Results 81 to 90 of about 5,479 (195)

Selective excitatory effects of γ‐glutamyl‐glycine, a glutathione metabolite, on GluN1 NMDA and mGlu5 receptors impacting synaptic plasticity

British Journal of Pharmacology, EarlyView.
Background and Purpose Gamma‐glutamyl dipeptides are essentially produced after glutathione (GSH) degradation. While several γ‐glutamyl dipeptides have been detected in different organs and body fluids, their biological activity remains elusive. This is the case for γ‐Glutamyl‐Glycine (γ‐Glu‐Gly) which has been found in different brain areas.
Sandro Andreu, Victoria Gizzi, Ugo Pasco, Fatiha Sebih, Yattou Zitouni, Pablo Jimenez, Valérie Rolland, Alain Chavanieu, Sébastien Estaran, Matthieu Rousset, Thierry Cens, Guillaume Cazals, Pierre Charnet, Janique Guiramand, Catherine Cohen‐Solal, Claudine Ménard, Marie‐Céleste de Jésus Ferreira, Nathalie Chevallier, Sonia Cantel, Michel Vignes, Julien Roussel   +20 more
wiley   +1 more source

Methyl 4‐O‐Demethylbarbatate Destabilises HIF‐1α and Enhances Temozolomide Sensitivity in Glioma Cells

Cell Proliferation, EarlyView.
The lichen‐derived metabolite methyl 4‐O‐demethylbarbatate (Me‐4‐O‐DBA) suppresses glioma stemness, motility, and metabolic plasticity through inhibition of HIF‐1α signaling and synergistically enhances temozolomide activity, highlighting a potential strategy to target stemness‐driven therapeutic resistance in glioma.
Rui Zhou, Mücahit Varlı, Rundong Liu, Jieun Yu, Hyung‐Ho Ha, Jae‐Seoun Hur, Sang Kyum Kim, Hahyun Park, Hangun Kim   +8 more
wiley   +1 more source

Experimentally Validated Pharmacoinformatics Approach to Predict hERG Inhibition Potential of New Chemical Entities

Frontiers in Pharmacology, 2018
The hERG (human ether-a-go-go-related gene) encoded potassium ion (K+) channel plays a major role in cardiac repolarization. Drug-induced blockade of hERG has been a major cause of potentially lethal ventricular tachycardia termed Torsades de Pointes ...
Saba Munawar, Saba Munawar, Monique J. Windley, Edwin G. Tse, Matthew H. Todd, Adam P. Hill, Jamie I. Vandenberg, Ishrat Jabeen   +7 more
doaj   +1 more source

Safety, Tolerability, Pharmacokinetics and Exploratory Pharmacodynamics of Melanin‐Concentrating Hormone Receptor‐1 Antagonist RGH‐706 in Healthy and Overweight or Obese Men

Diabetes, Obesity and Metabolism, EarlyView.
ABSTRACT Aim This Phase 1 program evaluated the safety, tolerability, pharmacokinetics and exploratory pharmacodynamics of the novel melanin‐concentrating hormone receptor‐1 antagonist RGH‐706. Methods Study A was a first‐in‐man, randomized trial comprising a double‐blind, placebo‐controlled single‐ascending‐dose part (0.1–162.5 mg) and a two‐way ...
Thomas Brevig, Borbála Szepes, Zsófia Borbála Dombi, Gabriella Magyar, Zoltán Juhász, Margit Kapás, Éva Cseh, Zsuzsa Hegedűs, Tibor Farkas, Zsuzsanna Kiss, Balázs Szatmári   +10 more
wiley   +1 more source

Interaktionen am hERG-Kanal [PDF]

, 2010
Die schnelle Komponente des verzögerten, einwärtsgleichrichtenden K+-Stromes der Herzzelle (rapid delayed rectifier, IKr), die durch hERG (human ether-à-go-go-related gene) kodiert wird, ist für die Repolarisation des kardialen Aktionspotentials ...
Friemel, Anne
core  

Caenorhabditis elegans as an in vivo model system for human inherited primary arrhythmia syndromes

The Journal of Physiology, EarlyView.
Abstract figure legend Most genes involved in inherited primary arrhythmia syndromes (IPAS) are conserved in Caenorhabditis elegans, where genetic manipulation enables functional characterization of variants, identification of regulatory proteins, and in vivo drug testing.
Antoine Delinière, Thomas Boulin, Maëlle Jospin, Alexandre Janin, Gilles Millat, Philippe Chevalier, Olga Andrini   +6 more
wiley   +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

Electrophysiological, biochemical and immuncytochemical characterization of C-terminal HERG (LQT2) mutations [PDF]

, 2008
In fünf nicht verwandten Familien wurden unterschiedliche Mutationen gefunden, welche alle im C-Terminus von HERG lokalisiert waren und deren Träger insbesondere unter emotional oder durch Stress ausgelösten kardialen Attacken litten.
Choe, Chi-un
core  

Voltage‐gated potassium channels mediate thyroid hormone control of skeletal muscle excitability

The Journal of Physiology, EarlyView.
Abstract figure legend Thyroid hormone (TH)‐dependent remodelling of potassium (K+) channel networks regulates skeletal muscle (SkM) excitability. Triiodothyronine (T3), locally generated from thyroxine (T4) by type 2 deiodinase (D2), binds thyroid hormone receptors (TRα/β) and modulates transcription via thyroid response elements (TREs).
Annarita Nappi, Caterina Miro, Annunziata Gaetana Cicatiello, Ilaria Piccialli, Serena Sagliocchi, Lucia Acampora, Federica Restolfer, Rosa Sirica, Melania Murolo, Emery Di Cicco, Daniela Terracciano, Anna Pannaccione, Monica Dentice   +12 more
wiley   +1 more source

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