Results 21 to 30 of about 31,297 (199)

Calculations of the binding free energies of the Comprehensive in vitro Proarrhythmia Assay (CiPA) reference drugs to cardiac ion channels

Biophysics and Physicobiology, 2023
The evaluation of the inhibitory activities of drugs on multiple cardiac ion channels is required for the accurate assessment of proarrhythmic risks.
Tatsuki Negami, Tohru Terada
doaj   +1 more source

The triggering probability of radio-loud AGN: A comparison of high and low excitation radio galaxies in hosts of different colors [PDF]

, 2012
Low luminosity radio-loud active galactic nuclei (AGN) are generally found in massive red elliptical galaxies, where they are thought to be powered through gas accretion from their surrounding hot halos in a radiatively inefficient manner.
Abazajian, Baldwin, Balogh, Becker, Best, Best, Best, Best, Brinchmann, Condon, Croton, Evans, H. J. A. Röttgering, Hardcastle, Hickox, J. Brinchmann, Kauffmann, Kauffmann, Kauffmann, Martin, Matthews, P. N. Best, R. M. J. Janssen, Schmidt, Stoughton, Strateva, Strauss, Tadhunter, Tasse, Whysong, York   +30 more
core   +3 more sources

Action potential clamp and pharmacology of the variant 1 Short QT Syndrome T618I hERG K⁺ channel.

PLoS ONE, 2012
BackgroundThe familial Short QT Syndrome (SQTS) is associated with an increased risk of cardiac arrhythmia and sudden death. Gain-of-function mutations in the hERG K(+) channel protein have been linked to variant 1 of the SQTS. A hERG channel pore (T618I)
Aziza El Harchi, Dario Melgari, Yi Hong Zhang, Henggui Zhang, Jules C Hancox   +4 more
doaj   +1 more source

Pharmacologic Approach to Defective Protein Trafficking in the E637K-hERG Mutant with PD-118057 and Thapsigargin. [PDF]

PLoS ONE, 2013
Treatment of LQT2 is inadequate. Many drugs which can pharmacologically rescue defective protein trafficking in LQT2 also result in potent blockade of HERG current, negating their therapeutic benefit.
Haiyan Mao, Xiaoli Lu, Justin Michael Karush, Xiaoyan Huang, Xi Yang, Yanna Ba, Ying Wang, Ningsheng Liu, Jianqing Zhou, Jiangfang Lian   +9 more
doaj   +1 more source

Trafficking-deficient G572R-hERG and E637K-hERG activate stress and clearance pathways in endoplasmic reticulum. [PDF]

PLoS ONE, 2012
Long QT syndrome type 2 (LQT2) is the second most common type of all long QT syndromes. It is well-known that trafficking deficient mutant human ether-a-go-go-related gene (hERG) proteins are often involved in LQT2.
Ying Wang, Xiaoyan Huang, Jianqing Zhou, Xi Yang, Di Li, Haiyan Mao, Huan Huan Sun, Ningsheng Liu, Jiangfang Lian   +8 more
doaj   +1 more source

The role of Eag and HERG channels in cell proliferation and apoptotic cell death in SK-OV-3 ovarian cancer cell line. [PDF]

, 2011
The voltage gated potassium (K+) channels Eag and HERG have been implicated in the pathogenesis of various cancers, through association with cell cycle changes and programmed cell death.
Anish Bali, Asher, Viren, Averil Warren, Heidi Sowter, Raheela Khan, Robert Shaw, Viren Asher   +6 more
core   +5 more sources

hERG Blockade Prediction by Combining Site Identification by Ligand Competitive Saturation and Physicochemical Properties

Chemistry, 2022
The human ether-a-go-go-related gene (hERG) potassium channel is a well-known contributor to drug-induced cardiotoxicity and therefore is an extremely important target when performing safety assessments of drug candidates.
Himanshu Goel, Wenbo Yu, Alexander D. MacKerell   +2 more
doaj   +1 more source

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

In Vitro and In Silico Risk Assessment in Acquired Long QT Syndrome: The Devil Is in the Details

Frontiers in Physiology, 2017
Acquired long QT syndrome, mostly as a result of drug block of the Kv11. 1 potassium channel in the heart, is characterized by delayed cardiac myocyte repolarization, prolongation of the T interval on the ECG, syncope and sudden cardiac death due to the ...
William Lee, William Lee, Monique J. Windley, Monique J. Windley, Jamie I. Vandenberg, Jamie I. Vandenberg, Adam P. Hill, Adam P. Hill   +7 more
doaj   +1 more source

Characterization of the novel mutant A78T-HERG from a long QT syndrome type 2 patient: Instability of the mutant protein and stabilization by heat shock factor 1

Journal of Arrhythmia, 2016
Background: The human ether-a-go-go-related gene (HERG) encodes the α-subunit of rapidly activating delayed-rectifier potassium channels. Mutations in this gene cause long QT syndrome type 2 (LQT2).
Takehito Kondo, Ichiro Hisatome, Shouichi Yoshimura, Endang Mahati, Tomomi Notsu, Peili Li, Kazuhiko Iitsuka, Masaru Kato, Kazuyoshi Ogura, Junichiro Miake, Takeshi Aiba, Wataru Shimizu, Yasutaka Kurata, Shinji Sakata, Naoe Nakasone, Haruaki Ninomiya, Akira Nakai, Katsumi Higaki, Yasushi Kawata, Yasuaki Shirayoshi, Akio Yoshida, Kazuhiro Yamamoto   +21 more
doaj   +1 more source