Ion channels: structure of a molecular brake by Sansom, M

“…<p>A combination of crystallographic and mutagenesis studies on the HERG K⁺ channel, a key determinant of cardiac excitability, has suggested how the protein's extramembraneous amino-terminal domain might act as a ‘molecular brake’ that slows down channel deactivation.…”

Insight into the mechanism of inactivation and pH sensitivity in potassium channels from molecular dynamics simulations. by Stansfeld, P, Grottesi, A, Sands, Z, Sansom, MS, Gedeck, P, Gosling, M, Cox, B, Stanfield, P, Mitcheson, J, Sutcliffe, M

“…This process is rapid in the hERG K (+) channel and is fundamental to its physiological role. …”

Physical Exercise and the Hallmarks of Breast Cancer: A Narrative Review by Celia García-Chico, Susana López-Ortiz, Saúl Peñín-Grandes, José Pinto-Fraga, Pedro L. Valenzuela, Enzo Emanuele, Claudia Ceci, Grazia Graziani, Carmen Fiuza-Luces, Simone Lista, Alejandro Lucia, Alejandro Santos-Lozano

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The ion channel basis of pharmacological effects of amiodarone on myocardial electrophysiological properties, a comprehensive review by Illia Gelman, Neelakshi Sharma, Olivia Mckeeman, Peter Lee, Noah Campagna, Nicole Tomei, Adrian Baranchuk, Shetuan Zhang, Mohammad El-Diasty

“…The primary target of class III antiarrhythmic drugs is the cardiac human ether-a-go-go-related gene (hERG) encoded channel, KCNH2, commonly known as HERG, that conducts the rapidly activating delayed rectifier potassium current (IKr). …”
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Fluorescence-tracking of activation gating in human ERG channels reveals rapid S4 movement and slow pore opening. by Zeineb Es-Salah-Lamoureux, Robert Fougere, Ping Yu Xiong, Gail A Robertson, David Fedida

“…hERG channels are physiologically important ion channels which mediate cardiac repolarization as a result of their unusual gating properties. …”
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Acute osimertinib exposure induces electrocardiac changes by synchronously inhibiting the currents of cardiac ion channels by Peiwen Li, Xiaohui Tian, Gongxin Wang, Enshe Jiang, Yanming Li, Guoliang Hao

“…Osimertinib inhibited the hERG channel in a concentration-dependent manner, with an IC50 of 2.21 ± 1.29 μM. …”
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Testing the nonclinical Comprehensive In Vitro Proarrhythmia Assay (CiPA) paradigm with an established anti‐seizure medication: Levetiracetam case study by Annie Delaunois, François‐Xavier Mathy, Miranda Cornet, Vitalina Gryshkova, Chloé Korlowski, François Bonfitto, Juliane Koch, Anne‐Françoise Schlit, Simon Hebeisen, Elisa Passini, Blanca Rodriguez, Jean‐Pierre Valentin

“…Except a slight inhibition (<10%) of hERG and KV7.1/mink at 7.5 mM, that is, 30‐fold the free therapeutic plasma concentration (FTPC) at 1500 mg, LEV did not affect any other cardiac channels or hERG trafficking. …”
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Market Value Added as an Investment Selection Tool: A Portfolio Separation Test by David Cary, James Chong, Monica Her, G. Michael Phillips

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Electrophysiological Characterization of Spontaneously Contracting Cell Aggregates Obtained from Rainbow Trout Larvae with Multielectrode Arrays by Julia M. Mehnert, Matthias Brandenburger, Bianka Grunow

“…Many drugs interact with hERG potassium channels and consequently cause life threatening ventricular arrhythmias, further highlighting the importance of suitable model systems. …”
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Cardiac toxicity of fluoroquinolones and bedaquiline by G. N. Mozhokinа, A. G. Sаmoylovа

“…The article demonstrates the importance of concomitant factors (potassium level in the blood, concurrent heart disorders, a genetically determined amount of HERG receptors in the myocardium, concomitant drug therapy) in the development of the cardiac toxicity caused by fluoroquinolones and bedaquiline.…”
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Application of Pharmacokinetic Prediction Platforms in the Design of Optimized Anti-Cancer Drugs by Tyler C. Beck, Kendra Springs, Jordan E. Morningstar, Catherine Mills, Andrew Stoddard, Lilong Guo, Kelsey Moore, Cortney Gensemer, Rachel Biggs, Taylor Petrucci, Jennie Kwon, Kristina Stayer, Natalie Koren, Jaclyn Dunne, Diana Fulmer, Ayesha Vohra, Le Mai, Sarah Dooley, Julianna Weninger, Yuri Peterson, Patrick Woster, Thomas A. Dix, Russell A. Norris

“…Several PK prediction platforms exist, including pkCSM, SuperCypsPred, Pred-hERG, Similarity Ensemble Approach (SEA), and SwissADME. …”
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Calcium Transients Closely Reflect Prolonged Action Potentials in iPSC Models of Inherited Cardiac Arrhythmia by C. Ian Spencer, Shiro Baba, Kenta Nakamura, Ethan A. Hua, Marie A.F. Sears, Chi-cheng Fu, Jianhua Zhang, Sadguna Balijepalli, Kiichiro Tomoda, Yohei Hayashi, Paweena Lizarraga, Julianne Wojciak, Melvin M. Scheinman, Katriina Aalto-Setälä, Jonathan C. Makielski, Craig T. January, Kevin E. Healy, Timothy J. Kamp, Shinya Yamanaka, Bruce R. Conklin

“…In myocytes carrying an LQT2 mutation (HERG-A422T), APs and [Ca2+]i transients were prolonged in parallel. …”
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Association between physical activity and cardiovascular risk factors: Dose and sex matter by Alejandro Santos-Lozano, Alberto Torres Barrán, Pablo Fernández-Navarro, Pedro L. Valenzuela, Adrián Castillo-Garcia, Luis M. Ruilope, David Ríos Insua, José M. Ordovas, Victoria Ley, Alejandro Lucia

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Ion channel targeted mechanisms of anti-arrhythmic Chinese herbal medicine Xin Su Ning by Wang, T, Xie, W, Yu, J, Ellory, C, Wilkins, R, Zhu, Y-L, Ma, Y-L

“…In conclusion, the clinical antiarrhythmic efficacy of XSN is based on its class I and Class III antiarrhythmic properties by suppression hNaV1.5 channel and hERG channels, which are directly responsible for XSN’s effect on APA suppression and APD prolongation.…”

APETx4, a Novel Sea Anemone Toxin and a Modulator of the Cancer-Relevant Potassium Channel KV10.1 by Lien Moreels, Steve Peigneur, Diogo T. Galan, Edwin De Pauw, Lászlo Béress, Etienne Waelkens, Luis A. Pardo, Loïc Quinton, Jan Tytgat

“…Similar to the effect of the gating modifier toxin APETx1 on hERG, the inhibition of Kv10.1 by the isolated toxin is reduced at more positive voltages and the peptide seems to keep the channel in a closed state. …”
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Recent Advances in Nutrition for Disease Prevention and Sports Performance Enhancement by Pedro L. Valenzuela

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5-Chloro-2-(phenyldiazenyl)pyridine by Steffen Thies, Christian N&amp;#228;ther, Rainer Herges

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Exercise-Induced Cardiac Fatigue in Recreational Ultramarathon Runners at Moderate Altitude: Insights From Myocardial Deformation Analysis by Sebastián Wolff, José M. Picco, Leonel Díaz-González, Leonel Díaz-González, Pedro L. Valenzuela, Pedro L. Valenzuela, Emanuel Gonzalez-Dávila, Alejandro Santos-Lozano, Alejandro Santos-Lozano, Pablo Matile, David Wolff, Araceli Boraita, Alejandro Lucia, Alejandro Lucia

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Analysis and prediction of injury severity in single micromobility crashes with Random Forest by Almudena Sanjurjo-de-No, Ana María Pérez-Zuriaga, Alfredo García

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Model for long QT syndrome type 2 using human iPS cells demonstrates arrhythmogenic characteristics in cell culture by Anna L. Lahti, Ville J. Kujala, Hugh Chapman, Ari-Pekka Koivisto, Mari Pekkanen-Mattila, Erja Kerkelä, Jari Hyttinen, Kimmo Kontula, Heikki Swan, Bruce R. Conklin, Shinya Yamanaka, Olli Silvennoinen, Katriina Aalto-Setälä

“…Inherited type 2 LQTS (LQT2) and drug-induced LQTS both result from altered function of the hERG channel. We investigated whether the electrophysiological characteristics of LQT2 can be recapitulated in vitro using induced pluripotent stem cell (iPSC) technology. …”
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