Results 21 to 30 of about 17,722 (214)

Сardioprotective agents with biaromatic structure. Part 4. Potassium hERG channels blockers and modulators

Фармакокинетика и Фармакодинамика, 2023
The hERG subtype potassium channel (Kv11.1) is one of the most important and one of the most studied biological targets for the creation of cardioprotective agents.
G. V. Mokrov
doaj   +1 more source

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   +1 more source

Lead optimisation of dehydroemetine for repositioned use in malaria [PDF]

, 2020
Drug repositioning offers an effective alternative to de novo drug design to tackle the urgent need for novel anti-malarial treatments. The anti-amoebic compound, emetine dihydrochloride, has been identified as a potent in-vitro inhibitor of the multi ...
Abubaker, M, Bryce, RA, Burusco, KK, Fernández-Álvaro, E, Gutnov, A, Matthews, H, Nirmalan, NJ, Panwar, P, Wilkinson, JA   +8 more
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Design, synthesis and antibacterial activity of minor groove binders: the role of non-cationic tail groups [PDF]

, 2012
he design and synthesis of a new class of minor groove binder (MGBs) in which, the cationic tail group has been replaced by a neutral, polar variant including cyanoguanidine, nitroalkene, and trifluoroacetamide groups.
Bourdin, Claire, Breen, David, Clements, Carol, Donoghue, Gavin, Fox, Keith, Khalaf, Abedawn, MacMillan, Donna, Scott, Fraser, Sekibo, Doreen, Suckling, Colin   +9 more
core   +1 more source

Voltage-Dependent Gating of hERG Potassium Channels [PDF]

Frontiers in Pharmacology, 2012
The mechanisms by which voltage-gated channels sense changes in membrane voltage and energetically couple this with opening of the ion conducting pore has been the source of significant interest. In voltage-gated potassium (Kv) channels, much of our knowledge in this area comes from Shaker-type channels, for which voltage-dependent gating is quite ...
Cheng, Yen May, Claydon, Tom W.
openaire   +3 more sources

Chronic Administration of COVID-19 Drugs Fluvoxamine and Lopinavir Shortens Action Potential Duration by Inhibiting the Human Ether‐à‐go‐go–Related Gene and Cav1.2

Frontiers in Pharmacology, 2022
Background: Old drugs for new indications in the novel coronavirus disease of 2019 (COVID-19) pandemic have raised concerns regarding cardiotoxicity, especially the development of drug-induced QT prolongation.
Zequn Zheng, Zequn Zheng, Zequn Zheng, Dihui Cai, Dihui Cai, Yin Fu, Yin Fu, Ying Wang, Yongfei Song, Yongfei Song, Jiangfang Lian, Jiangfang Lian   +11 more
doaj   +1 more source

Molecular mechanisms underlying the pilsicainide-induced stabilization of hERG proteins in transfected mammalian cells

Journal of Arrhythmia, 2017
Background: Pilsicainide, classified as a relatively selective Na+ channel blocker, also has an inhibitory action on the rapidly-activating delayed-rectifier K+ current (IKr) through human ether-a-go-go-related gene (hERG) channels.
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   +17 more
doaj   +1 more source

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   +1 more source

The Effect of a Synthetic Estrogen, Ethinylestradiol, on the hERG Block by E-4031

Biomolecules, 2021
Inhibition of K+-conductance through the human ether-a-go-go related gene (hERG) channel leads to QT prolongation and is associated with cardiac arrhythmias.
Fumiya Tamura, Shintaro Sugimoto, Mana Sugimoto, Kazuho Sakamoto, Masahiko Yamaguchi, Takeshi Suzuki, Keiichi Fukuda, Masaki Ieda, Junko Kurokawa   +8 more
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Comprehensive translational assessment of human-induced pluripotent stem cell derived cardiomyocytes for evaluating drug-induced arrhythmias [PDF]

, 2016
Induced pluripotent stem cell-derived cardiomyocytes (iPSC-CM) hold promise for assessment of drug-induced arrhythmias and are being considered for use under the comprehensive in vitro proarrhythmia assay (CiPA).
Blinova, Ksenia, Brock, Mathew, Chan, Dulciana, Chvatal, Stacie, Crumb, William J., Galeotti, Loriano, Hortigon-Vinagre, Maria P., Johannesen, Lars, Lyn-Cook, Beverly, Millard, Daniel, Pang, Li, Ross, James, Smith, Godfrey, Stockbridge, Norman, Stohlman, Jayna, Strauss, David G., Vicente, Jose, Zamora Rodriguez, Victor   +17 more
core   +1 more source