Publications:

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Pharmacological activation of the hERG K+ channel for the management of the long QT syndrome: A review.

Journal Of Arrhythmia

El Harchi, Aziza A; Brincourt, Oriane O

Publication Date: 2022-08

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PubMed Link: 35936037

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Intracellular Binding of Terfenadine Competes with Its Access to Pancreatic ß-cell ATP-Sensitive K+ Channels and Human ether-à-go-go-Related Gene Channels.

The Journal Of Membrane Biology

Zünkler, Bernd J BJ; Wos-Maganga, Maria M; Bohnet, Stefanie S; Kleinau, Anne A; Manns, Detlef D; Chatterjee, Shivani S

Publication Date: 2022-06-28

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PubMed Link: 35763054

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• 232_2022_Article_252.pdf

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Inhibition of the hERG potassium channel by phenanthrene: a polycyclic aromatic hydrocarbon pollutant.

Cellular And Molecular Life Sciences : Cmls

Al-Moubarak, Ehab E; Shiels, Holly A HA; Zhang, Yihong Y; Du, Chunyun C; Hanington, Oliver O; Harmer, Stephen C SC; Dempsey, Christopher E CE; Hancox, Jules C JC

Publication Date: 2021-12

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PubMed Link: 34727194

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• 18_2021_Article_3967.pdf

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Inhibition of the hERG potassium channel by phenanthrene: a polycyclic aromatic hydrocarbon pollutant.

Cellular And Molecular Life Sciences : Cmls

Al-Moubarak, Ehab E; Shiels, Holly A HA; Zhang, Yihong Y; Du, Chunyun C; Hanington, Oliver O; Harmer, Stephen C SC; Dempsey, Christopher E CE; Hancox, Jules C JC

Publication Date: 2021-12

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PubMed Link: 34727194

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• 18_2021_Article_3967.pdf

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Molecular Dynamics-Derived Pharmacophore Model Explaining the Nonselective Aspect of KV10.1 Pore Blockers.

International Journal Of Molecular Sciences

Toplak, Žan Ž; Merzel, Franci F; Pardo, Luis A LA; Peterlin Mašič, Lucija L; Tomašič, Tihomir T

Publication Date: 2021-08-20

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PubMed Link: 34445705

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• ijms-22-08999.pdf

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Effects of Antiarrhythmic Drugs on hERG Gating in Human-Induced Pluripotent Stem Cell-Derived Cardiomyocytes From a Patient With Short QT Syndrome Type 1.

Frontiers In Pharmacology

Huang, Mengying M; Liao, Zhenxing Z; Li, Xin X; Yang, Zhen Z; Fan, Xuehui X; Li, Yingrui Y; Zhao, Zhihan Z; Lang, Siegfried S; Cyganek, Lukas L; Zhou, Xiaobo X; Akin, Ibrahim I; Borggrefe, Martin M; El-Battrawy, Ibrahim I

Publication Date: 2021

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PubMed Link: 34025432

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• fphar-12-675003.pdf

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Lipid regulation of hERG1 channel function.

Nature Communications

Miranda, Williams E WE; Guo, Jiqing J; Mesa-Galloso, Haydee H; Corradi, Valentina V; Lees-Miller, James P JP; Tieleman, D Peter DP; Duff, Henry J HJ; Noskov, Sergei Yu SY

Publication Date: 2021-03-03

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PubMed Link: 33658490

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• 41467_2021_Article_21681.pdf
• 41467_2021_21681_MOESM2_ESM.pdf

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Off-label use of chloroquine, hydroxychloroquine, azithromycin and lopinavir/ritonavir in COVID-19 risks prolonging the QT interval by targeting the hERG channel.

European Journal Of Pharmacology

Zequn, Zheng Z; Yujia, Wu W; Dingding, Qian Q; Jiangfang, Lian L

Publication Date: 2021-02-15

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PubMed Link: 33345848

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• main.pdf

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A structure-based computational workflow to predict liability and binding modes of small molecules to hERG.

Scientific Reports

Kalyaanamoorthy, Subha S; Lamothe, Shawn M SM; Hou, Xiaoqing X; Moon, Tae Chul TC; Kurata, Harley T HT; Houghton, Michael M; Barakat, Khaled H KH

Publication Date: 2020-10-01

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PubMed Link: 33004839

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• 41598_2020_Article_72889.pdf

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An Update on the Structure of hERG.

Frontiers In Pharmacology

Butler, Andrew A; Helliwell, Matthew V MV; Zhang, Yihong Y; Hancox, Jules C JC; Dempsey, Christopher E CE

Publication Date: 2019

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PubMed Link: 32038248

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• fphar-10-01572.pdf

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Cardiac toxicity of Triptergium wilfordii Hook F. may correlate with its inhibition to hERG channel.

Heliyon

Zhao, Wei W; Xiao, Liping L; Pan, Lanying L; Ke, Xianfu X; Zhang, Yanting Y; Zhong, Dian D; Xu, Jianwei J; Cao, Fumin F; Wu, Liren L; Chen, Yuan Y

Publication Date: 2019-10

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PubMed Link: 31667381

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The molecular determinants of R-roscovitine block of hERG channels.

Plos One

Cernuda, Bryan B; Fernandes, Christopher Thomas CT; Allam, Salma Mohamed SM; Orzillo, Matthew M; Suppa, Gabrielle G; Chia Chang, Zuleen Z; Athanasopoulos, Demosthenes D; Buraei, Zafir Z

Publication Date: 2019

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PubMed Link: 31479461

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• pone.0217733.pdf

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Potent hERG channel inhibition by sarizotan, an investigative treatment for Rett Syndrome.

Journal Of Molecular And Cellular Cardiology

Cheng, Hongwei H; Du, Chunyun C; Zhang, Yihong Y; James, Andrew F AF; Dempsey, Christopher E CE; Abdala, Ana P AP; Hancox, Jules C JC

Publication Date: 2019-10

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PubMed Link: 31362019

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The Pore-Lipid Interface: Role of Amino-Acid Determinants of Lipophilic Access by Ivabradine to the hERG1 Pore Domain.

Molecular Pharmacology

Perissinotti, Laura L; Guo, Jiqing J; Kudaibergenova, Meruyert M; Lees-Miller, James J; Ol'khovich, Marina M; Sharapova, Angelica A; Perlovich, German L GL; Muruve, Daniel A DA; Gerull, Brenda B; Noskov, Sergei Yu SY; Duff, Henry J HJ

Publication Date: 2019-08

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PubMed Link: 31182542

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Histidine at position 462 determines the low quinine sensitivity of ether-à-go-go channel superfamily member Kv 12.1.

British Journal Of Pharmacology

Dierich, Marlen M; van Ham, Willem B WB; Stary-Weinzinger, Anna A; Leitner, Michael G MG

Publication Date: 2019-08

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PubMed Link: 31032878

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• BPH-176-2708.pdf

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An in Vitro Assay of hERG K Channel Potency for a New EGFR Inhibitor FHND004.

Frontiers In Pharmacology

Jin, Tao T; Hu, Bingxue B; Chen, Shanshan S; Wang, Qiang Q; Dong, Xue X; Zhang, Yin Y; Zhu, Yongqiang Y; Zhang, Zhao Z

Publication Date: 2018

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PubMed Link: 29904349

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• fphar-09-00577.pdf

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Electrophysiological mechanisms of vandetanib-induced cardiotoxicity: Comparison of action potentials in rabbit Purkinje fibers and pluripotent stem cell-derived cardiomyocytes.

Plos One

Lee, Hyang-Ae HA; Hyun, Sung-Ae SA; Byun, Byungjin B; Chae, Jong-Hak JH; Kim, Ki-Suk KS

Publication Date: 2018

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PubMed Link: 29630634

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• pone.0195577.pdf

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Structural implications of hERG K+ channel block by a high-affinity minimally structured blocker.

The Journal Of Biological Chemistry

Helliwell, Matthew V MV; Zhang, Yihong Y; El Harchi, Aziza A; Du, Chunyun C; Hancox, Jules C JC; Dempsey, Christopher E CE

Publication Date: 2018-05-04

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PubMed Link: 29545312

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• zbc7040.pdf

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The Basis for Low-affinity hERG Potassium Channel Block by Sotalol.

Journal Of Pharmacology & Pharmacotherapeutics

Zhang, Yi Hong YH; Dempsey, Christopher E CE; Hancox, Jules C JC

Publication Date: 2017

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PubMed Link: 29081622

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• JPP-8-130.pdf

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Inhibitory effects and mechanism of dihydroberberine on hERG channels expressed in HEK293 cells.

Plos One

Yu, Dahai D; Lv, Lin L; Fang, Li L; Zhang, Bo B; Wang, Junnan J; Zhan, Ge G; Zhao, Lei L; Zhao, Xin X; Li, Baoxin B

Publication Date: 2017

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PubMed Link: 28763460

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• pone.0181823.pdf

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Drug trapping in hERG K+ channels: (not) a matter of drug size?

Medchemcomm

Linder, Tobias T; Bernsteiner, Harald H; Saxena, Priyanka P; Bauer, Florian F; Erker, Thomas T; Timin, Eugen E; Hering, Steffen S; Stary-Weinzinger, Anna A

Publication Date: 2016-03-01

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PubMed Link: 28337337

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Clemizole hydrochloride blocks cardiac potassium currents stably expressed in HEK 293 cells.

British Journal Of Pharmacology

Jie, Ling-Jun LJ; Wu, Wei-Yin WY; Li, Gang G; Xiao, Guo-Sheng GS; Zhang, Shetuan S; Li, Gui-Rong GR; Wang, Yan Y

Publication Date: 2017-02

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PubMed Link: 27886373

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New potential binding determinant for hERG channel inhibitors.

Scientific Reports

Saxena, P P; Zangerl-Plessl, E-M EM; Linder, T T; Windisch, A A; Hohaus, A A; Timin, E E; Hering, S S; Stary-Weinzinger, A A

Publication Date: 2016-04-12

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PubMed Link: 27067805

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• srep24182.pdf

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Molecular basis of hERG potassium channel blockade by the class Ic antiarrhythmic flecainide.

Journal Of Molecular And Cellular Cardiology

Melgari, Dario D; Zhang, Yihong Y; El Harchi, Aziza A; Dempsey, Christopher E CE; Hancox, Jules C JC

Publication Date: 2015-09

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PubMed Link: 26159617

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hERG potassium channel blockade by the HCN channel inhibitor bradycardic agent ivabradine.

Journal Of The American Heart Association

Melgari, Dario D; Brack, Kieran E KE; Zhang, Chuan C; Zhang, Yihong Y; El Harchi, Aziza A; Mitcheson, John S JS; Dempsey, Christopher E CE; Ng, G André GA; Hancox, Jules C JC

Publication Date: 2015-04-24

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PubMed Link: 25911606

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Anesthetic drug midazolam inhibits cardiac human ether-à-go-go-related gene channels: mode of action.

Drug Design, Development And Therapy

Vonderlin, Nadine N; Fischer, Fathima F; Zitron, Edgar E; Seyler, Claudia C; Scherer, Daniel D; Thomas, Dierk D; Katus, Hugo A HA; Scholz, Eberhard P EP

Publication Date: 2015

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PubMed Link: 25733807

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• dddt-9-867.pdf

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Pharmacological and electrophysiological characterization of AZSMO-23, an activator of the hERG K(+) channel.

British Journal Of Pharmacology

Mannikko, R R; Bridgland-Taylor, M H MH; Pye, H H; Swallow, S S; Abi-Gerges, N N; Morton, M J MJ; Pollard, C E CE

Publication Date: 2015-06

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PubMed Link: 25684549

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Ranolazine inhibition of hERG potassium channels: drug-pore interactions and reduced potency against inactivation mutants.

Journal Of Molecular And Cellular Cardiology

Du, Chunyun C; Zhang, Yihong Y; El Harchi, Aziza A; Dempsey, Christopher E CE; Hancox, Jules C JC

Publication Date: 2014-09

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PubMed Link: 24877995

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• mmc1.pdf

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HERG1 channel agonists and cardiac arrhythmia.

Current Opinion In Pharmacology

Sanguinetti, Michael C MC

Publication Date: 2014-04

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PubMed Link: 24721650

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Assessing hERG pore models as templates for drug docking using published experimental constraints: the inactivated state in the context of drug block.

Journal Of Chemical Information And Modeling

Dempsey, Christopher E CE; Wright, Dominic D; Colenso, Charlotte K CK; Sessions, Richard B RB; Hancox, Jules C JC

Publication Date: 2014-02-24

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PubMed Link: 24471705

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The KCNH2 genetic polymorphism (1956, C>T) is a novel biomarker that is associated with CCB and α,β-ADR blocker response in EH patients in China.

Plos One

He, Fazhong F; Luo, Jianquan J; Luo, Zhiying Z; Fan, Lan L; He, Yijing Y; Zhu, Dingliang D; Gao, Jinping J; Deng, Sheng S; Wang, Yan Y; Qian, Yuesheng Y; Zhou, Honghao H; Chen, Xiaoping X; Zhang, Wei W

Publication Date: 2013

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PubMed Link: 23613831

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ICA-105574 interacts with a common binding site to elicit opposite effects on inactivation gating of EAG and ERG potassium channels.

Molecular Pharmacology

Garg, Vivek V; Stary-Weinzinger, Anna A; Sanguinetti, Michael C MC

Publication Date: 2013-04

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PubMed Link: 23319419

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Mechanisms of zolpidem-induced long QT syndrome: acute inhibition of recombinant hERG K(+) channels and action potential prolongation in human cardiomyocytes derived from induced pluripotent stem cells.

British Journal Of Pharmacology

Jehle, J J; Ficker, E E; Wan, X X; Deschenes, I I; Kisselbach, J J; Wiedmann, F F; Staudacher, I I; Schmidt, C C; Schweizer, P A PA; Becker, R R; Katus, H A HA; Thomas, D D

Publication Date: 2013-03

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PubMed Link: 23061993

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Tuning of EAG K(+) channel inactivation: molecular determinants of amplification by mutations and a small molecule.

The Journal Of General Physiology

Garg, Vivek V; Sachse, Frank B FB; Sanguinetti, Michael C MC

Publication Date: 2012-09

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PubMed Link: 22930803

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Marine algal toxin azaspiracid is an open-state blocker of hERG potassium channels.

Chemical Research In Toxicology

Twiner, Michael J MJ; Doucette, Gregory J GJ; Rasky, Andrew A; Huang, Xi-Ping XP; Roth, Bryan L BL; Sanguinetti, Michael C MC

Publication Date: 2012-09-17

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PubMed Link: 22856456

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In silico analysis of conformational changes induced by mutation of aromatic binding residues: consequences for drug binding in the hERG K+ channel.

Plos One

Knape, Kirsten K; Linder, Tobias T; Wolschann, Peter P; Beyer, Anton A; Stary-Weinzinger, Anna A

Publication Date: 2011

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PubMed Link: 22194911

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Molecular determinants of pentamidine-induced hERG trafficking inhibition.

Molecular Pharmacology

Dennis, Adrienne T AT; Wang, Lu L; Wan, Hanlin H; Nassal, Drew D; Deschenes, Isabelle I; Ficker, Eckhard E

Publication Date: 2012-02

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PubMed Link: 22046004

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High potency inhibition of hERG potassium channels by the sodium-calcium exchange inhibitor KB-R7943.

British Journal Of Pharmacology

Cheng, Hongwei H; Zhang, Yihong Y; Du, Chunyun C; Dempsey, Christopher E CE; Hancox, Jules C JC

Publication Date: 2012-04

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PubMed Link: 21950687

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Effects of the histamine H(1) receptor antagonist hydroxyzine on hERG K(+) channels and cardiac action potential duration.

Acta Pharmacologica Sinica

Lee, Byung Hoon BH; Lee, Seung Ho SH; Chu, Daehyun D; Hyun, Jin Won JW; Choe, Han H; Choi, Bok Hee BH; Jo, Su-Hyun SH

Publication Date: 2011-09

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PubMed Link: 21892192

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Stereoselective Inhibition of the hERG1 Potassium Channel.

Frontiers In Pharmacology

Grilo, Liliana Sintra LS; Carrupt, Pierre-Alain PA; Abriel, Hugues H

Publication Date: 2010

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PubMed Link: 21833176

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Molecular determinants for activation of human ether-à-go-go-related gene 1 potassium channels by 3-nitro-n-(4-phenoxyphenyl) benzamide.

Molecular Pharmacology

Garg, Vivek V; Stary-Weinzinger, Anna A; Sachse, Frank F; Sanguinetti, Michael C MC

Publication Date: 2011-10

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PubMed Link: 21743002

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Trapping and dissociation of propafenone derivatives in HERG channels.

British Journal Of Pharmacology

Windisch, A A; Timin, En E; Schwarz, T T; Stork-Riedler, D D; Erker, T T; Ecker, Gf G; Hering, S S

Publication Date: 2011-04

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PubMed Link: 21175572

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Molecular determinants of human ether-à-go-go-related gene 1 (hERG1) K+ channel activation by NS1643.

Molecular Pharmacology

Grunnet, Morten M; Abbruzzese, Jennifer J; Sachse, Frank B FB; Sanguinetti, Michael C MC

Publication Date: 2011-01

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PubMed Link: 20876384

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Block of HERG k channel by classic histamine h(1) receptor antagonist chlorpheniramine.

The Korean Journal Of Physiology & Pharmacology : Official Journal Of The Korean Physiological Society And The Korean Society Of Pharmacology

Hong, Hee-Kyung HK; Jo, Su-Hyun SH

Publication Date: 2009-06

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PubMed Link: 19885040

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Pharmacological and electrophysiological characterization of nine, single nucleotide polymorphisms of the hERG-encoded potassium channel.

British Journal Of Pharmacology

Männikkö, Roope R; Overend, G G; Perrey, C C; Gavaghan, C L CL; Valentin, J-P JP; Morten, J J; Armstrong, M M; Pollard, C E CE

Publication Date: 2010-01

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PubMed Link: 19673885

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Molecular determinants of hERG channel block by terfenadine and cisapride.

Journal Of Pharmacological Sciences

Kamiya, Kaichiro K; Niwa, Ryoko R; Morishima, Mikio M; Honjo, Haruo H; Sanguinetti, Michael C MC

Publication Date: 2008-11

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PubMed Link: 18987434

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The 5-HT2 antagonist ketanserin is an open channel blocker of human cardiac ether-à-go-go-related gene (hERG) potassium channels.

British Journal Of Pharmacology

Tang, Q Q; Li, Z-Q ZQ; Li, W W; Guo, J J; Sun, H-Y HY; Zhang, X-H XH; Lau, C-P CP; Tse, H-F HF; Zhang, S S; Li, G-R GR

Publication Date: 2008-10

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PubMed Link: 18574455

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Acute effects of oestrogen on the guinea pig and human IKr channels and drug-induced prolongation of cardiac repolarization.

The Journal Of Physiology

Kurokawa, Junko J; Tamagawa, Masaji M; Harada, Nobuhiro N; Honda, Shin-Ichiro S; Bai, Chang-Xi CX; Nakaya, Haruaki H; Furukawa, Tetsushi T

Publication Date: 2008-06-15

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PubMed Link: 18440994

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Probing the binding sites and mechanisms of action of two human ether-a-go-go-related gene channel activators, 1,3-bis-(2-hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643) and 2-[2-(3,4-dichloro-phenyl)-2,3-dihydro-1H-isoindol-5-ylamino]-nicotinic acid (PD307243).

Molecular Pharmacology

Xu, Xulin X; Recanatini, Maurizio M; Roberti, Marinella M; Tseng, Gea-Ny GN

Publication Date: 2008-06

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PubMed Link: 18372399

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Doxazosin induces apoptosis of cells expressing hERG K+ channels.

European Journal Of Pharmacology

Thomas, Dierk D; Bloehs, Ramona R; Koschny, Ronald R; Ficker, Eckhard E; Sykora, Jaromir J; Kiehn, Johann J; Schlömer, Kathrin K; Gierten, Jakob J; Kathöfer, Sven S; Zitron, Edgar E; Scholz, Eberhard P EP; Kiesecker, Claudia C; Katus, Hugo A HA; Karle, Christoph A CA

Publication Date: 2008-01-28

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PubMed Link: 18054910

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Coexistence of hERG current block and disruption of protein trafficking in ketoconazole-induced long QT syndrome.

British Journal Of Pharmacology

Takemasa, H H; Nagatomo, T T; Abe, H H; Kawakami, K K; Igarashi, T T; Tsurugi, T T; Kabashima, N N; Tamura, M M; Okazaki, M M; Delisle, B P BP; January, C T CT; Otsuji, Y Y

Publication Date: 2008-02

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PubMed Link: 17965736

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Structural basis of action for a human ether-a-go-go-related gene 1 potassium channel activator.

Proceedings Of The National Academy Of Sciences Of The United States Of America

Perry, Matthew M; Sachse, Frank B FB; Sanguinetti, Michael C MC

Publication Date: 2007-08-21

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PubMed Link: 17693551

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Inhibition of the HERG potassium channel by the tricyclic antidepressant doxepin.

Biochemical Pharmacology

Duncan, R S RS; McPate, M J MJ; Ridley, J M JM; Gao, Z Z; James, A F AF; Leishman, D J DJ; Leaney, J L JL; Witchel, H J HJ; Hancox, J C JC

Publication Date: 2007-08-01

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PubMed Link: 17560554

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Mechanism of hERG K+ channel blockade by the fluoroquinolone antibiotic moxifloxacin.

British Journal Of Pharmacology

Alexandrou, Ari J AJ; Duncan, Rona S RS; Sullivan, Anneli A; Hancox, Jules C JC; Leishman, Derek J DJ; Witchel, Harry J HJ; Leaney, Joanne L JL

Publication Date: 2006-04

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PubMed Link: 16474415

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Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy.

British Journal Of Pharmacology

Kawakami, Kazunobu K; Nagatomo, Toshihisa T; Abe, Haruhiko H; Kikuchi, Kan K; Takemasa, Hiroko H; Anson, Blake D BD; Delisle, Brian P BP; January, Craig T CT; Nakashima, Yasuhide Y

Publication Date: 2006-03

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PubMed Link: 16314852

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Inhibition of cardiac HERG currents by the DNA topoisomerase II inhibitor amsacrine: mode of action.

British Journal Of Pharmacology

Thomas, Dierk D; Hammerling, Bettina C BC; Wu, Kezhong K; Wimmer, Anna-Britt AB; Ficker, Eckhard K EK; Kirsch, Glenn E GE; Kochan, Mary C MC; Wible, Barbara A BA; Scholz, Eberhard P EP; Zitron, Edgar E; Kathöfer, Sven S; Kreye, Volker A W VA; Katus, Hugo A HA; Schoels, Wolfgang W; Karle, Christoph A CA; Kiehn, Johann J

Publication Date: 2004-06

Variant appearance in text: HERG: Y652A

PubMed Link: 15148258

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Blockade of HERG potassium currents by fluvoxamine: incomplete attenuation by S6 mutations at F656 or Y652.

British Journal Of Pharmacology

Milnes, James T JT; Crociani, Olivia O; Arcangeli, Annarosa A; Hancox, Jules C JC; Witchel, Harry J HJ

Publication Date: 2003-07

Variant appearance in text: HERG: Y652A

PubMed Link: 12839862

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Position of aromatic residues in the S6 domain, not inactivation, dictates cisapride sensitivity of HERG and eag potassium channels.

Proceedings Of The National Academy Of Sciences Of The United States Of America

Chen, Jun J; Seebohm, Guiscard G; Sanguinetti, Michael C MC

Publication Date: 2002-09-17

Variant appearance in text: HERG: Y652A

PubMed Link: 12209010

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A structural basis for drug-induced long QT syndrome.

Proceedings Of The National Academy Of Sciences Of The United States Of America

Mitcheson, J S JS; Chen, J J; Lin, M M; Culberson, C C; Sanguinetti, M C MC

Publication Date: 2000-10-24

Variant appearance in text: HERG: Y652A

PubMed Link: 11005845

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