Results 71 to 80 of about 28,801 (226)

The Magnetic Field and Polarization Properties of Radio Galaxies in Different Accretion States

, 2015
We use the integrated polarized radio emission at 1.4 GHz ($\Pi_{\rm 1.4\,GHz}$) from a large sample of AGN (796 sources at redshifts ...
Banfield, J. K., Farnes, J. S., Gaensler, B. M., Lara-López, M. A., O'Sullivan, Shane P., van Velzen, S.   +5 more
core   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Global analysis reveals families of chemical motifs enriched for HERG inhibitors.

PLoS ONE, 2015
Promiscuous inhibition of the human ether-à-go-go-related gene (hERG) potassium channel by drugs poses a major risk for life threatening arrhythmia and costly drug withdrawals.
Fang Du, Joseph J Babcock, Haibo Yu, Beiyan Zou, Min Li   +4 more
doaj   +1 more source

Eag Domains Regulate LQT Mutant hERG Channels in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes. [PDF]

PLoS ONE, 2015
Human Ether á go-go Related Gene potassium channels form the rapid component of the delayed-rectifier (IKr) current in the heart. The N-terminal 'eag' domain, which is composed of a Per-Arnt-Sim (PAS) domain and a short PAS-cap region, is a critical ...
Qiang-Ni Liu, Matthew C Trudeau
doaj   +1 more source

Computational prediction of hERG blockers using homology modelling, molecular docking and QuaSAR studies

Results in Chemistry, 2021
A full-length three-dimensional structure of the tetrameric potassium ion channel (hERG Kv11.1) including the N- and C-terminal domains was built, with a diameter of 6 Å and 12 Å between the K + selectivity filter and the pore cavity residue Tyr652 of ...
Nataraj Sekhar Pagadala
doaj   +1 more source

Diabetes mellitus attenuates the repolarization reserve in mammalian heart [PDF]

, 2007
Objective: In diabetes mellitus several cardiac electrophysiological parameters are known to be affected. In rodent experimental diabetes models changes in these parameters were reported, but no such data are available in other mammalian species ...
Biliczki, Péter, Bíró, Tamás, Jost, Norbert, Kecskeméti, Valéria, Kocsis, Erzsébet, Lengyel, Csaba Attila, Magyar, János, Nánási, Péter Pál, Papp, Julius Gyula, Skoumal, Réka, Tóth, Miklós, Varró, András, Virág, László   +12 more
core   +1 more source

A novel selective stabilizer of the ryanodine receptor 2 prevents stress‐induced ventricular arrhythmias without impairing cardiac function

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Aberrant activation of type 2 ryanodine receptors (RyR2) causes lethal arrhythmias, such as catecholaminergic polymorphic ventricular tachycardia (CPVT). Developing drugs that suppress RyR2 hyperactivation may be key to novel arrhythmia treatments.
Nagomi Kurebayashi, Masami Kodama, Hana Inoue, Masato Konishi, Masami Sugihara, Takashi Murayama, Ryosuke Ishida, Koichiro Ishii, Shuichi Mori, Yukari Endo, Xi Zeng, Yukiko U. Inoue, Takayoshi Inoue, Satoru Noguchi, Hajime Nishio, Eri Nakashima, Norio Suzuki, Noriko Nakaya, Ryushi Sato, Yuya Otori, Ayuna Tsutsumi, Mirei Takahashi, Takayuki Oka, Haruo Ogawa, Kayoko Kanamitsu, Hiroyuki Kusuhara, Utako Yokoyama, Junko Kurokawa, Hiroyuki Kagechika, Takashi Sakurai   +29 more
wiley   +1 more source

Effects of Tannic Acid, Green Tea and Red Wine on hERG Channels Expressed in HEK293 Cells. [PDF]

PLoS ONE, 2015
Tannic acid presents in varying concentrations in plant foods, and in relatively high concentrations in green teas and red wines. Human ether-à-go-go-related gene (hERG) channels expressed in multiple tissues (e.g.
Xi Chu, Yusong Guo, Bingyuan Xu, Wenya Li, Yue Lin, Xiaorun Sun, Chunhua Ding, Xuan Zhang   +7 more
doaj   +1 more source

Drugs that act on both G protein‐coupled receptors (GPCRs) and kinases: potentiation of effects, side effects and general aspects of drug pleiotropy

British Journal of Pharmacology, EarlyView.
Abstract Background A drug designed for a specific target often interacts with multiple targets, either unintentionally or as part of its intended mechanism of action. This has been called pharmacological pleiotropy or polypharmacology. There are key endogenous ligands such as ATP, GABA and glutamate that act on various proteins in humans. Furthermore,
Hampus Ljunggren, Aleksandr Sokolov, Flavio Ballante, Robert Fredriksson, Francisco Lagunas‐Rangel, Alexander S. Hauser, Stefan Knapp, Jörgen Jonsson, Helgi B. Schiöth   +8 more
wiley   +1 more source

HERG Protein Plays a Role in Moxifloxacin-Induced Hypoglycemia

Journal of Diabetes Research, 2016
The purpose of this study was to investigate the effect of moxifloxacin on HERG channel protein and glucose metabolism. HERG expression was investigated using immunohistochemistry.
Hai-Yan Qiu, Sha-Sha Yuan, Fang-Yuan Yang, Ting-Ting Shi, Jin-Kui Yang   +4 more
doaj   +1 more source