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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 (Cambridge), ISSN 0092-8674, 04/2017, Volume 169, Issue 3, pp. 422 - 430.e10
K+ channel | drug-induced Long QT | hERG | voltage-dependent gating | inactivation | hERG block | cryo-EM | structure | channel | Biochemistry & Molecular Biology | Life Sciences & Biomedicine | Science & Technology | 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 | Index Medicus
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2. Full Text Targeting the Kv11.1 (hERG) channel with allosteric modulators. Synthesis and biological evaluation of three novel series of LUF7346 derivatives
by van Veldhoven, Jacobus P.D and Campostrini, Giulia and van Gessel, Constantijn J.E and Ward-van Oostwaard, Dorien and Liu, Rongfang and Mummery, Christine L and Bellin, Milena and IJzerman, Adriaan P
European journal of medicinal chemistry, ISSN 0223-5234, 2020, pp. 113033 - 113033
hiPSC-derived cardiomyocytes | LUF7346 | Human induced pluripotent stem cells (hiPSCs) | Dofetilide | Cardiotoxicity | Allosteric modulation | Kv11.1 (hERG) channel | 11.1 (hERG) channel | Index Medicus
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3. 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
KCNH2 | safety assessment | drug sensitivity | hERG | torsades de pointes | hERG 1a | hERG 1b | arrhythmia | hERG blockers | Kv11.1 | 11.1 | Life Sciences & Biomedicine | Pharmacology & Pharmacy | Science & Technology | 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 | Index Medicus | Research Papers
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4. 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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5. Full Text Identification of Quinoline-Based RIP2 Kinase Inhibitors with an Improved Therapeutic Index to the hERG Ion Channel
by Haile, Pamela A and Casillas, Linda N and Bury, Michael J and Mehlmann, John F and Singhaus, Robert and Charnley, Adam K and Hughes, Terry V and DeMartino, Michael P and Wang, Gren Z and Romano, Joseph J and Dong, Xiaoyang and Plotnikov, Nikolay V and Lakdawala, Ami S and Convery, Maire A and Votta, Bartholomew J and Lipshutz, David B and Desai, Biva M and Swift, Barbara and Capriotti, Carol A and Berger, Scott B and Mahajan, Mukesh K and Reilly, Michael A and Rivera, Elizabeth J and Sun, Helen H and Nagilla, Rakesh and LePage, Carol and Ouellette, Michael T and Totoritis, Rachel D and Donovan, Brian T and Brown, Barry S and Chaudhary, Khuram W and Gough, Peter J and Bertin, John and Marquis, Robert W
ACS medicinal chemistry letters, ISSN 1948-5875, 10/2018, Volume 9, Issue 10, pp. 1039 - 1044
kinase inhibitor | hERG | NOD1 | NOD2 | RIP2
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6. Full Text Interactions between amiodarone and the hERG potassium channel pore determined with mutagenesis and in silico docking
by Zhang, Yihong and Colenso, Charlotte K and El Harchi, Aziza and Cheng, Hongwei and Witchel, Harry J and Dempsey, Chris E and Hancox, Jules C
Biochemical pharmacology, ISSN 0006-2952, 08/2016, Volume 113, pp. 24 - 35
Antiarrhythmic | IKr | QT interval | hERG | Amiodarone | Long QT | Life Sciences & Biomedicine | Pharmacology & Pharmacy | Science & Technology | Amino Acid Sequence | Action Potentials - genetics | Anti-Arrhythmia Agents - pharmacology | Humans | Dose-Response Relationship, Drug | Patch-Clamp Techniques | Transfection | Alanine - genetics | Mutagenesis | HEK293 Cells | Protein Binding | ERG1 Potassium Channel - genetics | Molecular Docking Simulation | ERG1 Potassium Channel - antagonists & inhibitors | Mutation | Action Potentials - drug effects | Amiodarone - pharmacology | Potassium channels | Index Medicus | IC50, half-maximal inhibitory concentration | IKs, slow delayed rectifier potassium current | diLQTS, drug induced long QT syndrome | hERG, human-Ether-à-go-go-Related Gene | HEK, human embryonic kidney | IKr, rapid delayed rectifier potassium current | LQTS, long QT syndrome | DEA, desethylamiodarone | AF, atrial fibrillation | IhERG, ionic current carried by hERG potassium channels | I Kr
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7. Full Text 6‑Cyano Analogues of Bedaquiline as Less Lipophilic and Potentially Safer Diarylquinolines for Tuberculosis
by Tong, Amy S. T and Choi, Peter J and Blaser, Adrian and Sutherland, Hamish S and Tsang, Sophia K. Y and Guillemont, Jerome and Motte, Magali and Cooper, Christopher B and Andries, Koen and Van den Broeck, Walter and Franzblau, Scott G and Upton, Anna M and Denny, William A and Palmer, Brian D and Conole, Daniel
ACS medicinal chemistry letters, ISSN 1948-5875, 10/2017, Volume 8, Issue 10, pp. 1019 - 1024
lipophilicity | ATP synthase | diarylquinoline | hERG | Bedaquiline | tuberculosis
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8. Full Text Effects of trimethoprim–sulfadiazine and detomidine on the function of equine K v 11.1 channels in a two-electrode voltage-clamp (TEVC) oocyte model
by Trachsel, D.S and Tejada, M.A and Groesfjeld Christensen, V and Pedersen, P.J and Kanters, J.K and Buhl, R and Calloe, K and Klaerke, D.A
Journal of veterinary pharmacology and therapeutics, ISSN 0140-7783, 08/2018, Volume 41, Issue 4, pp. 536 - 545
Repolarization | acquired LQTS | hERG | potassium channels | heart
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9. Full Text Two mutations at different positions in the CNBH domain of the hERG channel accelerate deactivation and impair the interaction with the EAG domain
by Kume, Shinichiro and Shimomura, Takushi and Tateyama, Michihiro and Kubo, Yoshihiro
The Journal of physiology, ISSN 0022-3751, 10/2018, Volume 596, Issue 19, pp. 4629 - 4650
hERG channel | FRET | deactivation | Neurosciences | Physiology | Neurosciences & Neurology | Life Sciences & Biomedicine | Science & Technology | Deactivation | HERG protein | Ligands | Homology | Potassium channels (voltage-gated) | Fluorescence resonance energy transfer | Mutation | Index Medicus | Molecular and Cellular | Research Paper
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10. Full Text Design, synthesis and evaluation of benzothiazole derivatives as multifunctional agents
by Djuidje, Ernestine Nicaise and Sciabica, Sabrina and Buzzi, Raissa and Dissette, Valeria and Balzarini, Jan and Liekens, Sandra and Serra, Elena and Andreotti, Elisa and Manfredini, Stefano and Vertuani, Silvia and Baldisserotto, Anna
Bioorganic chemistry, ISSN 0045-2068, 08/2020, Volume 101, pp. 103960 - 103960
Antiproliferative | Antifungal | hERG channels | UV-filter | Antioxidant | Benzothiazoles | Index Medicus
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11. Full Text Off-label use of chloroquine, hydroxychloroquine, azithromycin and lopinavir/ritonavir in COVID-19 risks prolonging the QT interval by targeting the hERG channel
by Zequn, Zheng and Yujia, Wu and Dingding, Qian and Jiangfang, Lian
European journal of pharmacology, 12/2020, Volume 893, pp. 173813 - 173813
Index Medicus
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12. Full Text A receptor-independent effect of estrone sulfate on the hERG channel
by Kakusaka, Shoko and Asayama, Mahoko and Kaihara, Asami and Sasano, Tetsuo and Suzuki, Takeshi and Kurokawa, Junko and Furukawa, Tetsushi
Journal of pharmacological sciences, ISSN 1347-8613, 2009, Volume 109, Issue 1, pp. 152 - 156
Heart | channel (hERG) | Estrogen | Index Medicus
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13. Full Text Development of autotaxin inhibitors: A series of tetrazole cinnamides
by Thomson, Christopher G and Le Grand, Darren and Dowling, Mark and Beattie, David and Elphick, Lucy and Faller, Michael and Freeman, Mark and Hardaker, Elizabeth and Head, Victoria and Hemmig, Rene and Hill, Johan and Lister, Andrew and Pascoe, David and Rieffel, Sebastien and Shrestha, Binesh and Steward, Oliver and Zink, Florence
Bioorganic & medicinal chemistry letters, ISSN 0960-894X, 01/2021, Volume 31, pp. 127663 - 127663
hERG inhibition | PK/PD | Autotaxin inhibition | Clearance | Idiopathic pulmonary fibrosis | Index Medicus
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14. Full Text Heteroaryl ether analogues of an antileishmanial 7-substituted 2-nitroimidazooxazine lead afford attenuated hERG risk: In vitro and in vivo appraisal
by Thompson, Andrew M and O’Connor, Patrick D and Marshall, Andrew J and Yardley, Vanessa and Maes, Louis and Gupta, Suman and Launay, Delphine and Braillard, Stephanie and Chatelain, Eric and Wan, Baojie and Franzblau, Scott G and Ma, Zhenkun and Cooper, Christopher B and Denny, William A
European journal of medicinal chemistry, ISSN 0223-5234, 01/2021, Volume 209, pp. 112914 - 112914
Chagas disease | Pretomanid | hERG inhibition | in vivo efficacy | Leishmaniasis | Pharmacokinetics | Index Medicus
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15. Full Text The hERG K + channel: target and antitarget strategies in drug development
by Raschi, Emanuel and Vasina, Valentina and Poluzzi, Elisabetta and De Ponti, Fabrizio
Pharmacological research, ISSN 1043-6618, 2008, Volume 57, Issue 3, pp. 181 - 195
QT interval | HERG K + channels | Arrhythmia | Drug development | Torsades de pointes | HERG K | channels | Life Sciences & Biomedicine | Pharmacology & Pharmacy | Science & Technology | Ether-A-Go-Go Potassium Channels - antagonists & inhibitors | Arrhythmias, Cardiac - drug therapy | Animals | Ether-A-Go-Go Potassium Channels - drug effects | Humans | Potassium Channel Blockers - therapeutic use | Ether-A-Go-Go Potassium Channels - physiology | Long QT Syndrome - drug therapy | Torsades de Pointes - drug therapy | Arrhythmias, Cardiac - physiopathology | Potassium Channel Blockers - pharmacology | Neoplasms - drug therapy | Index Medicus
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