Results 101 to 110 of about 17,722 (214)

Functional and pharmacological characterization of an S5 domain hERG mutation associated with short QT syndrome

Heliyon, 2019
Congenital short QT syndrome (SQTS) is a repolarization disorder characterized by abbreviated QT intervals, atrial and ventricular arrhythmias and a risk of sudden death. This study characterized a missense mutation (I560T) in the S5 domain of the hERG K+
Andrew Butler, Yihong Zhang, A. Graham Stuart, Christopher E. Dempsey, Jules C. Hancox   +4 more
doaj   +1 more source

Modulation of hERG K+ Channel Deactivation by Voltage Sensor Relaxation

Frontiers in Pharmacology, 2020
The hERG (human-ether-à-go-go-related gene) channel underlies the rapid delayed rectifier current, Ikr, in the heart, which is essential for normal cardiac electrical activity and rhythm.
Yu Patrick Shi, Samrat Thouta, Thomas W. Claydon   +2 more
doaj   +1 more source

A minK-HERG complex regulates the cardiac potassium current I(Kr). [PDF]

, 1997
MinK is a widely expressed protein of relative molecular mass approximately 15K that forms potassium channels by aggregation with other membrane proteins.
Fishman, GI, Goldstein, SA, McDonald, TV, Meyers, MB, Ming, Z, Palma, E, Wang, KW, Yu, Z   +7 more
core  

Synthesis, Characterization, and Biological Evaluation of Aliphatic‐Substituted Benzimidazole Derivatives: Induction of Apoptosis, Cell Cycle Arrest, and Molecular Docking in Breast Cancer Cells

Drug Development Research, Volume 87, Issue 2, April 2026.
ABSTRACT A new series of aliphatic‐substituted benzimidazole derivatives was synthesized and structurally characterized to evaluate their potential anticancer activity. Among the synthesized compounds, compound 4 exhibited the most potent cytotoxic effects against MCF‐7 and MDA‐MB‐231 breast cancer cell lines, with IC₅₀ values comparable to those of ...
Murat Keser, Çisil Çamlı Pulat, Harika Atmaca, Hakan Akgün, Canan Albay, Emre Menteşe, Hakan Bektaş, Suleyman Ilhan   +7 more
wiley   +1 more source

Peimine inhibits hERG potassium channels through the channel inactivation states

Biomedicine & Pharmacotherapy, 2017
Fritillaria is a Chinese traditional herb. It has a long history and many medicinal usages including antitussive, anti-inflammatory and pain relieving actions. It is also used as food. However, its cardiac safety has not been tested. Peimine is one of the main active compounds of Fritillaria.
Liandi, Kan, Wei, Zhao, Lanying, Pan, Jianwei, Xu, Qingmao, Chen, Kai, Xu, Liping, Xiao, Yuan, Chen   +7 more
openaire   +2 more sources

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

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   +1 more source

Validation of a [3H]Astemizole Binding Assay in HEK293 Cells Expressing HERG K+ Channels

Journal of Pharmacological Sciences, 2004
A radioligand binding assay for the HERG (human ether-a-go-go-related gene) K+ channel was developed to identify compounds which may have inhibitory activity and potential cardiotoxicity.
Peter J.S. Chiu, Karen F. Marcoe, Sidney E. Bounds, Chun-Hsiung Lin, Jin-Jye Feng, Atsui Lin, Fong-Chi Cheng, William J. Crumb, Richard Mitchell   +8 more
doaj   +1 more source

The light and shadow of senescence and inflammation in cardiovascular pathology and regenerative medicine [PDF]

, 2017
Recent epidemiologic studies evidence a dramatic increase of cardiovascular diseases, especially associated with the aging of the world population. During aging, the progressive impairment of the cardiovascular functions results from the compromised ...
Cavarretta, Elena, Dal Sasso, Eleonora, Forte, Maurizio, Frati, Giacomo, Gerosa, Gino, Iop, Laura, Palmerio, Silvia, Peruzzi, Mariangela, Schirone, Leonardo, Sciarretta, Sebastiano   +9 more
core   +4 more sources

Mechanism and pharmacological rescue of berberine-induced hERG channel deficiency

Drug Design, Development and Therapy, 2015
Meng Yan,1 Kaiping Zhang,1 Yanhui Shi,1 Lifang Feng,1 Lin Lv,1 Baoxin Li1,2 1Department of Pharmacology, Harbin Medical University, 2State-Province Key Laboratory of Biopharmaceutical Engineering, Harbin, Heilongjiang, People’s Republic of China ...
Yan M, Zhang KP, Shi YH, Feng LF, Lv L, Li BX   +5 more
doaj  

Phα1β interaction with the Kv11.1 potassium channel in HEK293 cells transfected with the human ERG channel [PDF]

Journal of Venomous Animals and Toxins including Tropical Diseases
Background: This study examines the impact of Phα1β, a spider peptide derived from the venom of Phoneutria nigriventer, on the Kv11.1 potassium channel in HEK293 cells transfected with the human ERG potassium channel.
João B. Calixto, Adara Aurea dos Santos, Juliano Ferreira, Alessandra Hubner Souza, Célio José de Castro Junior, Marcus Vinicius Gomez   +5 more
doaj   +1 more source