keyword
MENU ▼
Read by QxMD icon Read
search

kv1.3

keyword
https://www.readbyqxmd.com/read/29142737/cloning-expression-and-identification-of-ktx-sp4-a-selective-kv1-3-peptidic-blocker-from-scorpiops-pococki
#1
Yan Zou, Feng Zhang, Yaxian Li, Yuanfang Wang, Yi Li, Zhengtao Long, Shujuan Shi, Li Shuai, Jiukai Liu, Zhiyong Di, Shijin Yin
Background: Specific and selective peptidic blockers of Kv1.3 channels can serve as a valuable drug lead for treating T cell-mediated autoimmune diseases, and scorpion venom is an important source of kv1.3 channel inhibitors. Through conducting transcriptomic sequencing for the venom gland of Scorpiops pococki from Xizang province of China, this research aims to discover a novel functional gene encoding peptidic blocker of Kv1.3, and identify its function. Results: We screened out a new peptide toxin KTX-Sp4 which had 43 amino acids including six cysteine residues...
2017: Cell & Bioscience
https://www.readbyqxmd.com/read/29139549/elevated-potassium-outward-currents-in-hyperoxia-treated-atrial-cardiomyocytes
#2
Z Vysotskaya, B Chidipi, J L Rodgers, X Tang, E Samal, N Kolliputi, S Mohapatra, E S Bennett, S K Panguluri
Supplementation of 100% oxygen is a very common intervention in intensive care units (ICU) and critical care centers for patients with dysfunctional lung and lung disorders. Although there is advantage in delivering sufficient levels of oxygen, hyperoxia is reported to be directly associated with increasing in-hospital deaths. Our previous studies reported ventricular and electrical remodeling in hyperoxia treated mouse hearts, and in this article, for the first time, we are investigating the effects of hyperoxia on atrial electrophysiology using whole-cell patch-clamp electrophysiology experiments along with assessment of Kv1...
November 15, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/29131061/kinetic-aspects-of-verapamil-binding-on-rate-on-wild-type-and-six-hkv1-3-mutant-channels
#3
Ann-Kathrin Diesch, Stephan Grissmer
BACKGROUND/AIMS: The human-voltage gated Kv1.3 channel (hKv1.3) is expressed in T- and B lymphocytes. Verapamil is able to block hKv1.3 channels. We characterized the effect of verapamil on currents through hKv1.3 channels paying special attention to the on-rate (kon) of verapamil. By comparing on-rates obtained in wild-type (wt) and mutant channels a binding pocket for verapamil and impacts of different amino acid residues should be investigated. METHODS: Using the whole-cell patch clamp technique the action of verapamil on currents through wild-type and six hKv1...
November 6, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29034212/regulation-of-proliferation-by-a-mitochondrial-potassium-channel-in-pancreatic-ductal-adenocarcinoma-cells
#4
Roberta Peruzzo, Andrea Mattarei, Matteo Romio, Cristina Paradisi, Mario Zoratti, Ildikò Szabò, Luigi Leanza
Previous results link the mitochondrial potassium channel Kv1.3 (mitoKv1.3) to the regulation of apoptosis. By synthesizing new, mitochondria-targeted derivatives (PAPTP and PCARBTP) of PAP-1, a specific membrane-permeant Kv1.3 inhibitor, we have recently provided evidence that both drugs acting on mitoKv1.3 are able to induce apoptosis and reduce tumor growth in vivo without affecting healthy tissues and cells. In the present article, by exploiting these new drugs, we addressed the question whether mitoKv1...
2017: Frontiers in Oncology
https://www.readbyqxmd.com/read/29018452/kv1-3-channel-blockade-modulates-the-effector-function-of-b-cells-in-granulomatosis-with-polyangiitis
#5
Judith Land, Lucas L Lintermans, Coen A Stegeman, Ernesto J Muñoz-Elías, Eric J Tarcha, Shawn P Iadonato, Peter Heeringa, Abraham Rutgers, Wayel H Abdulahad
B cells are central to the pathogenesis of granulomatosis with polyangiitis (GPA), exhibiting both (auto)antibody-dependent and -independent properties. Class-switched memory B cells in particular are a major source of pathogenic autoantibodies. These cells are characterized by high expression levels of Kv1.3 potassium channels, which may offer therapeutic potential for Kv1.3 blockade. In this study, we investigated the effect of the highly potent Kv1.3 blocker ShK-186 on B cell properties in GPA in vitro. Circulating B cell subsets were determined from 33 GPA patients and 17 healthy controls (HCs)...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28987271/co-independent-modification-of-k-channels-by-tricarbonyldichlororuthenium-ii-dimer-corm-2
#6
Guido Gessner, Nirakar Sahoo, Sandip M Swain, Gianna Hirth, Roland Schönherr, Ralf Mede, Matthias Westerhausen, Hans Henning Brewitz, Pascal Heimer, Diana Imhof, Toshinori Hoshi, Stefan H Heinemann
Although toxic when inhaled in high concentrations, the gas carbon monoxide (CO) is endogenously produced in mammals, and various beneficial effects are reported. For potential medicinal applications and studying the molecular processes underlying the pharmacological action of CO, so-called CO-releasing molecules (CORMs), such as tricabonyldichlororuthenium(II) dimer (CORM-2), have been developed and widely used. Yet, it is not readily discriminated whether an observed effect of a CORM is caused by the released CO gas, the CORM itself, or any of its intermediate or final breakdown products...
November 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28964116/revealing-kinetics-and-state-dependent-binding-properties-of-ikur-targeting-drugs-that-maximize-atrial-fibrillation-selectivity
#7
Nicholas Ellinwood, Dobromir Dobrev, Stefano Morotti, Eleonora Grandi
The KV1.5 potassium channel, which underlies the ultra-rapid delayed-rectifier current (IKur) and is predominantly expressed in atria vs. ventricles, has emerged as a promising target to treat atrial fibrillation (AF). However, while numerous KV1.5-selective compounds have been screened, characterized, and tested in various animal models of AF, evidence of antiarrhythmic efficacy in humans is still lacking. Moreover, current guidelines for pre-clinical assessment of candidate drugs heavily rely on steady-state concentration-response curves or IC50 values, which can overlook adverse cardiotoxic effects...
September 2017: Chaos
https://www.readbyqxmd.com/read/28962142/effects-of-selenium-on-myocardial-apoptosis-by-modifying-the-activity-of-mitochondrial-stat3-and-regulating-potassium-channel-expression
#8
Changjiang Zhang, Yinzhi Deng, Yuhua Lei, Jingbo Zhao, Wen Wei, Yuanhong Li
The present study investigated the effects of myocardial mitochondrial signal transduction and activator of transcription 3 (STAT3), succinate dehydrogenase activity and changes of potassium channel expression on cardiomyocyte apoptosis under low selenium conditions. Primary cultured cardiomyocytes from neonatal mice were divided into the non-toxic control group (0.1 µM sodium selenite) and low selenium treatment group (0.05 µM sodium selenite) according to different selenium concentrations. The expression of mitochondrial STAT3, p-STAT3, p-Kv1...
September 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28931540/review-on-the-secret-life-of-ion-channels-kv1-3-potassium-channels-and-cell-proliferation
#9
M Teresa Perez Garcia, Pilar Cidad, Jose R Lopez-Lopez
Kv1.3 channels are involved in the switch to proliferation of normally quiescent cells, being implicated in the control of cell cycle in many different cell types and in many different ways. They modulate membrane potential controlling K(+) fluxes, sense changes in potential and interact with many signaling molecules through their intracellular domains. From a mechanistic point of view, we can describe the role of Kv1.3 channels in proliferation with at least three different models. In the "membrane potential model", membrane hyperpolarization resulting from Kv1...
September 20, 2017: American Journal of Physiology. Cell Physiology
https://www.readbyqxmd.com/read/28888365/functional-reconstitution-of-cell-free-synthesized-purified-kv-channels
#10
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...
December 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28869943/targeting-the-potassium-channel-kv1-3-kills-glioblastoma-cells
#11
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
#12
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
#13
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
#14
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...
October 20, 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
#15
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
#16
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
#17
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
#18
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. Here, 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...
November 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
#19
RANDOMIZED CONTROLLED TRIAL
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
#20
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
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"