Results 11 to 20 of about 1,218,415 (224)

Structural modeling of hERG channel–drug interactions using Rosetta [PDF]

Frontiers in Pharmacology, 2023
The human ether-a-go-go-related gene (hERG) not only encodes a potassium-selective voltage-gated ion channel essential for normal electrical activity in the heart but is also a major drug anti-target.
Aiyana M. Emigh Cortez, Aiyana M. Emigh Cortez, Kevin R. DeMarco, Kevin R. DeMarco, Kazuharu Furutani, Kazuharu Furutani, Slava Bekker, Slava Bekker, Jon T. Sack, Jon T. Sack, Heike Wulff, Colleen E. Clancy, Colleen E. Clancy, Colleen E. Clancy, Igor Vorobyov, Igor Vorobyov, Vladimir Yarov-Yarovoy, Vladimir Yarov-Yarovoy   +17 more
doaj   +4 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   +4 more sources

Stimulation of HERG channel activity by β-catenin. [PDF]

PLoS ONE, 2012
The multifunctional protein ß-catenin governs as transcription factor the expression of a wide variety of genes relevant for cell proliferation and cell survival.
Carlos Munoz, Ambrish Saxena, Tatsiana Pakladok, Evgenii Bogatikov, Jan Wilmes, Guiscard Seebohm, Michael Föller, Florian Lang   +7 more
doaj   +6 more sources

hERG potassium channel inhibition by ivabradine requires channel gating [PDF]

Journal of Molecular and Cellular Cardiology, 2015
The file associated with this record is under a 12-month embargo from publication in accordance with the publisher's self-archiving policy, available at http://www.elsevier.com/about/company-information/policies/sharing. The full text may be available in the publisher links provided above.
Melgari, Dario, Brack, Kieran E, Zhang, Yihong, El Harchi, Aziza, Mitcheson, John S, Dempsey, Christopher E, Ng, G André, Hancox, Jules C   +7 more
core   +10 more sources

Molecular Insights Into the Gating Kinetics of the Cardiac hERG Channel, Illuminated by Structure and Molecular Dynamics [PDF]

Frontiers in Pharmacology, 2021
The rapidly activating delayed rectifier K+ current generated by the cardiac hERG potassium channel encoded by KCNH2 is the most important reserve current for cardiac repolarization.
Zheng Zequn, Lian Jiangfang
doaj   +2 more sources

Klotho sensitivity of the hERG channel [PDF]

FEBS Letters, 2013
Klotho, a hormone and enzyme, is a powerful regulator of ageing and life span. Klotho deficiency leads to cardiac arrythmia and sudden cardiac death. We thus explored whether klotho modifies cardiac K+‐channel hERG. Current was determined utilizing dual electrode voltage clamp and hERG protein abundance utilizing immunohistochemistry and ...
Munoz, Carlos, Pakladok, Tatsiana, Almilaji, Ahmad, Elvira, Bernat, Seebohm, Guiscard, Voelkl, Jakob, Föller, Michael, Shumilina, Ekaterina, Lang, Florian   +8 more
openaire   +4 more sources

High Glucose Represses hERG K+ Channel Expression through Trafficking Inhibition

Cellular Physiology and Biochemistry, 2015
Background/Aims: Abnormal QT prolongation is the most prominent cardiac electrical disturbance in patients with diabetes mellitus (DM). It is well known that the human ether-ago-go-related gene (hERG) controls the rapid delayed rectifier K+ current (IKr)
Yuan-Qi Shi, Meng Yan, Li-Rong Liu, Xiao Zhang, Xue Wang, Huai-Ze Geng, Xin Zhao, Bao-Xin Li   +7 more
doaj   +2 more sources

Berberine Induces hERG Channel Deficiency through Trafficking Inhibition

Cellular Physiology and Biochemistry, 2014
Aims: The human ether-a-go-go-related gene (hERG) encodes the α subunit of the IKr, which plays an essential role in repolarization of action potentials. hERG channels are targeted by various pro-arrhythmic drugs.
Kaiping Zhang, Duo Zhi, Ting Huang, Yan Gong, Meng Yan, Chen Liu, Ting Wei, Zengxiang Dong, Baoxin Li, Baofeng Yang   +9 more
doaj   +2 more sources

AttenhERG: a reliable and interpretable graph neural network framework for predicting hERG channel blockers [PDF]

Journal of Cheminformatics
Cardiotoxicity, particularly drug-induced arrhythmias, poses a significant challenge in drug development, highlighting the importance of early-stage prediction of human ether-a-go-go-related gene (hERG) toxicity.
Tianbiao Yang, Xiaoyu Ding, Elizabeth McMichael, Frank W. Pun, Alex Aliper, Feng Ren, Alex Zhavoronkov, Xiao Ding   +7 more
doaj   +2 more sources

Natural products modulating the hERG channel: heartaches and hope

Natural Product Reports, 2017
This review covers natural products modulating the hERG potassium channel. Risk assessment strategies, structural features of blockers, and the duality target/antitarget are discussed.
Jadel M. Kratz, Ulrike Grienke, Olaf Scheel, Stefan A. Mann, Judith M. Rollinger   +4 more
openaire   +6 more sources