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chloride channel activators

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https://www.readbyqxmd.com/read/28631282/biosynthesis-of-complex-indole-alkaloids-elucidation-of-the-concise-pathway-of-okaramines
#1
Chen-Yu Lai, Hsiao-Ching Lin, I-Wen Lo, Ranuka T Hewage, Yi-Chen Chen, Chien-Ting Chen, Chi-Fang Lee, Steven Lin, Man-Cheng Tang
The okaramines are a class of complex indole alkaloids isolated from Penicillium and Aspergillus species. Their potent insecticidal activity arises from selectively activating glutamate-gated chloride channels (GluCls) in invertebrates, not affecting human ligand-gated anion channels. Okaramines B (1) and D (2) contain a polycyclic skeleton, including an azocine ring and an unprecedented 2-dimethyl-3-methyl-azetidine ring. Due to their complex scaffold, okaramines have inspired many total synthesis efforts, but the enzymology of the okaramine biosynthetic pathway remains unexplored...
June 20, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28620305/comparative-effects-of-chloride-channel-inhibitors-on-lrrc8-vrac-mediated-chloride-conductance
#2
Jonas Friard, Michel Tauc, Marc Cougnon, Vincent Compan, Christophe Duranton, Isabelle Rubera
Chloride channels play an essential role in a variety of physiological functions and in human diseases. Historically, the field of chloride channels has long been neglected owing to the lack of powerful selective pharmacological agents that are needed to overcome the technical challenge of characterizing the molecular identities of these channels. Recently, members of the LRRC8 family have been shown to be essential for generating the volume-regulated anion channel (VRAC) current, a chloride conductance that governs the regulatory volume decrease (RVD) process...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28611584/glial-and-neuronal-glutamate-transporters-differ-in-the-na-requirements-for-activation-of-the-substrate-independent-anion-conductance
#3
Christopher B Divito, Jenna E Borowski, Nathan G Glasgow, Aneysis D Gonzalez-Suarez, Delany Torres-Salazar, Jon W Johnson, Susan G Amara
Excitatory amino acid transporters (EAATs) are secondary active transporters of L-glutamate and L- or D-aspartate. These carriers also mediate a thermodynamically uncoupled anion conductance that is gated by Na(+) and substrate binding. The activation of the anion channel by binding of Na(+) alone, however, has only been demonstrated for mammalian EAAC1 (EAAT3) and EAAT4. To date, no difference has been observed for the substrate dependence of anion channel gating between the glial, EAAT1 and EAAT2, and the neuronal isoforms EAAT3, EAAT4 and EAAT5...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28611235/improvement-in-exercise-duration-lung-function-and-well-being-in-g551d-cystic-fibrosis-patients-a-double-blind-placebo-controlled-randomised-cross-over-study-with-ivacaftor
#4
Dominic T Keating, Deirdre Edgeworth, Matthew Ellis, Brenda Button, Elyssa Williams, Denise Clark, Audrey Tierney, Stephane Heritier, Anastase Kotsimbos, John Wilson
G551D , a mutation of the cystic fibrosis transmembrane conductance regulator (CFTR) gene, results in impaired chloride channel function in cystic fibrosis (CF) with multiple end-organ manifestations. The effect of ivacaftor, a CFTR-potentiator, on exercise capacity in cystic fibrosis (CF) is unknown. Twenty G551D-CF patients were recruited to a single-centre, double-blind, placebo-controlled, 28-day crossover study of ivacaftor. Variables measured included percentage change from baseline (%Δ) of VO2max (maximal oxygen consumption, primary outcome) during cardiopulmonary exercise testing (CPET), relevant other CPET physiological variables, lung function, BMI, sweat chloride, and disease specific health related quality of life (QOL) measures (CFQ-R and Alfred Wellness (AWEscore))...
June 13, 2017: Clinical Science (1979-)
https://www.readbyqxmd.com/read/28603004/ion-channel-signaling-influences-cellular-proliferation-and-phagocyte-activity-during-axolotl-tail-regeneration
#5
Brandon M Franklin, S Randal Voss, Jeffrey L Osborn
Little is known about the potential for ion channels to regulate cellular behaviors during tissue regeneration. Here, we utilized an amphibian tail regeneration assay coupled with a chemical genetic screen to identify ion channel antagonists that altered critical cellular processes during regeneration. Inhibition of multiple ion channels either partially (anoctamin1/Tmem16a, anoctamin2/Tmem16b, KV2.1, KV2.2, L-type CaV channels and H/K ATPases) or completely (GlyR, GABAAR, KV1.5 and SERCA pumps) inhibited tail regeneration...
June 7, 2017: Mechanisms of Development
https://www.readbyqxmd.com/read/28592822/bacterial-sphingomyelinase-is-a-state-dependent-inhibitor-of-the-cystic-fibrosis-transmembrane-conductance-regulator-cftr
#6
B B Stauffer, G Cui, K A Cottrill, D T Infield, N A McCarty
Sphingomyelinase C (SMase) inhibits CFTR chloride channel activity in multiple cell systems, an effect that could exacerbate disease in CF and COPD patients. The mechanism by which sphingomyelin catalysis inhibits CFTR is not known but evidence suggests that it occurs independently of CFTR's regulatory "R" domain. In this study we utilized the Xenopus oocyte expression system to shed light on how CFTR channel activity is reduced by SMase. We found that the pathway leading to inhibition is not membrane delimited and that inhibited CFTR channels remain at the cell membrane, indicative of a novel silencing mechanism...
June 7, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28590059/sympatholytic-effect-of-intravascular-atp-is-independent-of-nitric-oxide-prostaglandins-na-k-atpase-and-kir-channels-in-humans
#7
Christopher M Hearon, Jennifer C Richards, Mathew L Racine, Gary J Luckasen, Dennis G Larson, Michael J Joyner, Frank A Dinenno
Exercise and intravascular ATP elicit vasodilatation that is dependent on activation of inwardly rectifying potassium (KIR ) channels, with a modest reliance on nitric oxide (NO) and prostaglandin (PG) synthesis.  Both exercise and intravascular ATP attenuate sympathetic α-adrenergic vasoconstriction (sympatholysis). However, KIR channels, NO, PGs and Na(+) /K(+) -ATPase activity are not obligatory to observe sympatholysis during exercise. To further determine similarities between exercise and intravascular ATP, we tested the hypothesis that inhibition of KIR channels, NO and PG synthesis, and Na(+) /K(+) -ATPase, would not alter the ability of ATP to blunt α1 -adrenergic vasoconstriction...
June 7, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28585036/differential-expression-pattern-of-protein-markers-for-predicting-chemosensitivity-of-dexamethasone-based-chemotherapy-of-b-cell-acute-lymphoblastic-leukemia
#8
Nasrin Dehghan-Nayeri, Peyman Eshghi, Kourosh Goudarzi Pour, Mostafa Rezaei-Tavirani, Mir Davood Omrani, Ahmad Gharehbaghian
Dexamethasone is considered as a direct chemotherapeutic agent in the treatment of pediatric acute lymphoblastic leukemia (ALL). Beside the advantages of the drug, some problems arising from the dose-related side effects are challenging issues during the treatment. Accordingly, the classification of patients to dexamethasone sensitive and resistance groups can help to select optimizing the therapeutic dose with the lowest adverse effects particularly in sensitive cases. For this purpose, we investigated inhibited proliferation and induced cytotoxicity in NALM-6 cells, as sensitive cells, after dexamethasone treatment...
June 5, 2017: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/28576828/the-intracellular-chloride-channel-proteins-clic1-and-clic4-induce-il-1%C3%AE-transcription-and-activate-the-nlrp3-inflammasome
#9
Raquel Domingo-Fernández, Rebecca C Coll, Jay Kearney, Samuel Breit, Luke Aj O'Neill
The NLRP3 inflammasome is a multiprotein complex that regulates the activation of caspase-1 leading to the maturation of the pro-inflammatory cytokines IL-1β and IL-18, and promoting pyroptosis. Classically, the NLRP3 inflammasome in murine macrophages is activated by the recognition of pathogen-associated molecular patterns and by many structurally unrelated factors. Understanding the precise mechanism of NLRP3 activation by such wide array of stimuli remains elusive, but several signaling events, including cytosolic efflux and influx of select ions have been suggested...
June 2, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28576654/mutations-on-m3-helix-of-plutella-xylostella-glutamate-gated-chloride-channel-confer-unequal-resistance-to-abamectin-by-two-different-mechanisms
#10
Xingliang Wang, Alin M Puinean, Andrias O O Reilly, Martin S Williamson, Charles L C Smelt, Neil S Millar, Yidong Wu
Abamectin is one of the most widely used avermectins for agricultural pests control, but the emergence of resistance around the world is proving a major threat to its sustained application. Abamectin acts by directly activating glutamate-gated chloride channels (GluCls) and modulating other Cys-loop ion channels. To date, three mutations occurring in the transmembrane domain of arthropod GluCls are associated with target-site resistance to abamectin: A309V in Plutella xylostella GluCl (PxGluCl), G323D in Tetranychus urticae GluCl1 (TuGluCl1) and G326E in TuGluCl3...
May 31, 2017: Insect Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28575529/abnormal-%C3%AE-aminobutyric-acid-neurotransmission-in-a-kcnq2-model-of-early-onset-epilepsy
#11
Taku Uchida, Christoph Lossin, Yukiko Ihara, Masanobu Deshimaru, Yuchio Yanagawa, Susumu Koyama, Shinichi Hirose
OBJECTIVE: Mutations of the KCNQ2 gene, which encodes the Kv 7.2 subunit of voltage-gated M-type potassium channels, have been associated with epilepsy in the neonatal period. This developmental stage is unique in that the neurotransmitter gamma aminobutyric acid (GABA), which is inhibitory in adults, triggers excitatory action due to a reversed chloride gradient. METHODS: To examine whether KCNQ2-related neuronal hyperexcitability involves neonatally excitatory GABA, we examined 1-week-old knockin mice expressing the Kv 7...
June 2, 2017: Epilepsia
https://www.readbyqxmd.com/read/28566357/living-with-a-leaky-skin-upregulation-of-ion-transport-proteins-during-sloughing
#12
Nicholas C Wu, Rebecca L Cramp, Craig E Franklin
Amphibian skin is a multifunctional organ providing protection from the external environment and facilitating the physiological exchange of gases, water and salts with the environment. In order to maintain these functions, the outer layer of skin is regularly replaced in a process called sloughing. During sloughing, the outermost layer of the skin is removed in its entirety, which has the potential to interfere with skin permeability and ion transport, disrupting homeostasis. In this study, we measured, in vivo, the effects of sloughing on the cutaneous efflux of ions in toads Rhinella marina kept in freshwater conditions...
June 1, 2017: Journal of Experimental Biology
https://www.readbyqxmd.com/read/28561733/structural-basis-for-anion-conduction-in-the-calcium-activated-chloride-channel-tmem16a
#13
Cristina Paulino, Yvonne Neldner, Andy Km Lam, Valeria Kalienkova, Janine Denise Brunner, Stephan Schenck, Raimund Dutzler
The calcium-activated chloride channel TMEM16A is a member of a conserved protein family that comprises ion channels and lipid scramblases. Although the structure of the scramblase nhTMEM16 has defined the architecture of the family, it was unknown how a channel has adapted to cope with its distinct functional properties. Here we have addressed this question by the structure determination of mouse TMEM16A by cryo-electron microscopy and a complementary functional characterization. The protein shows a similar organization to nhTMEM16, except for changes at the site of catalysis...
May 31, 2017: ELife
https://www.readbyqxmd.com/read/28559167/the-stoichiometry-of-the-tmem16a-ion-channel-determined-in-intact-plasma-membranes-of-cos-7-cells-using-liquid-phase-electron-microscopy
#14
Diana B Peckys, Christof Stoerger, Lorenz Latta, Ulrich Wissenbach, Veit Flockerzi, Niels de Jonge
TMEM16A is a membrane protein forming a calcium-activated chloride channel. A homodimeric stoichiometry of the TMEM16 family of proteins has been reported but an important question is whether the protein resides always in a dimeric configuration in the plasma membrane or whether monomers of the protein are also present in its native state within in the intact plasma membrane. We have determined the stoichiometry of the human (h)TMEM16A within whole COS-7 cells in liquid. For the purpose of detecting TMEM16A subunits, single proteins were tagged by the streptavidin-binding peptide within extracellular loops accessible by streptavidin coated quantum dot (QD) nanoparticles...
May 27, 2017: Journal of Structural Biology
https://www.readbyqxmd.com/read/28554723/new-treatments-targeting-the-basic-defects-in-cystic-fibrosis
#15
Isabelle Fajac, Claire E Wainwright
Cystic fibrosis (CF) is a monogenic autosomal recessive disorder affecting around 75,000 individuals worldwide. It is a multi-system disease but the main morbidity and mortality is caused by chronic lung disease. Due to newborn screening, a multidisciplinary approach to care and intensive symptomatic treatment, the prognosis has dramatically improved over the last decades and there are currently more adults than children in many countries. However, CF is still a very severe disease with a current median age of life expectancy in the fourth decade of life...
May 26, 2017: La Presse Médicale
https://www.readbyqxmd.com/read/28553230/the-lrrc8a-mediated-swell-activated-chloride-conductance-is-dispensable-for-vacuolar-homeostasis-in-neutrophils
#16
Philippe Behe, Juliet R Foote, Adam P Levine, Craig D Platt, Janet Chou, Fernando Benavides, Raif S Geha, Anthony W Segal
The dialysis of human and mouse neutrophils in patch clamp experiments in the conventional whole-cell mode induces the emergence of a chloride (Cl(-)) current that appeared to be primarily regulated by cytoplasmic ionic strength. The characteristics of this current resembled that of the classical, and ubiquitous volume-sensitive outwardly rectifying Cl(-) current: strong outward rectification, selectivity sequence of the Eisenman1 type, insensitivity to external pH and strong inhibition by tamoxifen, DCPIB and WW781...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28546154/synergistic-mucus-secretion-by-histamine-and-il-4-through-tmem16a-in-airway-epithelium
#17
Ju Wan Kang, Yong Hyuk Lee, Min Jeong Kang, Hyun Jae Lee, Ryung Oh, Hyun Jin Min, Wan Namkung, Jae Young Choi, Sang Nam Lee, Chang-Hoon Kim, Joo-Heon Yoon, Hyung-Ju Cho
Histamine is an important mediator of allergic reactions, and mucus hypersecretion is a major allergic symptom. However, the direct effect of histamine on mucus secretion from airway mucosal epithelia has not been clearly demonstrated. TMEM16A is a Ca2+-activated chloride channel, and it is closely related to fluid secretion in airway mucosal epithelia. We investigated whether histamine directly induces fluid secretion from epithelial cells or submucosal glands (SMG) and mechanisms related therewith in allergic airway diseases...
May 25, 2017: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/28539652/ano1-inhibits-cardiac-fibrosis-after-myocardial-infraction-via-tgf-%C3%AE-smad3-pathway
#18
Yao Gao, Yan Mei Zhang, Li Jun Qian, Ming Chu, Jian Hong, Di Xu
As a newly identified factor in calcium-activated chloride channel, ANO1 participates in various physiological processes like proliferation and differentiation, and expresses in human cardiac fibroblasts. In this experiment, we investigated the function of ANO1 in cardiac fibrosis after myocardial infraction (MI) with methods of Western blotting, Quantitative real-time PCR (qRT-PCR), metabolic reduction of 3-(4,5-dimethylthiozol-2-yl)-2, 5-diphenyltetrazo-lium bromide (MTT), immunofluorescence and confocal imaging, and Masson's trichrome staining...
May 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28536821/impaired-motor-coordination-and-learning-in-mice-lacking-anoctamin-2-calcium-gated-chloride-channels
#19
Franziska Neureither, Katharina Ziegler, Claudia Pitzer, Stephan Frings, Frank Möhrlen
Neurons communicate through excitatory and inhibitory synapses. Both lines of communication are adjustable and allow the fine tuning of signal exchange required for learning processes in neural networks. Several distinct modes of plasticity modulate glutamatergic and GABAergic synapses in Purkinje cells of the cerebellar cortex to promote motor control and learning. In the present paper, we present evidence for a role of short-term ionic plasticity in the cerebellar circuit activity. This type of plasticity results from altered chloride driving forces at the synapses that molecular layer interneurons form on Purkinje cell dendrites...
May 23, 2017: Cerebellum
https://www.readbyqxmd.com/read/28536248/the-signaling-lipid-phosphatidylinositol-3-5-bisphosphate-targets-plant-clc-a-anion-h-exchange-activity
#20
Armando Carpaneto, Anna Boccaccio, Laura Lagostena, Eleonora Di Zanni, Joachim Scholz-Starke
Phosphatidylinositol-3,5-bisphosphate (PI(3,5)P2) is a low-abundance signaling lipid associated with endo-lysosomal and vacuolar membranes in eukaryotic cells. Recent studies on Arabidopsis indicated a critical role of PI(3,5)P2 in vacuolar acidification and morphology during ABA-induced stomatal closure, but the molecular targets in plant cells remained unknown. By using patch-clamp recordings on Arabidopsis vacuoles, we show here that PI(3,5)P2 does not affect the activity of vacuolar H(+)-pyrophosphatase or vacuolar H(+)-ATPase...
May 23, 2017: EMBO Reports
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