Results 1 to 10 of about 31,297 (199)

PIKfyve Sensitivity of hERG Channels

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   +1 more source

NBD-Based Environment-Sensitive Fluorescent Probes for the Human Ether-a-Go-Go–Related Gene Potassium Channel

Frontiers in Molecular Biosciences, 2021
Three environment-sensitive probes were developed for the hERG channel based on the nitrobenzoxadiazole fluorophore herein. After careful evaluation, probes M1 and M3 were found to have a high affinity for imaging the hERG channel in the cell-based ...
Qi Li, Lijuan Chai, Gaopan Dong, Xiaomeng Zhang, Lupei Du   +4 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

HPLC-based activity profiling for pharmacologically and toxicologically relevant natural products – principles and recent examples

Pharmaceutical Biology, 2019
Context: Discovery of pharmacologically active natural products as starting points for drug development remains important and, for reasons of consumer safety, the identification of toxicologically relevant compounds in herbal drugs. Objective: To explain,
Matthias Hamburger
doaj   +1 more source

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he design and synthesis of a new class of minor groove binder (MGBs) in which, the cationic tail group has been replaced by a neutral, polar variant including cyanoguanidine, nitroalkene, and trifluoroacetamide groups.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

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

An Update on the Structure of hERG

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   +1 more source

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   +1 more source

Gain of function mutants: Ion channels and G protein-coupled receptors [PDF]

, 2000
Many ion channels and receptors display striking phenotypes for gain-of-function mutations but milder phenotypes for null mutations. Gain of molecular function can have several mechanistic bases: selectivity changes, gating changes including constitutive
Karschin, Andreas, Lester, Henry A.
core   +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