Results 181 to 190 of about 17,722 (214)

HERG channel trafficking.

Novartis Foundation symposium, 2005
Mutations in the cardiac potassium channel hERG/IKr cause inherited long QT syndrome with increased susceptibility to ventricular arrhythmias. Several mutations in hERG produce trafficking-deficient channels that are retained in the endoplasmic reticulum (ER). Surface expression of certain mutations (i.e. hERG G601S) can be restored by specific channel
Eckhard, Ficker, Adrienne, Dennis, Yuri, Kuryshev, Barbara A, Wible, Arthur M, Brown   +4 more
openaire   +1 more source

Effects of donepezil on hERG potassium channels

Brain Research, 2015
Donepezil is a potent, selective inhibitor of acetylcholinesterase, which is used for the treatment of Alzheimer's disease. Whole-cell patch-clamp technique and Western blot analyses were used to study the effects of donepezil on the human ether-a-go-go-related gene (hERG) channel.
Yun Ju, Chae, Hong Joon, Lee, Ji Hyun, Jeon, In-Beom, Kim, Jin-Sung, Choi, Ki-Wug, Sung, Sang June, Hahn   +6 more
openaire   +2 more sources

Aconitine blocks HERG and Kv1.5 potassium channels

Journal of Ethnopharmacology, 2010
Aconitum has been widely used to treat various diseases in China for a long time. However, improper use of this drug results in severe intoxication. Aconitine (ACO), a diterpenoid alkaloid from aconitum, mainly contributes to cardio-toxic effects of aconitum and has also been commonly known to induce arrhythmias in animal models.
Yifu, Li, Danna, Tu, Hua, Xiao, Yimei, Du, Anruo, Zou, Yuhua, Liao, Shaohong, Dong   +6 more
openaire   +2 more sources

Predictive models for hERG potassium channel blockers

Bioorganic & Medicinal Chemistry Letters, 2005
We report here a general method for the prediction of hERG potassium channel blockers using computational models generated from correlation analyses of a large dataset and pharmacophore-based GRIND descriptors. These 3D-QSAR models are compared favorably with other traditional and chemometric based HQSAR methods.
CIANCHETTA, GIOVANNI, Li Y., Kang J., Rampe D., FRAVOLINI, Arnaldo, CRUCIANI, Gabriele, Vaz R. J.   +6 more
openaire   +2 more sources

Current pharmacogenomic studies on hERG potassium channels

Trends in Molecular Medicine, 2013
Genetic polymorphisms in human ether-a-go-go-related gene (hERG) potassium channels are associated with many complex diseases and sensitivity to channel-related drugs. Genotypes may underlie different sensitivities to the same drug, and different drugs selectively repair the functional deficits caused by individual mutations.
Fa-Zhong, He, Howard L, McLeod, Wei, Zhang   +2 more
openaire   +2 more sources

An Automated Docking Protocol for hERG Channel Blockers

Journal of Chemical Information and Modeling, 2013
A docking protocol aimed at obtaining a consistent qualitative and quantitative picture of binding for a series of hERG channel blockers is presented. To overcome the limitations experienced by standard procedures when docking blockers at hERG binding site, we designed a strategy that explicitly takes into account the conformations of the channel ...
DI MARTINO, GIOVANNI PAOLO, MASETTI, MATTEO, CECCARINI, LUISA, CAVALLI, ANDREA, RECANATINI, MAURIZIO   +4 more
openaire   +3 more sources

hERG Channel Inhibitors in Extracts of Coptidis Rhizoma

Planta Medica, 2011
Inhibition of the hERG channel delays repolarization and prolongs the QT interval and cardiac action potential which can lead to sudden death. Several drugs have been withdrawn from the market due to hERG channel inhibition. In the search of hERG channel inhibitors of natural origin, we established an HPLC-based profiling approach which combines HPLC ...
Schramm, A., Baburin, I., Hering, S., Hamburger, M.   +3 more
openaire   +4 more sources

Ligand Structural Aspects of hERG Channel Blockade

Current Topics in Medicinal Chemistry, 2008
Sudden death as a side effect of action of non-antiarrhythmic drugs is a major pharmacological safety concern facing the pharmaceutical industry and the health regulatory authorities. A number of drugs have been withdrawn from the market in recent years due to cardiovascular toxicity associated with undesirable blockade of hERG potassium channel ...
openaire   +2 more sources

The hERG potassium channel and hERG screening for drug-induced torsades de pointes

Pharmacology & Therapeutics, 2008
Drug-induced torsades de pointes (TdP) arrhythmia is a major safety concern in the process of drug design and development. The incidence of TdP tends to be low, so early pre-clinical screens rely on surrogate markers of TdP to highlight potential problems with new drugs.
Hancox, JC, McPate, MJW, El Harchi, A, Zhang, YH   +3 more
openaire   +3 more sources

Modulation of HERG channel inactivation by external cations

European Biophysics Journal, 2003
We investigated the effect of external cations on the permeability characteristics and gating kinetics of the human ether- à- go- go-related gene (HERG) current using the whole-cell patch-clamp technique. Inward HERG currents were recorded on hyperpolarization in 140 mM external Cs(+) and Rb(+), as well as K(+). The permeability ratios of Rb(+) and Cs(+
Jae Boum, Youm, Yung E, Earm, Won-Kyung, Ho   +2 more
openaire   +2 more sources