolution and energy demand of excitatory synapses. In addition to their primary transport function, EAATs also function as anion channels. Recent research has shed light on the physiological and pathophysiological roles of EAAT anion channels.
FRONTIERS IN CELLULAR NEUROSCIENCE
(2022)