keyword
MENU ▼
Read by QxMD icon Read
search

kca3.1

keyword
https://www.readbyqxmd.com/read/29161243/the-combined-activation-of-kca3-1-and-inhibition-of-kv11-1-herg1-currents-contribute-to-overcome-cisplatin-resistance-in-colorectal-cancer-cells
#1
Serena Pillozzi, Massimo D'Amico, Gianluca Bartoli, Luca Gasparoli, Giulia Petroni, Olivia Crociani, Tiziano Marzo, Angela Guerriero, Luigi Messori, Mirko Severi, Roberto Udisti, Heike Wulff, K George Chandy, Andrea Becchetti, Annarosa Arcangeli
BACKGROUND: Platinum-based drugs such as Cisplatin are commonly employed for cancer treatment. Despite an initial therapeutic response, Cisplatin treatment often results in the development of chemoresistance. To identify novel approaches to overcome Cisplatin resistance, we tested Cisplatin in combination with K(+) channel modulators on colorectal cancer (CRC) cells. METHODS: The functional expression of Ca(2+)-activated (KCa3.1, also known as KCNN4) and voltage-dependent (Kv11...
November 21, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/29155298/mechanisms-of-l-alpha-lysophosphatidylinositol-induced-relaxation-in-human-pulmonary-arteries
#2
Olga Karpińska, Marta Baranowska-Kuczko, Barbara Malinowska, Monika Kloza, Magdalena Kusaczuk, Agnieszka Gęgotek, Paweł Golec, Irena Kasacka, Hanna Kozłowska
AIMS: l-Alpha-lysophosphatidylinositol (LPI) is an endogenous agonist of G protein-coupled receptor 55 (GPR55) which relaxes mesenteric arteries on activation. The aim of the present study was to determine the influence and underlying mechanisms of LPI-induced relaxation in human pulmonary arteries (hPAs). MAIN METHODS: Functional studies were performed in isolated hPAs using organ bath technique. The expression of GPR55 in hPAs and bronchioles was determined by real-time qPCR, Western blot analysis, and immunohistochemistry...
November 16, 2017: Life Sciences
https://www.readbyqxmd.com/read/29098165/a-trpm4-inhibitor-9-phenanthrol-inhibits-glucose-and-glucagon-like-peptide-1-induced-insulin-secretion-from-rat-islets-of-langerhans
#3
Zuheng Ma, Anneli Björklund, Md Shahidul Islam
Pancreatic β-cells express several ion channels of the transient receptor potential family, which play important roles in mediating the stimulus-secretion coupling. One of these channels, the TRPM4 is a Ca(2+)-activated monovalent cation channel. This channel is inhibited by 9-phenanthrol, which also inhibits the TMEM16a Cl(-) channel, and activates the Ca(2+)-activated K(+) channel, Kca3.1. The net effects of ion-channel modulation by 9-phenantherol on the insulin secretion remain unclear. We tested the effects of 9-phenanthrol on glucose- and GLP-1-induced insulin secretion from isolated rat islets in static incubations...
2017: Journal of Diabetes Research
https://www.readbyqxmd.com/read/29075181/kca3-1-inhibition-switches-the-astrocyte-phenotype-during-astrogliosis-associated-with-ischemic-stroke-via-endoplasmic-reticulum-stress-and-mapk-signaling-pathways
#4
Zhihua Yu, Mengni Yi, Tianjiao Wei, Xiaoling Gao, Hongzhuan Chen
Ischemic stroke is a devastating neurological disease that can initiate a phenotype switch in astrocytes. Reactive astrogliosis is a significant pathological feature of ischemic stroke and is accompanied by changes in gene expression, hypertrophied processes and proliferation. The intermediate-conductance Ca(2+)-activated potassium channel KCa3.1 has been shown to contribute to astrogliosis-induced neuroinflammation in Alzheimer's disease (AD). We here present evidence, from both astrocytes subjected to oxygen-glucose deprivation (OGD) and from the brains of mice subjected to permanent middle cerebral artery occlusion (pMCAO), that KCa3...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29038242/activity-dependent-facilitation-of-cav1-3-calcium-channels-promotes-kca3-1-activation-in-hippocampal-neurons
#5
Giriraj Sahu, Hadhimulya Asmara, Fang-Xiong Zhang, Gerald W Zamponi, Ray W Turner
CaV1 L-type calcium channels are key to regulating neuronal excitability, with the range of functional roles enhanced by interactions with calmodulin, accessory proteins, or CaMKII that modulate channel activity. In hippocampal pyramidal cells a prominent elevation of CaV1 activity is apparent in late channel openings that can last for seconds following a depolarizing stimulus train. The current study tested the hypothesis that a reported interaction between CaV1.3 channels, the scaffolding protein densin, and CaMKII could generate a facilitation of channel activity that outlasts a depolarizing stimulus...
October 16, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29038048/the-influence-of-doca-salt-hypertension-and-chronic-administration-of-the-faah-inhibitor-urb597-on-kca2-3-kca3-1-edh-type-relaxation-in-rat-small-mesenteric-arteries
#6
Monika Kloza, Marta Baranowska-Kuczko, Barbara Malinowska, Olga Karpińska, Ewa Harasim-Symbor, Irena Kasacka, Hanna Kozłowska
The aim of this study was to examine the influence of deoxycorticosterone acetate-salt (DOCA-salt) hypertension and chronic treatment with the fatty acid amide hydrolase inhibitor, URB597, on small and intermediate conductance calcium-activated potassium channels and endothelium-dependent hyperpolarization (KCa2.3/KCa3.1-EDH) in rat small mesenteric arteries (sMAs). The EDH-type response was investigated, in endothelium-intact sMAs using a wire myograph, by examining acetylcholine-evoked vasorelaxation in the presence of N(ω)-nitro-L-arginine methyl ester and indomethacin (inhibitors of nitric oxide synthase and cyclooxygenase, respectively)...
October 14, 2017: Vascular Pharmacology
https://www.readbyqxmd.com/read/29037241/the-potassium-channel-kca3-1-constitutes-a-pharmacological-target-for-astrogliosis-associated-with-ischemia-stroke
#7
Mengni Yi, Tianjiao Wei, Yanxia Wang, Qin Lu, Gaoxian Chen, Xiaoling Gao, Herbert M Geller, Hongzhuan Chen, Zhihua Yu
BACKGROUND: Reactive astrogliosis is one of the significantly pathological features in ischemic stroke accompanied with changes in gene expression, morphology, and proliferation. KCa3.1 was involved in TGF-β-induced astrogliosis in vitro and also contributed to astrogliosis-mediated neuroinflammation in neurodegeneration disease. METHODS: Wild type mice and KCa3.1(-/-) mice were subjected to permanent middle cerebral artery occlusion (pMCAO) to evaluate the infarct areas by 2,3,5-triphenyltetrazolium hydrochloride staining and neurological deficit...
October 16, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28993731/small-and-intermediate-calcium-activated-potassium-channel-openers-improve-rat-endothelial-and-erectile-function
#8
Simon G Comerma-Steffensen, Ingrid Carvacho, Elise R Hedegaard, Ulf Simonsen
Modulation of endothelial calcium-activated potassium (KCa) channels has been proposed as an approach to restore endothelial function. The present study investigated whether novel openers of KCa channels with small (KCa2.x) and intermediate (KCa3.1) conductance, NS309 and NS4591, improve endothelium-dependent relaxation and erectile function. Rat corpus cavernosum (CC) strips were mounted for isometric tension recording and processed for immunoblotting. Mean arterial pressure (MAP), intracavernosal pressure (ICP), and electrocardiographic (ECG) measurements were conducted in anesthetized rats...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28975890/identification-and-validation-of-novel-prognostic-markers-in-renal-cell-carcinoma
#9
Maj Rabjerg
Kidney cancer (Renal Cell Carcinoma (RCC)) is one of the most deadly malignancies due to frequent late diagnosis and poor treatment options. Histologically, RCC embraces a wide variety of different subtypes with the clear cell variant (ccRCC) being the most common, accounting for 75-90% of all RCCs. At present, the surveillance protocols for follow-up of RCC patients after radical nephrectomy are based on the American Joint Committee on Cancers (AJCC) pathological tumor-node-metastasis (TNM) classification system...
October 2017: Danish Medical Journal
https://www.readbyqxmd.com/read/28970794/functional-cooperation-between-kca3-1-and-trpv4-channels-in-bronchial-smooth-muscle-cell-proliferation-associated-with-chronic-asthma
#10
Zhihua Yu, Yanxia Wang, Lu Qin, Hongzhuan Chen
Airway smooth muscle cells (SMC) proliferation contributes to the airways remodeling and irreversible airway obstruction during severe asthma, but the mechanisms of airway SMC proliferation are poorly understood. Intracellular Ca(2)(+) levels play an important role in regulating cell proliferation. We have previously reported KCa3.1 channels regulated human bronchial smooth muscle (HBSM) cells proliferation via the Ca(2+) influx as a consequence of membrane hyperpolarization. However, the role of potassium channels KCa3...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28875832/structure-gating-and-basic-functions-of-the-ca2-activated-k-channel-of-intermediate-conductance
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
keyword
keyword
104101
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"