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chloride channel activators

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https://www.readbyqxmd.com/read/29143559/k-cl-co-transporter-2-kcc2-a-membrane-trafficking-perspective
#1
Bor Luen Tang
K(+)-Cl(-) co-transporter 2 (KCC2/SLC12A5) is a neuronal specific cation chloride co-transporter which is active under isotonic conditions, and thus a key regulator of intracellular Cl(-) levels. It also has an ion transporter-independent structural role in modulating the maturation and regulation of excitatory glutamatergic synapses. KCC2 levels are developmentally regulated, and a postnatal upregulation of KCC2 generates a low intracellular chloride concentration that allows the neurotransmitters γ-aminobutyric acid (GABA) and glycine to exert inhibitory neurotransmission through its Cl(-) permeating channel...
November 16, 2017: Molecular Membrane Biology
https://www.readbyqxmd.com/read/29136777/anti-hypertensive-and-vasodilatory-effects-of-amended-banxia-baizhu-tianma-tang
#2
Chu Shan Tan, Yean Chun Loh, Chiew Hoong Ng, Yung Sing Ch'ng, Mohd Zaini Asmawi, Mariam Ahmad, Mun Fei Yam
Although Banxia Baizhu Tianma Tang (BBT) has been long administered for hypertensive treatment in Traditional Chinese Medicine (TCM), the ratio of the herbal components that makes up the formulation has not been optimized with respect to the anti-hypertensive effect that it inherently possesses. A newly amended BBT (ABBT) formulation was developed using the evidence-based approach of orthogonal stimulus-response compatibility model. The ABBT showed enhanced therapeutic effect while maintaining its traditional theoretical approach rooted in TCM...
November 7, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29134279/dietary-k-and-cl-independently-regulate-basolateral-conductance-in-principal-and-intercalated-cells-of-the-collecting-duct
#3
Viktor N Tomilin, Oleg Zaika, Arohan R Subramanya, Oleh Pochynyuk
The renal collecting duct contains two distinct cell types, principal and intercalated cells, expressing potassium Kir4.1/5.1 (KCNJ10/16) and chloride ClC-K2 (ClC-Kb in humans) channels on their basolateral membrane, respectively. Both channels are thought to play important roles in controlling systemic water-electrolyte balance and blood pressure. However, little is known about mechanisms regulating activity of Kir4.1/5.1 and ClC-K2/b. Here, we employed patch clamp analysis at the single channel and whole cell levels in freshly isolated mouse collecting ducts to investigate regulation of Kir4...
November 13, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/29127487/towards-a-unified-understanding-of-lithium-action-in-basic-biology-and-its-significance-for-applied-biology
#4
REVIEW
Eric Jakobsson, Orlando Argüello-Miranda, See-Wing Chiu, Zeeshan Fazal, James Kruczek, Santiago Nunez-Corrales, Sagar Pandit, Laura Pritchet
Lithium has literally been everywhere forever, since it is one of the three elements created in the Big Bang. Lithium concentration in rocks, soil, and fresh water is highly variable from place to place, and has varied widely in specific regions over evolutionary and geologic time. The biological effects of lithium are many and varied. Based on experiments in which animals are deprived of lithium, lithium is an essential nutrient. At the other extreme, at lithium ingestion sufficient to raise blood concentration significantly over 1 mM/, lithium is acutely toxic...
November 10, 2017: Journal of Membrane Biology
https://www.readbyqxmd.com/read/29123240/dna-methylation-regulates-tmem16a-ano1-expression-through-multiple-cpg-islands-in-head-and-neck-squamous-cell-carcinoma
#5
Andrey Finegersh, Scott Kulich, Theresa Guo, Alexander V Favorov, Elana J Fertig, Ludmila V Danilova, Daria A Gaykalova, Joseph A Califano, Umamaheswar Duvvuri
ANO1 is a calcium-activated chloride channel that is frequently overexpressed in head and neck squamous cell carcinoma (HNSCC) and other cancers. While ANO1 expression negatively correlates with survival in several cancers, its epigenetic regulation is poorly understood. We analyzed HNSCC samples from TCGA and a separate dataset of HPV+ oropharyngeal squamous cell carcinoma (OPSCC) samples to identify differentially methylated regions. E6 and E7 transfected normal oral keratinocytes (NOK) were used to induce hypermethylation of the ANO1 promoter...
November 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29117522/the-fast-component-of-herg-gating-charge-an-interaction-between-d411-in-the-s1-and-s4-residues
#6
Ying Dou, Logan C Macdonald, Yue Wu, David Fedida
Kv11.1 (hERG) is a voltage-gated potassium channel that shows very slow ionic current activation kinetics, and an unusual underlying biphasic gating charge movement with fast and slow components that differ greatly in time course. The structural basis and role of the fast component of gating charge (Qfast) is unclear, and its relationship to the slow activation of hERG channels is not understood. In this study we have used the cut-open oocyte voltage-clamp technique to investigate the relationship of fast gating charge movement-to-residue interactions between D411 at the bottom of the S1, and lower S4 domain charged and uncharged residues...
November 7, 2017: Biophysical Journal
https://www.readbyqxmd.com/read/29107231/influence-of-the-rdl-a301s-mutation-in-the-brown-planthopper-nilaparvata-lugens-on-the-activity-of-phenylpyrazole-insecticides
#7
William T Garrood, Christoph T Zimmer, Oliver Gutbrod, Bettina Lüke, Martin S Williamson, Chris Bass, Ralf Nauen, T G Emyr Davies
We discovered the A301S mutation in the RDL GABA-gated chloride channel of fiprole resistant rice brown planthopper, Nilaparvata lugens populations by DNA sequencing and SNP calling via RNASeq. Ethiprole selection of two field N. lugens populations resulted in strong resistance to both ethiprole and fipronil and resulted in fixation of the A301S mutation, as well as the emergence of another mutation, Q359E in one of the selected strains. To analyse the roles of these mutations in resistance to phenylpyrazoles, three Rdl constructs: wild type, A301S and A301S+Q359E were expressed in Xenopus laevis oocytes and assessed for their sensitivity to ethiprole and fipronil using two-electrode voltage-clamp electrophysiology...
October 2017: Pesticide Biochemistry and Physiology
https://www.readbyqxmd.com/read/29102290/ion-channels-as-targets-to-treat-cystic-fibrosis-lung-disease
#8
S Lorraine Martin, Vinciane Saint-Criq, Tzyh-Chang Hwang, László Csanády
Lung health relies on effective mucociliary clearance and innate immune defence mechanisms. In cystic fibrosis (CF), an imbalance in ion transport due to an absence of chloride ion secretion, caused by mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) and a concomitant sodium hyperabsorption, caused by dyregulation of the epithelial sodium channel (ENaC), results in mucus stasis which predisposes the lungs to cycles of chronic infection and inflammation leading to lung function decline...
October 25, 2017: Journal of Cystic Fibrosis: Official Journal of the European Cystic Fibrosis Society
https://www.readbyqxmd.com/read/29101464/gabaa-receptor-a-unique-modulator-of-excitability-ca-2-signaling-and-catecholamine-release-of-rat-chromaffin-cells
#9
REVIEW
Tzitzitlini Alejandre-García, Johanna G Peña-Del Castillo, Arturo Hernández-Cruz
The role of gamma-aminobutyric acid (GABA) in adrenal medulla chromaffin cell (CC) function is just beginning to unfold. GABA is stored in catecholamine (CA)-containing dense core granules and is presumably released together with CA, ATP, and opioids in response to physiological stimuli, playing an autocrine-paracrine role on CCs. The reported paradoxical "dual action" of GABAA-R activation (enhancement of CA secretion and inhibition of synaptically evoked CA release) is only one aspect of GABA's multifaceted actions...
November 3, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/29100477/activation-of-anoctamin-1-limits-pulmonary-endothelial-cell-proliferation-via-p38-mapk-dependent-apoptosis
#10
Ayed M Allawzi, Alexander Vang, Richard T Clements, Bong Sook Jhun, Nouaying R Kue, Thomas J Mancini, Amy K Landi, Dmitry Terentyev, Jin O-Uchi, Suzy A Comhair, Serpil C Erzurum, Gaurav Choudhary
Hyperproliferative endothelial cells (ECs) play an important role in the pathogenesis of PAH. Anoctamin-1 (Ano1), a calcium activated chloride channel, can regulate cell proliferation and cell cycle in multiple cell types. However, the expression and function of Ano1 in the pulmonary endothelium is unknown. We examined whether Ano1 was expressed in pulmonary ECs and if altering Ano1 activity would affect EC survival. Expression and localization of Ano1 in rat lung microvascular ECs (RLMVECs) was assessed using immunoblot, immunofluorescence, and subcellular fractionation...
November 3, 2017: American Journal of Respiratory Cell and Molecular Biology
https://www.readbyqxmd.com/read/29091893/isoflurane-post-conditioning-down-regulates-expression-of-aquaporin-4-in-rats-with-cerebral-ischemia-reperfusion-injury-and-is-possibly-related-to-bone-morphogenetic-protein-4-smad1-5-8-signaling-pathway
#11
Min Yuan, Mingyue Ge, Jiangwen Yin, Zhigang Dai, Liping Xie, Yan Li, Xuejiao Liu, Li Peng, Guixing Zhang, Junqiang Si, Ketao Ma, Sheng Wang
AIM: Aquaporins (AQPs) are water-channels that play important roles in brain water homeostasis and cerebral edema induced by brain injury. This study aimed to investigate the relationship between AQP4, bone morphogenetic protein 4 (BMP4)/Smad1/5/8 signaling pathway and isoflurane post-conditiong, which has effects on brain edema in rats with cerebral ischemia/reperfusion (I/R) injury. METHODS: Cerebral I/R injury was induced in rats by using the middle cerebral artery occlusion (MCAO) model for 90min, followed by 24h of reperfusion...
October 27, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29091309/epiregulin-ereg-is-upregulated-through-an-il-1%C3%AE-autocrine-loop-in-caco-2-epithelial-cells-with-reduced-cftr-function
#12
Macarena Massip-Copiz, Mariángeles Clauzure, Ángel G Valdivieso, Tomás A Santa-Coloma
CFTR is a cAMP-regulated chloride channel, whose mutations produce cystic fibrosis. The impairment of CFTR activity increases the intracellular Cl(-) concentration, which in turn produces an increased interleukin-1β (IL-1β) secretion. The secreted IL-1β then induces an autocrine positive feedback loop, further stimulating IL-1β priming and secretion. Since IL-1β can transactivate the epidermal growth factor receptor (EGFR), we study here the levels of expression for different EGFR ligands in Caco-2/pRS26 cells (expressing shRNA against CFTR resulting in a reduced CFTR expression and activity)...
November 1, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29089046/the-novel-isoxazoline-ectoparasiticide-lotilaner-credelio%C3%A2-a-non-competitive-antagonist-specific-to-invertebrates-%C3%AE-aminobutyric-acid-gated-chloride-channels-gabacls
#13
Lucien Rufener, Vanessa Danelli, Daniel Bertrand, Heinz Sager
BACKGROUND: The isoxazolines are a novel class of parasiticides that are potent inhibitors of γ-aminobutyric acid (GABA)-gated chloride channels (GABACls) and, to a lesser extent, of inhibitory glutamate-gated chloride channels (GluCls). Lotilaner (Credelio™), a novel representative of this chemical class, is currently evaluated for its excellent ectoparasiticide properties. METHODS: In this study, we investigated the molecular mode of action and pharmacology of lotilaner...
November 1, 2017: Parasites & Vectors
https://www.readbyqxmd.com/read/29081444/ca-2-calmodulin-dependent-protein-kinase-ii-%C3%AE-dependent-serine727-phosphorylation-is-required-for-tmem16a-ca-2-activated-cl-channel-regulation-in-cerebrovascular-cells
#14
Cai-Xia Lin, Xiao-Fei Lv, Feng Yuan, Xiang-Yu Li, Ming-Ming Ma, Can-Zhao Liu, Jia-Guo Zhou, Guan-Lei Wang, Yong-Yuan Guan
BACKGROUND: TMEM16A is a critical component of Ca(2+)-activated chloride channels (CaCCs) and mediates basilar arterial smooth muscle cell (BASMC) proliferation in hypertensive cerebrovascular remodeling. CaMKII is a negative regulator of CaCC, and four CaMKII isoforms (α, β, γ and δ) are expressed in vasculature; however, it is unknown which and how CaMKII isoforms affect TMEM16A-associated CaCC and BASMC proliferation.Methods and Results:Patch clamp and small interfering RNA (siRNA) knockdown of different CaMKII isoforms revealed that only CaMKIIγ inhibited native Ca(2+)-activated chloride currents (ICl...
October 28, 2017: Circulation Journal: Official Journal of the Japanese Circulation Society
https://www.readbyqxmd.com/read/29080503/effects-of-ca-2-glu-and-gaba-on-hbest1-and-composite-hbest1-popc-surface-films
#15
Tonya D Andreeva, Svetla D Petrova, Kirilka Mladenova, Veselina Moskova-Doumanova, Tanya Topouzova-Hristova, Yulia Petseva, Nikola Mladenov, Konstantin Balashev, Zdravko Lalchev, Jordan A Doumanov
Bestrophinopathies are ocular diseases caused by mutations in the human bestrophin-1 (hBest1) - transmembrane Ca(2+)-activated chloride channel protein, mainly expressed in the retinal pigment epithelium (RPE) cells. hBest1 is also an important transporter for neurotransmitters such as glutamate (Glu) and γ-aminobutyric acid (GABA) in the nervous system. Recently, a new biological role of hBest1, related to its possible involvement in the pathology of brain diseases (Alzheimer's, Parkinson's disease) has been proposed...
October 18, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29079713/a-common-mechanism-for-cftr-potentiators
#16
Han-I Yeh, Yoshiro Sohma, Katja Conrath, Tzyh-Chang Hwang
Cystic fibrosis (CF) is a channelopathy caused by loss-of-function mutations of the cystic fibrosis transmembrane conductance regulator (CFTR) gene, which encodes a phosphorylation-activated and adenosine triphosphate (ATP)-gated chloride channel. In the past few years, high-throughput drug screening has successfully realized the first US Food and Drug Administration-approved therapy for CF, called ivacaftor (or VX-770). A more recent CFTR potentiator, GLPG1837 (N-(3-carbamoyl-5,5,7,7-tetramethyl-4,7-dihydro-5H-thieno[2,3-c]pyran-2-yl)-1H-pyrazole-3-carboxamide), has been shown to exhibit a higher efficacy than ivacaftor for the G551D mutation, yet the underlying mechanism of GLPG1837 remains unclear...
October 27, 2017: Journal of General Physiology
https://www.readbyqxmd.com/read/29069080/un-gating-and-allosteric-modulation-of-a-pentameric-ligand-gated-ion-channel-captured-by-molecular-dynamics
#17
Nicolas E Martin, Siddharth Malik, Nicolas Calimet, Jean-Pierre Changeux, Marco Cecchini
Pentameric ligand-gated ion channels (pLGICs) mediate intercellular communication at synapses through the opening of an ion pore in response to the binding of a neurotransmitter. Despite the increasing availability of high-resolution structures of pLGICs, a detailed understanding of the functional isomerization from closed to open (gating) and back is currently missing. Here, we provide the first atomistic description of the transition from open to closed (un-gating) in the glutamate-gated chloride channel (GluCl) from Caenorhabditis Elegans...
October 2017: PLoS Computational Biology
https://www.readbyqxmd.com/read/29055807/ivermectin-reduces-motor-coordination-serum-testosterone-and-central-neurotransmitter-levels-but-does-not-affect-sexual-motivation-in-male-rats
#18
N Moreira, T M Sandini, T M Reis-Silva, P Navas-Suáresz, A V V Auada, I Lebrun, J C Flório, M M Bernardi, H S Spinosa
Ivermectin (IVM) is a macrocyclic lactone used for the treatment of parasitic infections and widely used in veterinary medicine as endectocide. In mammals, evidence indicates that IVM interacts with γ-aminobutyric acid (GABA)-mediated chloride channels. GABAergic system is involved in the manifestation of sexual behavior. We previously found that IVM at therapeutic doses did not alter sexual behavior in male rats, but at a higher dose, the appetitive phase of sexual behavior was impaired. Thus, we investigated whether the reduction of sexual behavior that was previously observed was a consequence of motor or motivational deficits that are induced by IVM...
October 18, 2017: Reproductive Toxicology
https://www.readbyqxmd.com/read/29055231/correcting-cftr-folding-defects-by-small-molecule-correctors-to-cure-cystic-fibrosis
#19
REVIEW
Marjolein Mijnders, Bertrand Kleizen, Ineke Braakman
Pharmacological intervention to treat the lethal genetic disease cystic fibrosis has become reality, even for the severe, most common folding mutant F508del CFTR. CFTR defects range from absence of the protein, misfolding that leads to degradation rather than cell-surface localization (such as F508del), to functional chloride-channel defects on the cell surface. Corrector and potentiator drugs improve cell-surface location and channel activity, respectively, and combination therapy of two correctors and a potentiator have shown synergy...
October 18, 2017: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/29046300/manganese-promotes-intracellular-accumulation-of-aqp2-via-modulating-f-actin-polymerization-and-reduces-urinary-concentration-in-mice
#20
Lei Lei, Ming Huang, Limin Su, Dongping Xie, Fahmy A Mamuya, Onju Ham, Kenji Tsuji, Teodor G Păunescu, Baoxue Yang, Hua A Jenny Lu
Aquaporin-2 (AQP2) is a water channel protein expressed in principal cells (PCs) of the kidney collecting ducts (CDs) and plays a critical role in mediating water reabsorption and urine concentration. AQP2 undergoes both regulated trafficking mediated by vasopressin (VP) and constitutive recycling, which is independent of VP. For both pathways, actin cytoskeletal dynamics is a key determinant of AQP2 trafficking. We report here that manganese chloride (MnCl2) is a novel and potent regulator of AQP2 trafficking in cultured cells and in the kidney...
October 18, 2017: American Journal of Physiology. Renal Physiology
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