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https://www.readbyqxmd.com/read/28738160/atrial-selective-k-channel-blockers-potential-antiarrhythmic-drugs-in-atrial-fibrillation
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
#9
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...
June 8, 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
#10
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
#11
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...
May 23, 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
#12
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
https://www.readbyqxmd.com/read/28504408/kv1-3-channels-facilitate-the-connection-between-metabolism-and-blood-flow-in-the-heart
#13
REVIEW
Vahagn Ohanyan, Liya Yin, Raffi Bardakjian, Christopher Kolz, Molly Enrick, Tatevik Hakobyan, Jordan Luli, Kathleen Graham, Mohamed Khayata, Suzanna Logan, John Kmetz, William M Chilian
The connection between metabolism and flow in the heart, metabolic dilation, is essential for cardiac function. We recently found redox-sensitive Kv1.5 channels play a role in coronary metabolic dilation; however, more than one ion channel likely plays a role in this process as animals null for these channels still showed limited coronary metabolic dilation. Accordingly, we examined the role of another Kv1 family channel, the energetically linked Kv1.3 channel, in coronary metabolic dilation. We measured myocardial blood flow (contrast echocardiography) during norepinephrine-induced increases in cardiac work (heart rate x mean arterial pressure) in WT, WT mice given correolide (preferential Kv1...
May 2017: Microcirculation: the Official Journal of the Microcirculatory Society, Inc
https://www.readbyqxmd.com/read/28495226/a-gas-flow-model-for-layered-landfills-with-vertical-extraction-wells
#14
Shi-Jin Feng, Qi-Teng Zheng, Hai-Jian Xie
This paper developed a two-dimensional axisymmetric analytical model for layered landfills with vertical wells. The model uses a horizontal layered structure to describe the waste non-homogeneity with depth in gas generation, permeability and temperature. The governing equations in the cylindrical coordinate system were transformed to dimensionless forms and solved using a method of eigenfunction expansion. After verification, the effects of different well boundary conditions and gas extraction systems on recovery efficiency were investigated...
May 8, 2017: Waste Management
https://www.readbyqxmd.com/read/28484740/expression-of-ion-channels-in-perivascular-stem-cells-derived-from-human-umbilical-cords
#15
Eunbi Kim, Won Sun Park, Seok-Ho Hong
Potassium channels, the largest group of pore proteins, selectively regulate the flow of potassium (K(+)) ions across cell membranes. The activity and expression of K(+) channels are critical for the maintenance of normal functions in vessels and neurons, and for the regulation of cell differentiation and maturation. However, their role and expression in stem cells have been poorly understood. In this study, we isolated perivascular stem cells (PVCs) from human umbilical cords and investigated the expression patterns of big-conductance Ca(2+)-activated K(+) (BKCa) and voltage-dependent K(+) (Kv) channels using the reverse transcription polymerase chain reaction...
March 2017: Balsaeng'gwa Saengsig
https://www.readbyqxmd.com/read/28472608/epigenetic-regulation-of-voltage-gated-potassium-ion-channel-molecule-kv1-3-in-mechanisms-of-colorectal-cancer
#16
Tao He, Can Wang, Meiying Zhang, Xiaomei Zhang, Shufang Zheng, Enqiang Linghu, Mingzhou Guo
Colorectal cancer (CRC) is among the leading causes of cancer-related death throughout the world. Aberrant expression of voltage-gated potassium ion channel molecule Kv1.3 has been reported in various cancers. To explore the expression and regulation of Kv1.3 in colorectal cancer, 7 colorectal cancer cell lines and 147 cases of primary colorectal cancer were involved in this study. Kv1.3 was expressed in LOVO and SW480 cells and loss of expression was found in RKO, DLD1, SW620, HCT116, and HT29 cells. Complete methylation was found in RKO, DLD1, SW620, HCT116, and HT29 cells, partial methylation was found in LOVO and SW480 cells...
March 2017: Discovery Medicine
https://www.readbyqxmd.com/read/28432329/affinity-biosensors-using-recombinant-native-membrane-proteins-displayed-on-exosomes-application-to-botulinum-neurotoxin-b-receptor
#17
Richard Desplantes, Christian Lévêque, Benjamin Muller, Manuela Lotierzo, Géraldine Ferracci, Michel Popoff, Michael Seagar, Robert Mamoun, Oussama El Far
The development of simple molecular assays with membrane protein receptors in a native conformation still represents a challenging task. Exosomes are extracellular vesicles which, due to their stability and small size, are suited for analysis in various assay formats. Here, we describe a novel approach to sort recombinant fully native and functional membrane proteins to exosomes using a targeting peptide. Specific binding of high affinity ligands to the potassium channel Kv1.2, the G-protein coupled receptor CXCR4, and the botulinum neurotoxin type B (BoNT/B) receptor, indicated their correct assembly and outside out orientation in exosomes...
April 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28426823/observation-of-%C3%AF-pore-currents-in-mutant-hkv1-2_v370c-potassium-channels
#18
Pavel Tyutyaev, Stephan Grissmer
Current through the σ-pore was first detected in hKv1.3_V388C channels, where the V388C mutation in hKv1.3 channels opened a new pathway (σ-pore) behind the central α-pore. Typical for this mutant channel was inward current at potentials more negative than -100 mV when the central α-pore was closed. The α-pore blockers such as TEA+ and peptide toxins (CTX, MTX) could not reduce current through the σ-pore of hKv1.3_V388C channels. This new pathway would proceed in parallel to the α-pore in the S6-S6 interface gap...
2017: PloS One
https://www.readbyqxmd.com/read/28412597/peptide-blockers-of-kv1-3-channels-in-t-cells-as-therapeutics-for-autoimmune-disease
#19
REVIEW
K George Chandy, Raymond S Norton
The voltage-gated Kv1.3 channel in T lymphocytes is a validated therapeutic target for diverse autoimmune diseases. Here we review the discovery of Kv1.3, its physiological role in T cells, and why it is an attractive target for modulating autoimmune responses. We focus on peptide inhibitors because the first Kv1.3-selective inhibitor in human trials is a peptide derived from a marine organism. Two broad classes of peptides block Kv1.3, the first from scorpions and the second from sea anemones. We describe their structures, their binding site in the external vestibule of Kv1...
June 2017: Current Opinion in Chemical Biology
https://www.readbyqxmd.com/read/28408885/fludarabine-inhibits-kv1-3-currents-in-human-b-lymphocytes
#20
Alicia de la Cruz, Alba Vera-Zambrano, Diego A Peraza, Carmen Valenzuela, Juan M Zapata, Gema Perez-Chacon, Teresa Gonzalez
Fludarabine (F-ara-A) is a purine analog commonly used in the treatment of indolent B cell malignancies that interferes with different aspects of DNA and RNA synthesis. KV1.3 K(+) channels are membrane proteins involved in the maintenance of K(+) homeostasis and the resting potential of the cell, thus controlling signaling events, proliferation and apoptosis in lymphocytes. Here we show that F-ara-A inhibits KV currents in human B lymphocytes. Our data indicate that KV1.3 is expressed in both BL2 and Dana B cell lines, although total KV1...
2017: Frontiers in Pharmacology
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