keyword
MENU ▼
Read by QxMD icon Read
search

kv1.3

keyword
https://www.readbyqxmd.com/read/28888365/functional-reconstitution-of-cell-free-synthesized-purified-kv-channels
#1
Stéphane Renauld, Sandra Cortes, Beate Bersch, Xavier Henry, Michel De Waard, Béatrice Schaack
The study of ion channel activity and the screening of possible inhibitor molecules require reliable methods for production of active channel proteins, their insertion into artificial membranes and for the measurement of their activity. Here we report on cell-free expression of soluble and active Kv1.1 and Kv1.3 channels and their efficient insertion into liposomes. Two complementary methods for the determination of the electrical activity of the proteoliposome-embedded channels were compared using Kv1.1 as a model system: (1) single channel recordings in droplet interface bilayers (DIB) and (2) measurement of the membrane voltage potential generated by a potassium ion diffusion potential using the voltage-sensitive fluorescent dye oxonol VI...
September 6, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28869943/targeting-the-potassium-channel-kv1-3-kills-glioblastoma-cells
#2
Elisa Venturini, Luigi Leanza, Michele Azzolini, Stephanie Kadow, Andrea Mattarei, Michael Weller, Ghazaleh Tabatabai, Michael J Edwards, Mario Zoratti, Cristina Paradisi, Ildikò Szabò, Erich Gulbins, Katrin Anne Becker
BACKGROUND/AIMS: Glioblastoma (GBM) is one of the most aggressive cancers, counting for a high number of the newly diagnosed patients with central nervous system (CNS) cancers in the United States and Europe. Major features of GBM include aggressive and invasive growth as well as a high resistance to treatment. Kv1.3, a potassium channel of the shaker family, is expressed in the inner mitochondrial membrane of many cancer cells. Inhibition of mitochondrial Kv1.3 was shown to induce apoptosis in several tumor cells at doses that were not lethal for normal cells...
September 1, 2017: Neuro-Signals
https://www.readbyqxmd.com/read/28863820/sterol-regulation-of-voltage-gated-k-channels
#3
Andras Balajthy, Peter Hajdu, Gyorgy Panyi, Zoltan Varga
Cholesterol is an essential lipid building block of the cellular plasma membrane. In addition to its structural role, it regulates the fluidity and raft structure of the membrane and influences the course of numerous membrane-linked signaling pathways and the function of transmembrane proteins, including ion channels. This is supported by a vast body of scientific data, which demonstrates the modulation of ion channels with a great variety of ion selectivity, gating, and tissue distribution by changes in membrane cholesterol...
2017: Current Topics in Membranes
https://www.readbyqxmd.com/read/28830445/responses-of-rat-and-mouse-primary-microglia-to-pro-and-anti-inflammatory-stimuli-molecular-profiles-k-channels-and-migration
#4
Doris Lam, Starlee Lively, Lyanne C Schlichter
BACKGROUND: Acute CNS damage is commonly studied using rat and mouse models, but increasingly, molecular analysis is finding species differences that might affect the ability to translate findings to humans. Microglia can undergo complex molecular and functional changes, often studied by in vitro responses to discrete activating stimuli. There is considerable evidence that pro-inflammatory (M1) activation can exacerbate tissue damage, while anti-inflammatory (M2) states help resolve inflammation and promote tissue repair...
August 22, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28802123/clathrodin-hymenidin-and-oroidin-and-their-synthetic-analogues-as-inhibitors-of-the-voltage-gated-potassium-channels
#5
Nace Zidar, Aleš Žula, Tihomir Tomašič, Marc Rogers, Robert W Kirby, Jan Tytgat, Steve Peigneur, Danijel Kikelj, Janez Ilaš, Lucija Peterlin Mašič
We have prepared three alkaloids from the Agelas sponges, clathrodin, hymenidin and oroidin, and a series of their synthetic analogues, and evaluated their inhibitory effect against six isoforms of the Kv1 subfamily of voltage-gated potassium channels, Kv1.1-Kv1.6, expressed in Chinese Hamster ovary (CHO) cells using automated patch clamp electrophysiology assay. The most potent inhibitor was the (E)-N-(3-(2-amino-1H-imidazol-4-yl)allyl)-4,5-dichloro-1H-pyrrole-2-carboxamide (6g) with IC50 values between 1...
August 7, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28793216/smit1-modifies-kcnq-channel-function-and-pharmacology-by-physical-interaction-with-the-pore
#6
Rían W Manville, Daniel L Neverisky, Geoffrey W Abbott
Voltage-gated potassium channels of the KCNQ (Kv7) subfamily are essential for control of cellular excitability and repolarization in a wide range of cell types. Recently, we and others found that some KCNQ channels functionally and physically interact with sodium-dependent solute transporters, including myo-inositol transporters SMIT1 and SMIT2, potentially facilitating various modes of channel-transporter signal integration. In contrast to indirect effects such as channel regulation by SMIT-transported, myo-inositol-derived phosphatidylinositol 4,5-bisphosphate (PIP2), the mechanisms and functional consequences of the physical interaction of channels with transporters have been little studied...
August 8, 2017: Biophysical Journal
https://www.readbyqxmd.com/read/28791017/differentially-expressed-potassium-channels-are-associated-with-function-of-human-effector-memory-cd8-t-cells
#7
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/28745785/analysis-on-the-relationship-and-mechanism-of-high-blood-pressure-and-vascular-aging-on-the-condition-that-the-gender-and-age-matches
#8
L-J Yan, H-T Yang, H-Y Duan, J-T Wu, X-W Fan, S-L Wang, C-G Qiu
OBJECTIVE: The relationship between hypertension and the mechanism of the expression of T-lymphocyte Kv1.3 channels in vascular aging has been analyzed in this study based on the gender and age matches' principle. PATIENTS AND METHODS: Thirty patients have been consecutively chosen with vascular aging caused by hypertension (group A), while 30 cases of high blood pressure not merged with vascular aging (group B) were chosen, and 30 cases of healthy volunteers (group C), conforming to gender and age 1:1 and the closest matching principle, were studied...
July 2017: European Review for Medical and Pharmacological Sciences
https://www.readbyqxmd.com/read/28738160/atrial-selective-k-channel-blockers-potential-antiarrhythmic-drugs-in-atrial-fibrillation
#9
Ursula Ravens
In the wake of demographic change in Western countries atrial fibrillation has reached an epidemiological scale, yet current strategies for drug treatment of the arrhythmia lack sufficient efficacy and safety. In search of novel medications, atrial-selective drugs that specifically target atrial over other cardiac functions have been developed. In this lecture, I will address drugs acting on potassium (K+) channels that are either predominantly expressed in atria or possess electrophysiological properties distinct in atria from ventricles...
July 24, 2017: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28723914/safety-and-pharmacodynamics-of-dalazatide-a-kv1-3-channel-inhibitor-in-the-treatment-of-plaque-psoriasis-a-randomized-phase-1b-trial
#10
Eric J Tarcha, Chelsea M Olsen, Peter Probst, David Peckham, Ernesto J Muñoz-Elías, James G Kruger, Shawn P Iadonato
BACKGROUND: Dalazatide is a specific inhibitor of the Kv1.3 potassium channel. The expression and function of Kv1.3 channels are required for the function of chronically activated memory T cells, which have been shown to be key mediators of autoimmune diseases, including psoriasis. OBJECTIVE: The primary objective was to evaluate the safety of repeat doses of dalazatide in adult patients with mild-to-moderate plaque psoriasis. Secondary objectives were to evaluate clinical proof of concept and the effects of dalazatide on mediators of inflammation in the blood and on chronically activated memory T cell populations...
2017: PloS One
https://www.readbyqxmd.com/read/28695745/treating-autoimmune-disorders-with-venom-derived-peptides
#11
Bingzheng Shen, Zhijian Cao, Wenxin Li, Jean-Marc Sabatier, Yingliang Wu
The effective treatment of autoimmune diseases remains a challenge. Voltage-gated potassium Kv1.3 channels, which are expressed in lymphocytes, are a new therapeutic target for treating autoimmune disease. Consequently, Kv1.3 channel-inhibiting venom-derived peptides are a prospective resource for new drug discovery and clinical application. Area covered: Preclinical and clinical studies have produced a wealth of information on Kv1.3 channel-inhibiting venom-derived peptides, especially from venomous scorpions and sea anemones...
July 11, 2017: Expert Opinion on Biological Therapy
https://www.readbyqxmd.com/read/28683073/high-throughput-electrophysiological-assays-for-voltage-gated-ion-channels-using-syncropatch-768pe
#12
Tianbo Li, Gang Lu, Eugene Y Chiang, Tania Chernov-Rogan, Jane L Grogan, Jun Chen
Ion channels regulate a variety of physiological processes and represent an important class of drug target. Among the many methods of studying ion channel function, patch clamp electrophysiology is considered the gold standard by providing the ultimate precision and flexibility. However, its utility in ion channel drug discovery is impeded by low throughput. Additionally, characterization of endogenous ion channels in primary cells remains technical challenging. In recent years, many automated patch clamp (APC) platforms have been developed to overcome these challenges, albeit with varying throughput, data quality and success rate...
2017: PloS One
https://www.readbyqxmd.com/read/28672906/t-lymphocyte-kv1-3-channel-activation-triggers-the-nlrp3-inflammasome-signaling-pathway-in-hypertensive-patients
#13
Jian Zhu, Yan Yang, Si-Gan Hu, Qiu-Bing Zhang, Jie Yu, Yuan-Ming Zhang
The aim of the current study was to investigate the correlation between voltage-gated potassium 1.3 (Kv1.3) channel of peripheral blood T-lymphocytes and the NLR family pyrin domain containing 3 (NLRP3) inflammasome pathway in hypertensive patients. Peripheral blood samples from the hypertensive Kazakh patients (n=30) and healthy Kazakh subjects (n=30) were collected. The T lymphocytes and serum were separated, and the state of Kv1.3 channels was detected using the patch-clamp technique. Reverse transcription-quantitative polymerase chain reaction and western blot analyses were used to detect the mRNA and protein expression levels of key molecules [NLRP3, caspase-1 and interleuking (IL)-β] in the lymphocyte NLRP3 inflammasome pathway, while serum IL-1β content was measured by ELISA assay...
July 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28651603/a-systems-pharmacology-based-approach-to-identify-novel-kv1-3-channel-dependent-mechanisms-in-microglial-activation
#14
Srikant Rangaraju, Syed Ali Raza, Andrea Pennati, Qiudong Deng, Eric B Dammer, Duc Duong, Michael W Pennington, Malu G Tansey, James J Lah, Ranjita Betarbet, Nicholas T Seyfried, Allan I Levey
BACKGROUND: Kv1.3 potassium channels regulate microglial functions and are overexpressed in neuroinflammatory diseases. Kv1.3 blockade may selectively inhibit pro-inflammatory microglia in neurological diseases but the molecular and cellular mechanisms regulated by Kv1.3 channels are poorly defined. METHODS: We performed immunoblotting and flow cytometry to confirm Kv1.3 channel upregulation in lipopolysaccharide (LPS)-activated BV2 microglia and in brain mononuclear phagocytes freshly isolated from LPS-treated mice...
June 26, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28623364/distribution-and-kinetics-of-the-kv1-3-blocking-peptide-hstx1-r14a-in-experimental-rats
#15
Ralf Bergmann, Manja Kubeil, Kristof Zarschler, Sandeep Chhabra, Rajeev B Tajhya, Christine Beeton, Michael W Pennington, Michael Bachmann, Raymond S Norton, Holger Stephan
The peptide HsTX1[R14A] is a potent and selective blocker of the voltage-gated potassium channel Kv1.3, which is a highly promising target for the treatment of autoimmune diseases and other conditions. In order to assess the biodistribution of this peptide, it was conjugated with NOTA and radiolabelled with copper-64. [(64)Cu]Cu-NOTA-HsTX1[R14A] was synthesised in high radiochemical purity and yield. The radiotracer was evaluated in vitro and in vivo. The biodistribution and PET studies after intravenous and subcutaneous injections showed similar patterns and kinetics...
June 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28596825/kv1-3-channel-blocker-imktx88-maintains-blood-brain-barrier-in-experimental-autoimmune-encephalomyelitis
#16
Jie Huang, Song Han, Qi Sun, Yipeng Zhao, Junchen Liu, Xiaolu Yuan, Wenqian Mao, Biwen Peng, Wanhong Liu, Jun Yin, Xiaohua He
BACKGROUND: Disruption of blood-brain barrier (BBB) and subsequent infiltration of auto-reactive T lymphocytes are major characteristics of multiple sclerosis (MS) and experimental autoimmune encephalomyelitis (EAE). Kv1.3 channel blockers are demonstrated potential therapeutic effects on MS patients and EAE models, maybe via reducing activation of T cells. However, it remains to be explored whether Kv1.3 channel blockers maintain integrity of BBB in MS model. RESULTS: In this study, ImKTx88, a highly selective Kv1...
2017: Cell & Bioscience
https://www.readbyqxmd.com/read/28596383/reinvestigation-of-the-biological-activity-of-d-allo-shk-protein
#17
Bobo Dang, Sandeep Chhabra, Michael W Pennington, Raymond S Norton, Stephen B H Kent
ShK toxin from the sea anemone Stichodactyla helianthus is a 35-residue protein that binds to the Kv1.3 ion channel with high affinity. Recently we determined the X-ray structure of ShK toxin by racemic crystallography, in the course of which we discovered that d-ShK has a near-background IC50 value ∼50,000 times lower than that of the l-ShK toxin. This lack of activity was at odds with previously reported results for an ShK diastereomer designated d-allo-ShK, for which significant biological activity had been observed in a similar receptor-blocking assay...
July 28, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28552341/methamphetamine-potentiates-hiv-1gp120-induced-microglial-neurotoxic-activity-by-enhancing-microglial-outward-k-current
#18
Jianuo Liu, Enquan Xu, Guihua Tu, Han Liu, Jiangtao Luo, Huangui Xiong
Methamphetamine (Meth) abuse not only increases the risk of human immunodeficiency virus-1 (HIV-1) infection, but exacerbates HIV-1-associated neurocognitive disorders (HAND) as well. The mechanisms underlying the co-morbid effect are not fully understood. Meth and HIV-1 each alone interacts with microglia and microglia express voltage-gated potassium (KV) channel KV1.3. To understand whether KV1.3 functions an intersecting point for Meth and HIV-1, we studied the augment effect of Meth on HIV-1 glycoprotein 120 (gp120)-induced neurotoxic activity in cultured rat microglial cells...
July 2017: Molecular and Cellular Neurosciences
https://www.readbyqxmd.com/read/28549558/the-kv1-3-channel-blocker-vm24-enhances-muscle-glucose-transporter-4-mobilization-but-does-not-reduce-body-weight-gain-in-diet-induced-obese-male-rats
#19
Lorraine Jaimes-Hoy, Georgina B Gurrola, Miguel Cisneros, Patricia Joseph-Bravo, Lourival D Possani, Jean-Louis Charli
AIMS: Voltage-gated potassium channels 1.3 (Kv1.3) can be targeted to reduce diet-induced obesity and insulin resistance in mice. Since species-specific differences in Kv1.3 expression and pharmacology have been observed, we tested the effect of Vm24, a high-affinity specific blocker of Kv1.3 channels from Vaejovis mexicanus smithi, on body weight (BW), glucose tolerance and insulin resistance in diet-induced obese rats. MATERIALS AND METHODS: Young adult male Wistar rats were switched to a high-fat/high-fructose (HFF) diet...
July 15, 2017: Life Sciences
https://www.readbyqxmd.com/read/28544933/cardiotoxic-effect-of-levofloxacin-and-ciprofloxacin-in-rats-with-without-acute-myocardial-infarction-impact-on-cardiac-rhythm-and-cardiac-expression-of-kv4-3-kv1-2-and-nav1-5-channels
#20
Ahmed M Abdelrady, Sawsan A Zaitone, Noha E Farag, Manal S Fawzy, Yasser M Moustafa
Prolongation of QT interval is possible with fluoroquinolones, yet the underlying contributing factors have not been elucidated. Two widely used fluoroquinolone drugs were at the focus of this study in rats with/without acute myocardial dysfunction (AMI) induced by isoproterenol. The effects of levofloxacin and ciprofloxacin on the cardiac mRNA expression of rat Kv4.3, Kv1.2 and Nav1.5 mRNAs were determined. Administration of the two antibiotics produced dose-dependent changes in ECG parameters that were more prominent in rats with AMI than healthy rats; this was accompanied by elevations in serum lactate dehydrogenase and creatine kinase-MB...
August 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
keyword
keyword
53068
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"