Results 11 to 20 of about 36,434 (294)

An Update on the Structure of hERG [PDF]

Frontiers in Pharmacology, 2020
The human voltage-sensitive K+ channel hERG plays a fundamental role in cardiac action potential repolarization, effectively controlling the QT interval of the electrocardiogram.
Andrew Butler, Matthew V. Helliwell, Yihong Zhang, Jules C. Hancox, Christopher E. Dempsey   +4 more
doaj   +6 more sources

CardioGenAI: a machine learning-based framework for re-engineering drugs for reduced hERG liability [PDF]

Journal of Cheminformatics
The link between in vitro hERG ion channel inhibition and subsequent in vivo QT interval prolongation, a critical risk factor for the development of arrythmias such as Torsade de Pointes, is so well established that in vitro hERG activity alone is often ...
Gregory W. Kyro, Matthew T. Martin, Eric D. Watt, Victor S. Batista   +3 more
doaj   +4 more sources

Structural modeling of the hERG potassium channel and associated drug interactions

Frontiers in Pharmacology, 2022
The voltage-gated potassium channel, KV11.1, encoded by the human Ether-à-go-go-Related Gene (hERG), is expressed in cardiac myocytes, where it is crucial for the membrane repolarization of the action potential.
Jan Maly, Jan Maly, Aiyana M. Emigh, Aiyana M. Emigh, Kevin R. DeMarco, Kevin R. DeMarco, Kazuharu Furutani, Jon T. Sack, Colleen E. Clancy, Colleen E. Clancy, Igor Vorobyov, Igor Vorobyov, Vladimir Yarov-Yarovoy   +12 more
doaj   +2 more sources

PIKfyve Sensitivity of hERG Channels [PDF]

Cellular Physiology and Biochemistry, 2013
Background/Aims: Human ether-a-go-go (hERG) channels contribute to cardiac repolarization and participate in the regulation of tumor cell proliferation.
Tatsiana Pakladok, Ahmad Almilaji, Carlos Munoz, Ioana Alesutan, Florian Lang   +4 more
doaj   +3 more sources

Mechanism of hERG inhibition by gating-modifier toxin, APETx1, deduced by functional characterization

BMC Molecular and Cell Biology, 2021
Background Human ether-à-go-go-related gene potassium channel 1 (hERG) is a voltage-gated potassium channel, the voltage-sensing domain (VSD) of which is targeted by a gating-modifier toxin, APETx1.
Kazuki Matsumura, Takushi Shimomura, Yoshihiro Kubo, Takayuki Oka, Naohiro Kobayashi, Shunsuke Imai, Naomi Yanase, Madoka Akimoto, Masahiro Fukuda, Mariko Yokogawa, Kazuyoshi Ikeda, Jun-ichi Kurita, Yoshifumi Nishimura, Ichio Shimada, Masanori Osawa   +14 more
doaj   +2 more sources

A Receptor-Independent Effect of Estrone Sulfate on the hERG Channel

Journal of Pharmacological Sciences, 2009
We recently reported that physiological concentrations of 17β-estradiol partially down-regulate cardiac rapidly-activating delayed rectifier K+ currents (hERG currents) independently of estrogen-receptor signaling.
Shoko Kakusaka, Mahoko Asayama, Asami Kaihara, Tetsuo Sasano, Takeshi Suzuki, Junko Kurokawa, Tetsushi Furukawa   +6 more
doaj   +3 more sources

Integrating drug effects on individual cardiac ionic currents and cardiac action potentials to understand nonclinical translation to clinical ECG changes [PDF]

Frontiers in Pharmacology
Concomitant inhibition of the late Na+ current (INaL) and/or the L-type Ca2+ current (ICaL) has been hypothesized to mitigate hERG block-mediated QTC prolongation.
Lars Johannesen, Najah Abi-Gerges, Katrina Sweat, Ana Roup, Guy Page, Claudia Alvarez Baron, Huimei Yu, Wendy W. Wu   +7 more
doaj   +2 more sources

Multi-laboratory comparisons of manual patch clamp hERG data generated using standardized protocols and following ICH S7B Q&A 2.1 best practices [PDF]

Scientific Reports
Acute block of hERG channels is the most common mechanism underlying drug-induced QTC prolongation and potentially fatal Torsade de Pointes arrhythmia. Updates to ICH E14 Q&As now allow for using negative nonclinical data, including hERG, to support QTC ...
Claudia Alvarez Baron, Jun Zhao, Huimei Yu, Ming Ren, Nicolas Thiebaud, Donglin Guo, Giri Vegesna, Cheng-Hui Hsiao, Ryan DePalma, Sabyasachy Mistry, Isra Tariq, Md Shadiqur Rashid Roni, Omnia A. Ismaiel, Murali K. Matta, Vikram Patel, Manni Mashaee, Jose Vicente, Lars Johannesen, Jiansong Sheng, Simon Hebeisen, James Kramer, Andrew Bruening-Wright, Koji Nakano, Hiroshi Matsukawa, Jennifer Beck Pierson, Wendy W. Wu   +25 more
doaj   +2 more sources

LncRNA MALAT1/Calpain-1 Axis in ATO Induced hERG Channel Deficiency [PDF]

Drug Design, Development and Therapy
Caichuan Yan,* Yuexin Li,* Xiaoxu Li, Yang Li, Yuhao Zhang, Jinyang Sun, Qirui Ding, Xin Zhao, Baoxin Li Department of Pharmacology, College of Pharmacy, Harbin Medical University, Harbin, People’s Republic of China*These authors contributed ...
Yan C, Li Y, Li X, Li Y, Zhang Y, Sun J, Ding Q, Zhao X, Li B   +8 more
doaj   +2 more sources

Construction of an integrated database for hERG blocking small molecules.

PLoS ONE, 2018
The inhibition of the hERG potassium channel is closely related to the prolonged QT interval, and thus assessing this risk could greatly facilitate the development of therapeutic compounds and the withdrawal of hazardous marketed drugs.
Tomohiro Sato, Hitomi Yuki, Keiji Ogura, Teruki Honma   +3 more
doaj   +2 more sources