Facilitation of hERG Activation by Its Blocker: A Mechanism to Reduce Drug-Induced Proarrhythmic Risk by Kazuharu Furutani

Subjects: “…hERG channel…”
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The S4-S5 linker acts as a signal integrator for HERG K+ channel activation and deactivation gating. by Chai Ann Ng, Matthew D Perry, Peter S Tan, Adam P Hill, Philip W Kuchel, Jamie I Vandenberg

“…Human ether-à-go-go-related gene (hERG) K(+) channels have unusual gating kinetics. …”
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Computational prediction of hERG blockers using homology modelling, molecular docking and QuaSAR studies by Nataraj Sekhar Pagadala

Subjects: “…hERG…”
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Changes in channel trafficking and protein stability caused by LQT2 mutations in the PAS domain of the HERG channel. by Carol A Harley, Catarina S H Jesus, Ricardo Carvalho, Rui M M Brito, João H Morais-Cabral

“…Inherited human long-QT2 syndrome (LQTS) results from mutations in the gene encoding the HERG channel. Several LQT2-associated mutations have been mapped to the amino terminal cytoplasmic Per-Arnt-Sim (PAS) domain of the HERG1a channel subunit. …”
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Modelling effects of Sotalol on Action Potential morphology using a novel Markov model of the HERG channel by Brennan, T, Fink, M, Rodriguez, B, Tarassenko, L

The faint source population at 15.7 GHz – III. A high-frequency study of HERGs and LERGs by Whittam, I, Riley, J, Green, D, Jarvis, M

“…Optical spectra are used to classify 17 of the sources as high-excitation or low-excitation radio galaxies (HERGs and LERGs, respectively), for the remaining sources three other methods are used; these are optical compactness, X-ray observations and mid-infrared colour-colour diagrams. 32 sources are HERGs and 35 are LERGs while the remaining 29 sources could not be classified. …”

Application of Human Stem Cell−derived Cardiomyocytes in Safety Pharmacology Requires Caution Beyond hERG by Jonsson, M, Vos, M, Mirams, G, Duker, G, Sartipy, P, de Boer, T, van Veen, T

“…The only compound that triggered EADs was hERG blocker Cisapride. Computer simulations and APclamp showed that the immature AP of hESC-CM prevents proper functioning of INa-channels, and result in lower peak/maximal currents of several other channels, compared to the adult situation. …”

Application of human stem cell-derived cardiomyocytes in safety pharmacology requires caution beyond hERG by Jonsson, M, Vos, M, Mirams, G, Duker, G, Sartipy, P, De Boer, T, Van Veen, T

“…The only compound that triggered EADs was hERG blocker Cisapride. Computer simulations and AP clamp showed that the immature AP of hESC-CM prevents proper functioning of I Na-channels, and result in lower peak/maximal currents of several other channels, compared to the adult situation. …”

Application of human stem cell-derived cardiomyocytes in safety pharmacology requires caution beyond hERG. by Jonsson, M, Vos, M, Mirams, G, Duker, G, Sartipy, P, de Boer, T, van Veen, T

“…The only compound that triggered EADs was hERG blocker Cisapride. Computer simulations and AP clamp showed that the immature AP of hESC-CM prevents proper functioning of I(Na)-channels, and result in lower peak/maximal currents of several other channels, compared to the adult situation. …”

Modelling effects of Sotalol on Action Potential morphology using a novel Markov model of the HERG channel by Brennan, T, Fink, M, Rodriguez, B, Tarassenko, LT

The faint source population at 15.7 GHz - III. A high-frequency study of HERGs and LERGs by Whittam, I, Riley, J, Green, D, Jarvis, M

“…Optical spectra are used to classify 17 of the sources as high-excitation or low-excitation radio galaxies (HERGs and LERGs respectively), for the remaining sources three other methods are used; these are optical compactness, X-ray observations and mid-infrared colour--colour diagrams. 32 sources are HERGs and 35 are LERGs while the remaining 29 sources could not be classified. …”

Spirocycle MmpL3 Inhibitors with Improved hERG and Cytotoxicity Profiles as Inhibitors of Mycobacterium tuberculosis Growth by Peter C. Ray, Margaret Huggett, Penelope A. Turner, Malcolm Taylor, Laura A. T. Cleghorn, Julie Early, Anuradha Kumar, Shilah A. Bonnett, Lindsay Flint, Douglas Joerss, James Johnson, Aaron Korkegian, Steven Mullen, Abraham L. Moure, Susan H. Davis, Dinakaran Murugesan, Michael Mathieson, Nicola Caldwell, Curtis A. Engelhart, Dirk Schnappinger, Ola Epemolu, Fabio Zuccotto, Jennifer Riley, Paul Scullion, Laste Stojanovski, Lisa Massoudi, Gregory T. Robertson, Anne J. Lenaerts, Gail Freiberg, Dale J. Kempf, Thierry Masquelin, Philip A. Hipskind, Joshua Odingo, Kevin D. Read, Simon R. Green, Paul G. Wyatt, Tanya Parish

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Evolutionary coupling analysis guides identification of mistrafficking-sensitive variants in cardiac K+ channels: Validation with hERG by Yihong Zhang, Amy L. Grimwood, Jules C. Hancox, Stephen C. Harmer, Christopher E. Dempsey

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Validation of a [3H]Astemizole Binding Assay in HEK293 Cells Expressing HERG K+ Channels by Peter J.S. Chiu, Karen F. Marcoe, Sidney E. Bounds, Chun-Hsiung Lin, Jin-Jye Feng, Atsui Lin, Fong-Chi Cheng, William J. Crumb, Richard Mitchell

“…Pharmacological characterization of the [3H]astemizole binding assay for HERG K+ channels was performed using HERG-expressing HEK293 cells. …”
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Pharmacologic Approach to Defective Protein Trafficking in the E637K-hERG Mutant with PD-118057 and Thapsigargin. by Haiyan Mao, Xiaoli Lu, Justin Michael Karush, Xiaoyan Huang, Xi Yang, Yanna Ba, Ying Wang, Ningsheng Liu, Jianqing Zhou, Jiangfang Lian

“…Furthermore, the effect of PD-118057 and thapsigargin on the dominant negative E637K-hERG mutant has not been previously investigated.IN THIS STUDY, WE INVESTIGATED: (a) the effect of PD-118057 and thapsigargin on the current amplitudes of WT-hERG and WT/E637K-hERG channels; (b) the effect of PD-118057 and thapsigargin on the biophysical properties of WT-hERG and WT/E637K-hERG channels; (c) whether drug treatment can rescue channel processing and trafficking defects of the WT/E637K-hERG mutant.The whole-cell Patch-clamp technique was used to assess the effect of PD-118057 and thapsigargin on the electrophysiological characteristics of the rapidly activating delayed rectifier K(+) current (Ikr) of the hERG protein channel. …”
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Chaperone Rer1 involves in transport of hERG potassium channel protein in cell line HEK293T by CHEN Bang-sheng, YU Xiao-ling, MAO Fei-yan, LIAN Jiang-fang, YU Xu-yun

Subjects: “…chaperone|rer1|herg|lqts…”
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Suppression of hERG K+ current and cardiac action potential prolongation by 4-hydroxynonenal via dual mechanisms by Seong Woo Choi, Si Won Choi, Young Keul Jeon, Sung-Hwan Moon, Yin-Hua Zhang, Sung Joon Kim

“…Western blot analysis using surface biotinylation revealed a reduction in mature membrane hERG protein after treatment with 4-HNE10L. Proteasomal degradation inhibitors, such as bortezomib, prevented the 4-HNE10L-induced decrease in mature hERG, suggesting a retrograde degradation of membrane hERG due to 4-HNE. …”
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Variable Expression of Long QT Syndrome Among Gene Carriers from Families with Five Different HERG Mutations by Jesaia Benhorin, Arthur J. Moss, Matthew Bak, Wojciech Zareba, Elizabeth S. Kaufman, Batsheva Kerem, Jeffrey A. Towbin, Silvia Priori, Robert S. Kass, Bernard Attali, Arthur M. Brown, Eckhard Ficker

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Recognition of high-specificity hERG K+ channel inhibitor-induced arrhythmia in cardiomyocytes by automated template matching by Hao Wang, Hongbo Li, Xinwei Wei, Tao Zhang, Yuting Xiang, Jiaru Fang, Peiran Wu, Xi Xie, Ping Wang, Ning Hu

“…Arrhythmia induced by gene mutations, heart disease, or hERG K+ channel inhibitors is a serious CVD that can lead to sudden death or heart failure. …”
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Multiple mechanisms underlie reduced potassium conductance in the p.T1019PfsX38 variant of hERG by Majid K. Al Salmani, Rezvan Tavakoli, Wajid Zaman, Ahmed Al Harrasi

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