Results 61 to 70 of about 33,807 (258)

NSAIDS AS MODULATORS OF CATION CHANNELS: FENAMATES REPURPOSING IN CHANNELOPATHIES

ChemMedChem, Accepted Article.
Cationic ion channels are transmembrane proteins that regulate the flux of cations (potassium, sodium, and calcium) across cell membrane, playing a pivotal role in many cellular functions. Disruptions of their activity can lead to the so‐called genetic or acquired channelopathies, a heterogeneous group of diseases that affect multiple human systems ...
Paola Laghetti, Concetta Altamura, Simone Dell’Atti, Jean-François Desaphy, Ilaria Saltarella   +4 more
wiley   +1 more source

Toward a Consensus Model of the hERG Potassium Channel [PDF]

ChemMedChem, 2010
AbstractMalfunction of hERG potassium channels, due to inherited mutations or inhibition by drugs, can cause long QT syndrome, which can lead to life‐threatening arrhythmias. A three‐dimensional structure of hERG is a prerequisite to understand the molecular basis of hERG malfunction.
Soren Wacker, Anna Stary, Anna Stary, Bert L. de Groot, Gert Vriend, Ulrich Zachariae, Johan Åqvist, Yasmin Karimi-Nejad, Lars Boukharta   +8 more
openaire   +7 more sources

Assessment of the Effects of Fruquintinib on Cardiac Safety in Patients with Metastatic Colorectal Cancer

The Journal of Clinical Pharmacology, EarlyView.
Abstract Fruquintinib is a highly selective oral inhibitor of vascular endothelial growth factor receptors 1, 2, and 3, approved by the US Food and Drug Administration and the European Commission for the treatment of previously treated metastatic colorectal cancer (mCRC), regardless of biomarker status. This study used concentration QT interval (C‐QTc)
Xiaofei Zhou, Alice Toms, Dave Morton, Xiaohui Wang, Adekemi Taylor, Arvind Dasari, Neeraj Gupta, Caly Chien   +7 more
wiley   +1 more source

Proton and Zinc Effects on HERG Currents [PDF]

Biophysical Journal, 1999
The proton and Zn2+ effects on the human ether-a-go-go related gene (HERG) channels were studied after expression in Xenopus oocytes and stable transfection in the mammalian L929 cell line. Experiments were carried out using the two-electrode voltage clamp at room temperature (oocytes) or the whole-cell patch clamp technique at 35 degrees C (L929 cells)
José Jalife, Mario Delmar, Justus M.B. Anumonwo, Steven M. Taffet, Jorge Horta   +4 more
openaire   +3 more sources

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

Salen‐Type Copper(II) Complexes: Synthesis, Characterization, Computational Studies, Molecular Docking, Anticancer Potential, and Pharmacokinetic Prediction

ChemistryOpen, EarlyView.
Integrating synthesis, density functional theory studies, molecular docking, cytotoxicity, and ADMET predictions, this study identifies [CuII(salen)(H2O)2] (2) as a selective anticancer agent. Docking and in vitro assays highlight its favorable target interactions, selective anticancer activity, and reduced toxicity toward normal fibroblasts ...
Abdellatif A. Helaly, Bandar A. Babgi, Yoji Kobayashi, Rohit K. Rai, Ehab M. M. Ali, Abdulaziz A. Kalantan, Walid M. I. Hassan, Mostafa A. Hussien, Muhammad M. I. Ismail   +8 more
wiley   +1 more source

In‐Silico Exploration of the StreptomeDB Database for Potential Irreversible DprE1 Inhibitors toward Antitubercular Treatment

ChemistryOpen, EarlyView.
StreptomeDB‐derived nitro compounds are screened against Mycobacterium tuberculosis decaprenylphosphoryl‐D‐riboseoxidase (DprE1) . Covalent docking, molecular dynamics simulations, and molecularmechanics/generalized Born surface area analyses identify hydroxythaxtomin and lajollamycin B as potent DprE1 inhibitors, surpassing the reference PBTZ169 in ...
Doaa G. M. Mahmoud, Gamal A. H. Mekhemer, Mohamed‐Elamir F. Hegazy, Jabir H. Al‐Fahemi, Mahmoud A. A. Ibrahim   +4 more
wiley   +1 more source

Potassium channel subunits encoded by the KCNE gene family: physiology and pathophysiology of the MinK-related peptides (MiRPs). [PDF]

, 2001
Voltage-gated potassium channels provide tightly Controlled, ion-specific pathways across membranes and are key to the normal function of nerves muscles. They arise from the assembly of four pore-forming proteins called alpha-subunits.
Abbott, GW, Goldstein, SA
core  

Spin Properties of Supermassive Black Holes with Powerful Outflows

, 2016
Relationships between beam power and accretion disk luminosity are studied for a sample of 55 HERG, 13 LERG, and 29 RLQ with powerful outflows. The ratio of beam power to disk luminosity tends to be high for LERG, low for RLQ, and spans the full range of
Daly, Ruth A.
core   +1 more source

Upregulation of Functional Kv11.1 Isoform Expression by Inhibition of Intronic Polyadenylation with Antisense Morpholino Oligonucleotides

, 2012
The KCNH2 gene encodes the Kv11.1 potassium channel that conducts the rapidly activating delayed rectifier current in the heart. KCNH2 pre-mRNA undergoes alternative processing; intron 9 splicing leads to the formation of a functional, full-length Kv11 ...
Gong, Qiuming, Stump, Matthew R., Zhou, Zhengfeng   +2 more
core   +2 more sources