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1. Full Text Cryo-EM Structure of the Open Human Ether-à-go-go-Related K+ Channel hERG
by Wang, Weiwei and MacKinnon, Roderick
Cell, ISSN 0092-8674, 04/2017, Volume 169, Issue 3, pp. 422 - 430.e10
The human -related potassium channel (hERG, Kv11.1) is a voltage-dependent channel known for its role in repolarizing the cardiac action potential. hERG... 
K+ channel | drug-induced Long QT | hERG | voltage-dependent gating | inactivation | hERG block | cryo-EM | structure | channel | INACTIVATION | HUMAN INWARD RECTIFIER | POTASSIUM CHANNELS | DETERMINANTS | BIOCHEMISTRY & MOLECULAR BIOLOGY | PURIFICATION | BLOCK | CARDIAC-ARRHYTHMIA | PROLONGATION | LONG-QT SYNDROME | PROTEINS | CELL BIOLOGY | Cryoelectron Microscopy | Amino Acid Sequence | Sequence Alignment | ERG1 Potassium Channel - ultrastructure | ERG1 Potassium Channel - chemistry | Humans | Models, Molecular | Protein Conformation | ERG1 Potassium Channel - isolation & purification | ERG1 Potassium Channel - metabolism
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2. Full Text Theoretical evaluation of ADMET properties for coumarin derivatives as compounds with therapeutic potential
by Żołek, Teresa and Maciejewska, Dorota
European Journal of Pharmaceutical Sciences, ISSN 0928-0987, 11/2017, Volume 109, pp. 486 - 502
Coumarins have received a considerable attention in the last three decades as the lead structures for the discovery of orally administrated chemotherapeutics.... 
7-Hydroxycoumarin derivatives | hERG K+ channel | Molecular docking and molecular dynamics | ADMET theoretical properties | channel | hERG K | hERG K plus channel | TORSADES-DE-POINTES | BINDING MODE | VIVO | NATURAL-PRODUCTS | DRUG DISCOVERY | IN-VITRO | HERG | METABOLISM | BIOLOGICAL EVALUATION | PHARMACOLOGY & PHARMACY | CHANNEL BLOCKERS | Humans | Coumarins - pharmacokinetics | Cytochrome P-450 Enzyme System - metabolism | Biological Availability | Coumarins - chemistry | ERG1 Potassium Channel - metabolism | Blood Proteins - metabolism | Molecular Dynamics Simulation | Blood-Brain Barrier - metabolism | Jejunum - metabolism | Models, Biological | 1-Octanol - chemistry | Water - chemistry | Ligands | Coumarins - toxicity | Coumarins | Health aspects | Analysis | Molecular dynamics | Adsorption | Index Medicus
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3. Full Text Antiarrhythmic properties of phenylpiperazine derivatives of phenytoin with α 1-adrenoceptor affinities
by Handzlik, Jadwiga and Bajda, Marek and Zygmunt, Małgorzata and MacIg, Dorota and Dybała, Małgorzata and Bednarski, Marek and Filipek, Barbara and Malawska, Barbara and Kieć-Kononowicz, Katarzyna
Bioorganic and Medicinal Chemistry, ISSN 0968-0896, 04/2012, Volume 20, Issue 7, pp. 2290 - 2303
An association between α -adrenoceptor affinities, hERG K -antagonistic properties and antiarrhythmic activities for a series of phenylpiperazine derivatives... 
hERG | Phenylpiperazine | Antiarrhythmic activity | Hydantoin
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4. Full Text The influence of hERG1a and hERG1b isoforms on drug safety screening in iPSC-CMs
by Goversen, Birgit and Jonsson, Malin Kb and van den Heuvel, Nikki Hl and Rijken, Rianne and Vos, Marc A and van Veen, Toon Ab and de Boer, Teun P
Progress in biophysics and molecular biology, ISSN 0079-6107, 02/2019
The human Ether-à-go-go Related Gene (hERG) encodes the pore forming subunit of the channel that conducts the rapid delayed rectifier potassium current I . I... 
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5. Full Text Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pKa Polar Moiety
by Ndubaku, Chudi O and Crawford, James J and Drobnick, Joy and Aliagas, Ignacio and Campbell, David and Dong, Ping and Dornan, Laura M and Duron, Sergio and Epler, Jennifer and Gazzard, Lewis and Heise, Christopher E and Hoeflich, Klaus P and Jakubiak, Diana and La, Hank and Lee, Wendy and Lin, Baiwei and Lyssikatos, Joseph P and Maksimoska, Jasna and Marmorstein, Ronen and Murray, Lesley J and O'Brien, Thomas and Oh, Angela and Ramaswamy, Sreemathy and Wang, Weiru and Zhao, Xianrui and Zhong, Yu and Blackwood, Elizabeth and Rudolph, Joachim
ACS Medicinal Chemistry Letters, ISSN 1948-5875, 12/2015, Volume 6, Issue 12, pp. 1241 - 1246
Kinase inhibitor | hERG | oncology
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6. Full Text A multiscale computational modelling approach predicts mechanisms of female sex risk in the setting of arousal‐induced arrhythmias
by Yang, Pei‐Chi and Perissinotti, Laura L and López‐Redondo, Fernando and Wang, Yibo and DeMarco, Kevin R and Jeng, Mao‐Tsuen and Vorobyov, Igor and Harvey, Robert D and Kurokawa, Junko and Noskov, Sergei Y and Clancy, Colleen E
The Journal of Physiology, ISSN 0022-3751, 07/2017, Volume 595, Issue 14, pp. 4695 - 4723
This study represents a first step toward predicting mechanisms of sex‐based arrhythmias that may lead to important developments in risk stratification and may... 
TdP | arrhythmias | hERG mutation | long‐QT | computational model | sex‐differences | dofetilide | sex-differences | long-QT | MENSTRUAL-CYCLE | PHYSIOLOGY | DRUG-BINDING | CARDIAC ION CHANNELS | LONG-QT SYNDROME | NEUROSCIENCES | VENTRICULAR REPOLARIZATION | FORCE-FIELD | HERG POTASSIUM CHANNEL | MOLECULAR-DYNAMICS SIMULATIONS | RABBIT HEARTS | AUTONOMIC NERVOUS-SYSTEM | Guinea Pigs | Phenethylamines - pharmacology | Anti-Arrhythmia Agents - pharmacology | Adrenergic beta-Agonists - pharmacology | Male | Sex Characteristics | Sulfonamides - pharmacology | Arrhythmias, Cardiac - physiopathology | Arousal - physiology | Animals | Models, Biological | Myocytes, Cardiac - physiology | Isoproterenol - pharmacology | Female | Ether-A-Go-Go Potassium Channels - physiology | Molecular Docking Simulation | Estradiol - pharmacology | Medical research | Computer-generated environments | Arrhythmia | Computer simulation | Estrogen | Medicine, Experimental | Progesterone | Risk factors | Cardiac arrhythmia | HERG protein | Molecular structure | Sex | Risk | Stimulation | Nervous system | Myocytes | Drug development | Arousal | Potassium channels (voltage-gated) | Mathematical models | Sexual behavior | Sympathetic nervous system | Patients | Discharge | Testosterone | Screening | Molecular modelling | Computer applications | Ventricle | Mutation | Females | Binding sites | Structure-function relationships | Cardiovascular | Research Paper
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7. Full Text Potent hERG channel inhibition by sarizotan, an investigative treatment for Rett Syndrome
by Cheng, Hongwei and Du, Chunyun and Zhang, Yihong and James, Andrew F and Dempsey, Christopher E and Abdala, Ana P and Hancox, Jules C
Journal of Molecular and Cellular Cardiology, ISSN 0022-2828, 10/2019, Volume 135, pp. 22 - 30
Rett Syndrome (RTT) is an X-linked neurodevelopmental disorder associated with respiratory abnormalities and, in up to ~40% of patients, with prolongation of... 
KCNH2 | Long QT syndrome | hERG | Rett Syndrome | Sarizotan
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8. Full Text hERG subunit composition determines differential drug sensitivity
by Abi‐Gerges, N and Holkham, H and Jones, EMC and Pollard, CE and Valentin, J‐P and Robertson, GA
British Journal of Pharmacology, ISSN 0007-1188, 09/2011, Volume 164, Issue 2b, pp. 419 - 432
BACKGROUND AND PURPOSE The majority of human ether‐a‐go‐go‐related gene (hERG) screens aiming to minimize the risk of drug‐induced long QT syndrome have been... 
KCNH2 | safety assessment | drug sensitivity | hERG | torsades de pointes | hERG 1a | 11.1 | hERG 1b | arrhythmia | hERG blockers | INTERVAL PROLONGATION | HIGH-THROUGHPUT | CARDIAC-ARRHYTHMIA | I-KR | MOLECULAR DETERMINANTS | LONG-QT SYNDROME | ELECTROPHYSIOLOGICAL CHARACTERIZATION | K(v)11.1 | OPEN-CHANNEL BLOCK | PHARMACOLOGY & PHARMACY | K+ CHANNEL | POTASSIUM CHANNEL | Drug Evaluation, Preclinical - methods | Fluoxetine - pharmacology | Protein Subunits | Arrhythmias, Cardiac - chemically induced | Humans | Torsades de Pointes - chemically induced | Torsades de Pointes - genetics | Long QT Syndrome - chemically induced | Ether-A-Go-Go Potassium Channels - genetics | Ether-A-Go-Go Potassium Channels - antagonists & inhibitors | Piperidines - pharmacology | Sensitivity and Specificity | HEK293 Cells | Inhibitory Concentration 50 | Long QT Syndrome - genetics | Pyridines - pharmacology | Action Potentials - drug effects | Arrhythmias, Cardiac - genetics | Cell Line, Transformed | Research Papers | Kv11.1
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9. Full Text Discovery and pharmacological profile of new hydrophilic 5-HT4receptor antagonists
by Brudeli, Bjarne and Navaratnarajah, Mirusha and Andressen, Kjetil Wessel and Manfra, Ornella and Moltzau, Lise Román and Nilsen, Nils Olav and Levy, Finn Olav and Klaveness, Jo
Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 09/2014, Volume 24, Issue 18, pp. 4598 - 4602
The synthesis and pharmacological data of some new and potent hydrophilic 5-HT receptor antagonists are described. Propanediol derivative 25 was identified as... 
hERG | receptor antagonists | 5-HT | Pharmacokinetic
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10. Full Text Evaluation of Possible Proarrhythmic Potency: Comparison of the Effect of Dofetilide, Cisapride, Sotalol, Terfenadine, and Verapamil on hERG and Native IKr Currents and on Cardiac Action Potential
by Orvos, Péter and Kohajda, Zsófia and Szlovák, Jozefina and Gazdag, Péter and Árpádffy-Lovas, Tamás and Tóth, Dániel and Geramipour, Amir and Tálosi, László and Jost, Norbert and Varró, András and Virág, László
Toxicological Sciences, ISSN 1096-6080, 04/2019, Volume 168, Issue 2, pp. 365 - 380
Abstract The proarrhythmic potency of drugs is usually attributed to the IKr current block. During safety pharmacology testing analysis of IKr in... 
hERG | safety pharmacology | cardiac action potential | proarrhythmia | I Kr
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11. Full Text Validation and Clinical Utility of the hERG IC50:Cmax Ratio to Determine the Risk of Drug‐Induced Torsades de Pointes: A Meta‐Analysis
by Lehmann, David F and Eggleston, William D and Wang, Dongliang
Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy, ISSN 0277-0008, 03/2018, Volume 38, Issue 3, pp. 341 - 348
Use of the QT interval corrected for heart rate (QTc) on the electrocardiogram (ECG) to predict torsades de pointes (TdP) risk from culprit drugs is neither... 
TdP risk | hERG IC | max | pharmacometrics | drug induced | meta‐analysis | 50:C | meta-analysis | hERG IC50:C | Decision-making | Antihistamines | Heart beat | Arrhythmia | Electrocardiogram | Electrocardiography | Epidemiology | Drugs | Correlation | Neuroleptics | HERG protein | Olanzapine | Calcium | Risk | Haloperidol | Drug development | Incidence | Confidence intervals | Torsades de pointes | Drug interaction | Potassium channels (voltage-gated) | Magnesium | Risperidone | EKG | Echocardiography | Decision making | Ziprasidone | Drug interactions | Exposure | Heart rate | Thioridazine | Ciprofloxacin | Potassium | Prolongation
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12. Full Text The role and mechanism of chaperones Calnexin/Calreticulin in which ALLN selectively rescues the trafficking defective of HERG-A561V mutation
by Wang, Ying and Shen, Tingting and Fang, Peiliang and Zhou, Junbo and Lou, Kenan and Cen, Zemin and Qian, Hai and Zhou, Jianqing and Liu, Ningsheng and Lian, Jiangfang
Bioscience Reports, ISSN 0144-8463, 09/2018, Volume 38, Issue 5, p. BSR20171269
Long QT (LQT) type 2 (LQT2) is caused by HERG mutation. L539fs/47 encodes a truncated protein, and its mechanisms in HERG mutation are unknown. HERG mutation... 
PROTEIN | TEMPERATURE | POTASSIUM CHANNELS | ER STRESS | BIOCHEMISTRY & MOLECULAR BIOLOGY | LONG-QT SYNDROME | ENDOPLASMIC-RETICULUM STRESS | QUALITY-CONTROL | PROTEOLYSIS | HERG CHANNELS | ATF6 | CELL BIOLOGY | HERG protein | Immunoprecipitation | Trafficking | Chaperones | Calnexin | Density | Proteins | Lysates | Calreticulin | Clonal deletion | Plasmids | Deletion | Potassium channels (voltage-gated) | Mutation | Protein transport | Propranolol
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13. Full Text Modulation of IKr inactivation by mutation N588K in KCNH2: A link to arrhythmogenesis in short QT syndrome
by Cordeiro, J.M and Brugada, R and Wu, Y.S and Hong, K and Dumaine, R
Cardiovascular Research, ISSN 0008-6363, 08/2005, Volume 67, Issue 3, pp. 498 - 509
Objective: Short QT syndrome (SQTS) is characterized by ventricular arrhythmias and sudden death. One form of SQTS is caused by mutation N588K in human... 
HERG | Short QT | Purkinje | Potassium channel | Arrhythmias
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14. Full Text Keeping it short and (not so) simple: characterizing hERG kinetics with sinusoidal waves
by Grandi, Eleonora
The Journal of Physiology, ISSN 0022-3751, 05/2018, Volume 596, Issue 10, pp. 1783 - 1784
mathematical model | IKr | hERG | Voltage clamp | NEUROSCIENCES | PHYSIOLOGY
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15. Full Text Cotranslational association of mRNA encoding subunits of heteromeric ion channels
by Fang Liu and David K. Jones and Willem J. de Lange and Gail A. Robertson
Proceedings of the National Academy of Sciences of the United States of America, ISSN 0027-8424, 4/2016, Volume 113, Issue 17, pp. 4859 - 4864
Oligomers of homomeric voltage-gated potassium channels associate early in biogenesis as the nascent proteins emerge from the polysome. Less is known about... 
KCNH2 | Microtranslatome | Cotranslational assembly | HERG | HERG 1a/1b | Protein Subunits | Protein Biosynthesis | Immunoprecipitation | Humans | RNA, Messenger - genetics | RNA, Small Interfering - pharmacology | Cells, Cultured | Ether-A-Go-Go Potassium Channels - genetics | RNA, Messenger - metabolism | Transfection | Membrane Potentials | Ryanodine Receptor Calcium Release Channel - genetics | HEK293 Cells | Myocytes, Cardiac - metabolism | Induced Pluripotent Stem Cells - cytology | Potassium Channels, Voltage-Gated - genetics | RNA, Small Interfering - metabolism | Physiological aspects | Ion channels | Messenger RNA | Observations | Genetic translation | Variables | Biomarkers | Mental depression | Sensory perception | Manic depression | Topography | Biological Sciences | hERG | microtranslatome | hERG 1a | cotranslational assembly
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16. Full Text Novel, Selective, and Developable Dopamine D3 Antagonists with a Modified “Amino” Region
by Micheli, Fabrizio
ChemMedChem, ISSN 1860-7179, 08/2017, Volume 12, Issue 16, pp. 1254 - 1260
This Minireview describes a presentation made at the XXIV National Meeting in Medicinal Chemistry (NMMC) held in Perugia (Italy), September 11–14, 2016. It... 
antagonists | hERG | dopamine D | receptors | medicinal chemistry
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