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https://www.readbyqxmd.com/read/28875832/structure-gating-and-basic-functions-of-the-ca2-activated-k-channel-of-intermediate-conductance
#1
Luigi Sforna, Alfredo Megaro, Mauro Pessia, Fabio Franciolini, Luigi Catacuzzeno
The KCa3.1 channel is the intermediate-conductance member of the Ca2+-activated K channel superfamily. Expressed in excitable and non-excitable cells, the KCa3.1 channel is voltage independent, its opening being exclusively gated by the binding of intracellular Ca2+ to calmodulin, a Ca2+-binding protein constitutively associated with the C-terminus of each KCa3.1 channel α subunit. Upon Ca2+ binding, the KCa3.1 channel activates with high affinity and in highly coordinated fashion giving steep Hill functions and relatively low EC50 values (100-350 nM)...
August 30, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28820911/phosphatidlyinositol-3-kinase-c2-beta-pi3kc2%C3%AE-is-a-potential-new-target-to-treat-ige-mediated-disease
#2
Shekhar Srivastava, Zhai Li, Edward Y Skolnik
Cross linking of the IgE receptor (FcεRI) on mast cells plays a critical role in IgE-dependent allergy including allergic rhinitis, asthma, anaphylaxis, and delayed type hypersensitivity reactions. The Ca2+ activated K+ channel, KCa3.1, plays a critical role in IgE-stimulated Ca2+ entry and degranulation in mast cells by helping to maintain a negative membrane potential, which provides an electrochemical gradient to drive Ca2+ influx. Of the 3 classes of PI3K, the class II PI3Ks are the least studied and little is known about the roles for class II PI3Ks in vivo in the context of the whole organism under normal and pathological conditions...
2017: PloS One
https://www.readbyqxmd.com/read/28791017/differentially-expressed-potassium-channels-are-associated-with-function-of-human-effector-memory-cd8-t-cells
#3
Ji Hyun Sim, Kyung Soo Kim, Hyoungjun Park, Kyung-Jin Kim, Haiyue Lin, Tae-Joo Kim, Hyun Mu Shin, Gwanghun Kim, Dong-Sup Lee, Chan-Wook Park, Dong Hun Lee, Insoo Kang, Sung Joon Kim, Chung-Hyun Cho, Junsang Doh, Hang-Rae Kim
The voltage-gated potassium channel, Kv1.3, and the Ca(2+)-activated potassium channel, KCa3.1, regulate membrane potentials in T cells, thereby controlling T cell activation and cytokine production. However, little is known about the expression and function of potassium channels in human effector memory (EM) CD8(+) T cells that can be further divided into functionally distinct subsets based on the expression of the interleukin (IL)-7 receptor alpha (IL-7Rα) chain. Herein, we investigated the functional expression and roles of Kv1...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28769813/modulation-of-retrograde-trafficking-of-kca3-1-in-a-polarized-epithelium
#4
Bob Shih-Liang Lee, Daniel C Devor, Kirk L Hamilton
In epithelia, the intermediate conductance, Ca(2+)-activated K(+) channel (KCa3.1) is targeted to the basolateral membrane (BLM) where this channel plays numerous roles in absorption and secretion. A growing body of research suggests that the membrane resident population of KCa3.1 may be critical in clinical manifestation of diseases. In this study, we investigated the key molecular components that regulate the degradation of KCa3.1 using a Fisher rat thyroid cell line stably expressing KCa3.1. Using immunoblot, Ussing chamber, and pharmacological approaches, we demonstrated that KCa3...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28760780/structural-determinants-for-the-selectivity-of-the-positive-kca3-1-gating-modulator-5-methylnaphtho-2-1-d-oxazol-2-amine-ska-121
#5
Brandon M Brown, Heesung Shim, Miao Zhang, Vladimir Yarov-Yarovoy, Heike Wulff
Intermediate-conductance (KCa3.1) and small-conductance (KCa2) calcium-activated K(+) channels are gated by calcium binding to calmodulin (CaM) molecules associated with the calmodulin-binding domain (CaM-BD) of these channels. The existing KCa activators, such as naphtho[1,2-d]thiazol-2-ylamine (SKA-31), 6,7-dichloro-1H-indole-2,3-dione 3-oxime (NS309), and 1-ethylbenzimidazolin-2-one (EBIO), activate both channel types with similar potencies. In a previous chemistry effort, we optimized the benzothiazole pharmacophore of SKA-31 toward KCa3...
October 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28707595/functional-roles-of-the-ca2-activated-k-channel-kca3-1-in-brain-tumors
#6
Giuseppina D' Alessandro, Cristina Limatola, Myriam Catalano
Glioblastoma is the most aggressive and deadly brain tumor, with low disease-free period even after surgery and combined radio and chemotherapies. Among the factors contributing to rapid tumor growth in the brain are the elevated proliferation and invasion rate, and the ability to induce a local immunosuppressive environment. The intermediate-conductance Ca2+-activated K+ channel KCa3.1 is expressed on glioblastoma cells and in tumor-infiltrating cells. In tumor cells, the functional expression of KCa3.1 is important to modulate cell invasion and proliferation...
July 13, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28694658/anti-steatotic-and-anti-fibrotic-effects-of-the-kca3-1-channel-inhibitor-senicapoc-in-non-alcoholic-liver-disease
#7
Latha Paka, David E Smith, Dawoon Jung, Siobhan McCormack, Ping Zhou, Bin Duan, Jing-Song Li, Jiaqi Shi, Yong-Jie Hao, Kai Jiang, Michael Yamin, Itzhak D Goldberg, Prakash Narayan
AIM: To evaluate a calcium activated potassium channel (KCa3.1) inhibitor attenuates liver disease in models of non-alcoholic fatty liver disease (NAFLD). METHODS: We have performed a series of in vitro and in vivo studies using the KCa3.1 channel inhibitor, Senicapoc. Efficacy studies of Senicapoc were conducted in toxin-, thioacetamide (TAA) and high fat diet (HFD)-induced models of liver fibrosis in rats. Efficacy and pharmacodynamic effects of Senicapoc was determined through biomarkers of apoptosis, inflammation, steatosis and fibrosis...
June 21, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28679649/involvement-of-ca-2-activated-k-channel-3-1-in-hypoxia-induced-pulmonary-arterial-hypertension-and-therapeutic-effects-of-tram-34-in-rats
#8
Shujin Guo, Yongchun Shen, Guangming He, Tao Wang, Dan Xu, Fuqiang Wen
Pulmonary artery hypertension (PAH) is an incurable disease associated with the proliferation of pulmonary artery smooth muscle cells (PASMCs) and vascular remodeling. The present study examined whether TRAM-34, a highly selective blocker of calcium-activated potassium channel 3.1 (Kca3.1), can help prevent such hypertension by reducing proliferation in PASMCs. Rats were exposed to hypoxia (10% O2) for 3 weeks and treated daily with TRAM-34 intraperitoneally from the first day of hypoxia. Animals were killed and examined for vascular hypertrophy, Kca3...
August 31, 2017: Bioscience Reports
https://www.readbyqxmd.com/read/28676010/kca3-1-channel-modulators-as-potential-therapeutic-compounds-for-glioblastoma
#9
Brandon M Brown, Brandon Pressley, Heike Wulff
The intermediate-conductance Ca2+-activated K+ channel KCa3.1 is widely expressed in cells of the immune system such as T- and B-lymphocytes, mast cells, macrophages and microglia, but also found in dedifferentiated vascular smooth muscle cells, fibroblasts and many cancer cells including pancreatic, prostate, leukemia and glioblastoma. In all these cell types KCa3.1 plays an important role in cellular activation, migration and proliferation by regulating membrane potential and Ca2+ signaling. KCa3.1 therefore constitutes an attractive therapeutic target for diseases involving excessive proliferation or activation of one more of these cell types and researchers both in academia and in the pharmaceutical industry have developed several potent and selective small molecule inhibitors of KCa3...
June 30, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28659615/kca3-1-activation-via-p2y2-purinergic-receptors-promotes-human-ovarian-cancer-cell-skov-3-migration
#10
L Robles-Martínez, E Garay, M G Martel-Gallegos, A Cisneros-Mejorado, D Pérez-Montiel, A Lara, R O Arellano
Disorders in cell signaling mediated by ATP or histamine, activating specific membrane receptors, have been frequently associated with tumorigenesis. Among the elements of response to purinergic (and histaminergic) signaling, ion channel activation controls essential cellular processes in cancer, such as cell proliferation, motility, and death. Here, we studied the effects that ATP had on electrical properties of human ovarian adenocarcinoma cells named SKOV-3. ATP caused increase in intracellular Ca(2+) concentration ([Ca(2+)]i) and, concurrently, it evoked a complex electrical response with a conspicuous outward component...
June 28, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28651800/cellular-mechanisms-underlying-the-inhibitory-effect-of-flufenamic-acid-on-chloride-secretion-in-human-intestinal-epithelial-cells
#11
Pawin Pongkorpsakol, Chantapol Yimnual, Varanuj Chatsudthipong, Vatcharin Rukachaisirikul, Chatchai Muanprasat
Intestinal Cl(-) secretion is involved in the pathogenesis of secretory diarrheas including cholera. We recently demonstrated that flufenamic acid (FFA) suppressed Vibriocholerae El Tor variant-induced intestinal fluid secretion via mechanisms involving AMPK activation and NF-κB-suppression. The present study aimed to investigate the effect of FFA on transepithelial Cl(-) secretion in human intestinal epithelial (T84) cells. FFA inhibited cAMP-dependent Cl(-) secretion in T84 cell monolayers with IC50 of ∼8 μM...
June 10, 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28552057/exploitation-of-novel-molecular-targets-to-treat-idiopathic-pulmonary-fibrosis-a-drug-discovery-perspective
#12
REVIEW
Bhuvaneshwar Vaidya, Ruaab Patel, Aaron Muth, Vivek Gupta
BACKGROUND: Idiopathic pulmonary fibrosis (IPF) is the most common fibrosing lung disease and is caused by excessive lung scarring. IPF-associated severe mortality can be attributed to late diagnosis due to its generic symptoms, and more importantly due to the lack of effective therapies available. Despite extensive research in the past decades, lung transplant still remains the most effective treatment for IPF. Though two drugs recently approved by FDA, Pirfenidone and Nintedanib, have shown an ability to reduce the progression of disease...
2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28507328/pro-inflammatory-ca-activated-k-channels-are-inhibited-by-hydroxychloroquine
#13
María Eugenia Schroeder, Sofía Russo, Carlos Costa, Juliana Hori, Inés Tiscornia, Mariela Bollati-Fogolín, Darío S Zamboni, Gonzalo Ferreira, Ernesto Cairoli, Marcelo Hill
Antimalarials have demonstrated beneficial effects in Systemic Lupus Erithematosus and Rheumatoid Arthritis. However, the mechanisms and the molecular players targeted by these drugs remain obscure. Although hydroxychloroquine (HCQ) is a known ion channel inhibitor, this property has not been linked to its anti-inflammatory effects. We aimed to study whether HCQ inhibits pro-inflammatory ion channels. Electrophysiology experiments demonstrated that HCQ inhibited Ca(++)-activated K(+) conductance in THP-1 macrophages in a dose-dependent manner...
May 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28488084/loop-diuretics-diminish-hemolysis-induced-by-%C3%AE-hemolysin-from-escherichia-coli
#14
Carl Martin Söderström, Steen K Fagerberg, Mette B Brogaard, Jens Leipziger, Marianne Skals, Helle A Praetorius
Uropathogenic Escherichia coli often produce the virulence factor α-hemolysin (HlyA), and the more severe the infection, the likelier it is to isolate HlyA-producing E. coli from patients. HlyA forms pores upon receptor-independent insertion of the toxin into biological membranes and it has been substantiated that HlyA-induced hemolysis is amplified by toxin-induced ATP release and activation of P2X receptors. Thus, hemolysis inflicted by HlyA is a protracted process involving signal transduction. It consists of early, marked cell shrinkage followed by swelling and eventually lysis...
May 9, 2017: Journal of Membrane Biology
https://www.readbyqxmd.com/read/28455747/oxidative-stress-promotes-myocardial-fibrosis-by-upregulating-kca3-1-channel-expression-in-agt-ren-double-transgenic-hypertensive-mice
#15
Li-Ping Wang, Su-Jing Fan, Shu-Min Li, Xiao-Jun Wang, Jun-Ling Gao, Xiu-Hong Yang
The intermediate-conductance Ca(2+)-activated K(+) (KCa3.1) channels play a pivotal role in the cardiac fibroblast proliferation and inflammatory reaction during the progression of myocardial fibrosis. However, the relationship between KCa3.1 expression and oxidative stress, the important factor of promoting fibrosis, has not been clearly established. This study was designed to investigate whether the role of oxidative stress in promoting myocardial fibrosis is related to KCa3.1 channel by using biochemical approaches...
April 28, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28364331/senicapoc-repurposing-a-drug-to-target-microglia-kca3-1-in-stroke
#16
Roland G W Staal, Jonathan R Weinstein, Megan Nattini, Manuel Cajina, Gamini Chandresana, Thomas Möller
Stroke is the leading cause of serious long-term disability and the fifth leading cause of death in the United States. Treatment options for stroke are few in number and limited in efficacy. Neuroinflammation mediated by microglia and infiltrating peripheral immune cells is a major component of stroke pathophysiology. Interfering with the inflammation cascade after stroke holds the promise to modulate stroke outcome. The calcium activated potassium channel KCa3.1 is expressed selectively in the injured CNS by microglia...
March 31, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28331181/multi-walled-carbon-nanotubes-act-as-a-chemokine-and-recruit-macrophages-by-activating-the-plc-ip3-crac-channel-signaling-pathway
#17
Hui Li, Xiao-Qiu Tan, Li Yan, Bo Zeng, Jie Meng, Hai-Yan Xu, Ji-Min Cao
The impact of nanomaterials on immune cells is gaining attention but is not well documented. Here, we report a novel stimulating effect of carboxylated multi-walled carbon nanotubes (c-MWCNTs) on the migration of macrophages and uncover the underlying mechanisms, especially the upstream signaling, using a series of techniques including transwell migration assay, patch clamp, ELISA and confocal microscopy. c-MWCNTs dramatically stimulated the migration of RAW264.7 macrophages when endocytosed, and this effect was abolished by inhibiting phospholipase C (PLC) with U-73122, antagonizing the IP3 receptor with 2-APB, and blocking calcium release-activated calcium (CRAC) channels with SK&F96365...
March 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28280458/jmv5656-a-novel-derivative-of-tlqp-21-triggers-the-activation-of-a-calcium-dependent-potassium-outward-current-in-microglial-cells
#18
Ilaria Rivolta, Anna Binda, Laura Molteni, Laura Rizzi, Elena Bresciani, Roberta Possenti, Jean-Alain Fehrentz, Pascal Verdié, Jean Martinez, Robert J Omeljaniuk, Vittorio Locatelli, Antonio Torsello
TLQP-21 (TLQPPASSRRRHFHHALPPAR) is a multifunctional peptide that is involved in the control of physiological functions, including feeding, reproduction, stress responsiveness, and general homeostasis. Despite the huge interest in TLQP-21 biological activity, very little is known about its intracellular mechanisms of action. In microglial cells, TLQP-21 stimulates increases of intracellular Ca(2+) that may activate functions, including proliferation, migration, phagocytosis and production of inflammatory molecules...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28248292/potassium-channels-kv1-3-and-kca3-1-cooperatively-and-compensatorily-regulate-antigen-specific-memory-t-cell-functions
#19
Eugene Y Chiang, Tianbo Li, Surinder Jeet, Ivan Peng, Juan Zhang, Wyne P Lee, Jason DeVoss, Patrick Caplazi, Jun Chen, Søren Warming, David H Hackos, Susmith Mukund, Christopher M Koth, Jane L Grogan
Voltage-gated Kv1.3 and Ca(2+)-dependent KCa3.1 are the most prevalent K(+) channels expressed by human and rat T cells. Despite the preferential upregulation of Kv1.3 over KCa3.1 on autoantigen-experienced effector memory T cells, whether Kv1.3 is required for their induction and function is unclear. Here we show, using Kv1.3-deficient rats, that Kv1.3 is involved in the development of chronically activated antigen-specific T cells. Several immune responses are normal in Kv1.3 knockout (KO) rats, suggesting that KCa3...
March 1, 2017: Nature Communications
https://www.readbyqxmd.com/read/28245384/-effects-of-tram-34-on-proliferation-and-invasion-of-leukemia-cell-line-hl-60
#20
Tian-Hua Jiang, Zhi-Gang Huang
OBJECTIVE: To investigate the effects of KCa3.1 channel inhibitor TRAM-34 on the proliferation and invasion of leukemia cell line HL-60. METHODS: HL-60 cells at logarithmic growth phase exposed to TRAM-34 at the final concentration of 25, 50, 75 and 100 nmol/L were used as experimental group. The HL-60 cells of control group was cultured in 10% fetal bovine serum-RPMI 1640. The proliferation inhibition rate of TRAM-34 on HL-60 cells was detected by adding MTT solution after 24, 48 and 72 h culture...
February 2017: Zhongguo Shi Yan Xue Ye Xue za Zhi
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