Molecular mechanisms underlying the pilsicainide-induced stabilization of hERG proteins in transfected mammalian cells by Takeshi Onohara, MD, Ichiro Hisatome, MD, Yasutaka Kurata, MD, Peili Li, MD, Tomomi Notsu, PhD, Kumi Morikawa, PhD, Naoyuki Otani, MD, Akio Yoshida, MD, Kazuhiko Iitsuka, MD, Masaru Kato, MD, Junichiro Miake, MD, Haruaki Ninomiya, MD, Katsumi Higaki, PhD, Yasuaki Shirayoshi, PhD, Takashi Nishihara, BE, Toshiyuki Itoh, PhD, Yoshinobu Nakamura, MD, Motonobu Nishimura, MD

Subjects: Get full text

Molecular Insights Into the Gating Kinetics of the Cardiac hERG Channel, Illuminated by Structure and Molecular Dynamics by Zheng Zequn, Lian Jiangfang

Subjects: “…HERG potassium channel…”
Get full text

A standardised hERG phenotyping pipeline to evaluate KCNH2 genetic variant pathogenicity by Barbara Oliveira‐Mendes, Sylvain Feliciangeli, Mélissa Ménard, Frank Chatelain, Malak Alameh, Jérôme Montnach, Sébastien Nicolas, Béatrice Ollivier, Julien Barc, Isabelle Baró, Jean‐Jacques Schott, Vincent Probst, Florence Kyndt, Isabelle Denjoy, Florian Lesage, Gildas Loussouarn, Michel De Waard

Subjects: Get full text

hERG Blockade Prediction by Combining Site Identification by Ligand Competitive Saturation and Physicochemical Properties by Himanshu Goel, Wenbo Yu, Alexander D. MacKerell

Subjects: Get full text

The macrolide drug erythromycin does not protect the hERG channel from inhibition by thioridazine and terfenadine by Aziza El Harchi, Andrew S. Butler, Yihong Zhang, Christopher E. Dempsey, Jules C. Hancox

Subjects: Get full text

Winnow based identification of potent hERG inhibitors <it>in silico</it>: comparative assessment on different datasets by Marchese Robinson Richard L, Glen Robert C, Mitchell John BO

The N-terminal tail of hERG contains an amphipathic α-helix that regulates channel deactivation. by Chai Ann Ng, Mark J Hunter, Matthew D Perry, Mehdi Mobli, Ying Ke, Philip W Kuchel, Glenn F King, Daniela Stock, Jamie I Vandenberg

“…The cytoplasmic N-terminal domain of the human ether-a-go-go related gene (hERG) K+ channel is critical for the slow deactivation kinetics of the channel. …”
Get full text

Fluorescent analogues of BeKm-1 with high and specific activity against the hERG channel by Lucie Vasseur, Alain Chavanieu, Stéphanie Combemale, Cécile Caumes, Rémy Béroud, Michel De Waard, Pierre Ducrot, Jean A. Boutin, Gilles Ferry, Thierry Cens

“…All analogues retained their specificity towards the hERG channel in electrophysiological experiments but displayed a lesser affinity. …”
Get full text

Age-dependent electrical and morphological remodeling of the Drosophila heart caused by hERG/seizure mutations. by Karen Ocorr, Alexander Zambon, Yoav Nudell, Santiago Pineda, Soda Diop, Min Tang, Takeshi Akasaka, Erika Taylor

“…One of the primary targets for therapeutic intervention has been the human ether a go-go (hERG) K+ channel that, together with the KCNQ channel, controls the rate and efficiency of repolarization in human myocardial cells. …”
Get full text

hERG-deficient human embryonic stem cell-derived cardiomyocytes for modelling QT prolongation by Yun Chang, Ya-nan Li, Rui Bai, Fujian Wu, Shuhong Ma, Amina Saleem, Siyao Zhang, Youxu Jiang, Tao Dong, Tianwei Guo, Chengwen Hang, Wen-jing Lu, Hongfeng Jiang, Feng Lan

“…Due to the lack of suitable animal and human models, the pathogenesis of LQT2 caused by human ether-a-go-go-related gene (hERG) deficiency is still unclear. In this study, we generated an hERG-deficient human cardiomyocyte (CM) model that simulates ‘human homozygous hERG mutations’ to explore the underlying impact of hERG dysfunction and the genotype–phenotype relationship of hERG deficiency. …”
Get full text

Rapid characterisation of hERG channel kinetics I: using an automated high-throughput system by Lei, CL, Clerx, M, Gavaghan, D, Polonchuk, L, Mirams, GR, Wang, K

“…We demonstrate its use on the Nanion SyncroPatch 384PE, a 384-well automated patch-clamp platform, by applying it to Chinese hamster ovary cells stably expressing hERG1a. From these recordings, we construct 124 cell-specific variants/parameterizations of a hERG model at 25°C. …”

Entre bande dessinée et jeu vidéo: Le Secret de la Licorne d’Hergé by Haniyeh Barahouie

Get full text

Cardiac toxicity of Triptergium wilfordii Hook F. may correlate with its inhibition to hERG channel by Wei Zhao, Liping Xiao, Lanying Pan, Xianfu Ke, Yanting Zhang, Dian Zhong, Jianwei Xu, Fumin Cao, Liren Wu, Yuan Chen

“…By using patch clamp techniques, we found that 0.05 mg/ml and 0.1 mg/ml of the aqueous crude extract of TWHF inhibit 21.4 ± 1.6% and 86.7 ± 5.7% (n = 5) of hERG current Amplitudes (IhERG) respectively. We further found that Celastrol, one of main components of TWHF, inhibits hERG with an IC50 of 0.83 μM. …”
Get full text

Ligand-based prediction of hERG-mediated cardiotoxicity based on the integration of different machine learning techniques by Pietro Delre, Pietro Delre, Giovanna J. Lavado, Giuseppe Lamanna, Giuseppe Lamanna, Michele Saviano, Alessandra Roncaglioni, Emilio Benfenati, Giuseppe Felice Mangiatordi, Domenico Gadaleta

Subjects: “…hERG…”
Get full text

Interleukin-6 inhibition of hERG underlies risk for acquired long QT in cardiac and systemic inflammation. by Ademuyiwa S Aromolaran, Ujala Srivastava, Alessandra Alí, Mohamed Chahine, Deana Lazaro, Nabil El-Sherif, Pier Leopoldo Capecchi, Franco Laghi-Pasini, Pietro Enea Lazzerini, Mohamed Boutjdir

“…In most cases of acquired LQTS, the target ion channel is the human ether-á-go-go-related gene (hERG) encoding the rapid component of the delayed rectifier K current, IKr, which plays a critical role in cardiac repolarization. …”
Get full text

An in Vitro Assay of hERG K+ Channel Potency for a New EGFR Inhibitor FHND004 by Tao Jin, Tao Jin, Bingxue Hu, Shanshan Chen, Shanshan Chen, Qiang Wang, Xue Dong, Yin Zhang, Yongqiang Zhu, Zhao Zhang

“…However, the inhibitory potency of FHND004 on hERG channels was significantly less than its precursor AZD9291. …”
Get full text

The Strength of hERG Inhibition by Erythromycin at Different Temperatures Might Be Due to Its Interacting Features with the Channels by Dongrong Cheng, Xiaofeng Wei, Yanting Zhang, Qian Zhang, Jianwei Xu, Jiaxin Yang, Junjie Yu, Antony Stalin, Huan Liu, Jintao Wang, Dian Zhong, Lanying Pan, Wei Zhao, Yuan Chen

Subjects: Get full text

Determinants of Isoform-Specific Gating Kinetics of hERG1 Channel: Combined Experimental and Simulation Study by Laura L. Perissinotti, Pablo M. De Biase, Jiqing Guo, Pei-Chi Yang, Miranda C. Lee, Colleen E. Clancy, Henry J. Duff, Sergei Y. Noskov

Subjects: Get full text

Parallel Recordings of Transmembrane hERG Channel Currents Based on Solvent-Free Lipid Bilayer Microarray by Ryusuke Miyata, Daisuke Tadaki, Daichi Yamaura, Shun Araki, Madoka Sato, Maki Komiya, Teng Ma, Hideaki Yamamoto, Michio Niwano, Ayumi Hirano-Iwata

Subjects: “…human <i>ether-a-go-go-</i>related gene (hERG) channel…”
Get full text

An LQT2-related mutation in the voltage-sensing domain is involved in switching the gating polarity of hERG by Zhipei Liu, Feng Wang, Hui Yuan, Fuyun Tian, Chuanyan Yang, Fei Hu, Yiyao Liu, Meiqin Tang, Meixuan Ping, Chunlan Kang, Ting Luo, Guimei Yang, Mei Hu, Zhaobing Gao, Ping Li

Subjects: “…hERG…”
Get full text