Publications:

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Common Structural Pattern for Flecainide Binding in Atrial-Selective Kv1.5 and Nav1.5 Channels: A Computational Approach.

Pharmaceutics

Mazola, Yuliet Y; Márquez Montesinos, José C E JCE; Ramírez, David D; Zúñiga, Leandro L; Decher, Niels N; Ravens, Ursula U; Yarov-Yarovoy, Vladimir V; González, Wendy W

Publication Date: 2022-06-27

Variant appearance in text: HERG: F656A

PubMed Link: 35890252

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• pharmaceutics-14-01356.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

Variant appearance in text: KCNH2: F656A

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

Variant appearance in text: KCNH2: F656A

PubMed Link: 34727194

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• 18_2021_Article_3967.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

Variant appearance in text: KCNH2: F656A

PubMed Link: 34025432

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• Main text
• fphar-12-675003.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

Variant appearance in text: Kv11.1: F656A

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

Variant appearance in text: HERG: F656A

PubMed Link: 33004839

Variant Present in the following documents:

• 41598_2020_Article_72889.pdf

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The macrolide drug erythromycin does not protect the hERG channel from inhibition by thioridazine and terfenadine.

Physiological Reports

El Harchi, Aziza A; Butler, Andrew S AS; Zhang, Yihong Y; Dempsey, Christopher E CE; Hancox, Jules C JC

Publication Date: 2020-03

Variant appearance in text: KCNH2: F656A

PubMed Link: 32147975

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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

Variant appearance in text: KCNH2: F656A

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

Variant appearance in text: HERG: F656A

PubMed Link: 31667381

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• main.pdf

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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

Variant appearance in text: Kv11.1: F656A

PubMed Link: 31479461

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• Main text
• 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

Variant appearance in text: KCNH2: F656A

PubMed Link: 31362019

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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

Variant appearance in text: HERG: F656A

PubMed Link: 29630634

Variant Present in the following documents:

• 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

Variant appearance in text: HERG: F656A

PubMed Link: 29545312

Variant Present in the following documents:

• zbc7040.pdf

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An unusual etiology of torsade de pointes-induced syncope.

Archives Of Medical Science : Ams

Morosin, Marco M; Dametto, Ermanno E; Bianco, Federica Del FD; Brieda, Marco M; Nicolosi, Gian L GL

Publication Date: 2017-04-01

Variant appearance in text: HERG: F656A

PubMed Link: 28507587

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• Main text
• AMS-13-29834.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

Variant appearance in text: HERG: F656A

PubMed Link: 28337337

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Interactions between amiodarone and the hERG potassium channel pore determined with mutagenesis and in silico docking.

Biochemical Pharmacology

Zhang, Yihong Y; Colenso, Charlotte K CK; El Harchi, Aziza A; Cheng, Hongwei H; Witchel, Harry J HJ; Dempsey, Chris E CE; Hancox, Jules C JC

Publication Date: 2016-08-01

Variant appearance in text: HERG: F656A

PubMed Link: 27256139

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• main.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

Variant appearance in text: HERG: F656A

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

Variant appearance in text: KCNH2: F656A

PubMed Link: 25911606

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The Link between Inactivation and High-Affinity Block of hERG1 Channels.

Molecular Pharmacology

Wu, Wei W; Gardner, Alison A; Sanguinetti, Michael C MC

Publication Date: 2015-06

Variant appearance in text: KCNH2: F656A

PubMed Link: 25855787

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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

Variant appearance in text: HERG: F656A

PubMed Link: 25733807

Variant Present in the following documents:

• dddt-9-867.pdf

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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

Variant appearance in text: HERG: F656A

PubMed Link: 24877995

Variant Present in the following documents:

• mmc1.pdf

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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

Variant appearance in text: HERG: F656A

PubMed Link: 24471705

Variant Present in the following documents:

• Main text
• ci400707h.pdf

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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

Variant appearance in text: KCNH2: F656A

PubMed Link: 23613831

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• Main text
• pone.0061317.pdf

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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

Variant appearance in text: KCNH2: F656A

PubMed Link: 23061993

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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

Variant appearance in text: HERG: F656A

PubMed Link: 22194911

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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

Variant appearance in text: KCNH2: F656A

PubMed Link: 21950687

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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

Variant appearance in text: KCNH2: F656A

PubMed Link: 21833176

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• Main text
• fphar-01-00137.pdf

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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

Variant appearance in text: HERG: F656A

PubMed Link: 21175572

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• Main text

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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

Variant appearance in text: HERG: F656A

PubMed Link: 19885040

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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

Variant appearance in text: HERG: F656A

PubMed Link: 18987434

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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

Variant appearance in text: LQT2: F656A

PubMed Link: 18372399

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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

Variant appearance in text: KCNH2: F656A

PubMed Link: 17965736

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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

Variant appearance in text: HERG: F656A

PubMed Link: 17560554

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Drug-induced long QT syndrome: hERG K+ channel block and disruption of protein trafficking by fluoxetine and norfluoxetine.

British Journal Of Pharmacology

Rajamani, S S; Eckhardt, L L LL; Valdivia, C R CR; Klemens, C A CA; Gillman, B M BM; Anderson, C L CL; Holzem, K M KM; Delisle, B P BP; Anson, B D BD; Makielski, J C JC; January, C T CT

Publication Date: 2006-11

Variant appearance in text: LQT2: F656A

PubMed Link: 16967046

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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

Variant appearance in text: HERG: F656A

PubMed Link: 16474415

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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: F656A

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: F656A

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: F656A

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: F656A

PubMed Link: 11005845

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