Results 101 to 110 of about 36,434 (294)
Clinical Pharmacology in Drug Development, EarlyView.Abstract The oral, small molecule inhibitor of activin receptor‐like kinase‐2, zilurgisertib (INCB000928), is under evaluation in fibrodysplasia ossificans progressiva. Cardiac safety was assessed using electrocardiogram (ECG) parameters and a plasma concentration‐heart rate‐corrected QT (C‐QTc) interval analysis of pooled data from single ascending ...
Yan‐ou Yang +5 more
wiley +1 more source
Hypoxia induced hERG trafficking defect linked to cell cycle arrest in SH-SY5Y cells.
PLoS ONE, 2019 The alpha subunit of the voltage gated human ether-a-go-go-related (hERG) potassium channel regulates cell excitability in a broad range of cell lines.
Damodara Reddy Vaddi +5 more
doaj +1 more source
Spirocyclic Diamine Scaffolds for Medicinal Chemistry
Helvetica Chimica Acta, EarlyView.Here we enumerated 391 spirocyclic diamine drug scaffolds with ring sizes four to eight and found that most of them are unknown. We prepared four novel such spirocycles and discovered a micromolar inhibitor of the M4 muscarinic receptor. ABSTRACT Medicinal chemistry requires the exploration of structurally diverse compound families to expand the ...
Aline Carrel +3 more
wiley +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
Scientific Reports, 2019 Assessing the hERG liability in the early stages of drug discovery programs is important. The recent increase of hERG-related information in public databases enabled various successful applications of machine learning techniques to predict hERG ...
Keiji Ogura +3 more
semanticscholar +1 more source
Interdisciplinary Medicine, EarlyView.TargetGen‐recurrent neural network (RNN), an advanced generative model, generated 28,708 unique and novel compounds, identifying SAK‐2970 as a potent antibiotic against drug‐resistant Staphylococcus aureus. Exhibiting strong biofilm inhibition, high therapeutic efficacy, and minimal systemic toxicity in vivo, SAK‐2970 highlights its safety and clinical
Shakeel Ahmad Khan +2 more
wiley +1 more source
Effects of an hERG Activator, ICA-105574, on Electrophysiological Properties of Canine Hearts
Journal of Pharmacological Sciences, 2013 In short QT syndrome, inherited gain-of-function mutations in the human ether a-go-go-related gene (hERG) K+ channel have been associated with development of fatal arrhythmias. This implies that drugs that activate hERG as a side effect may likewise pose
Mahoko Asayama +8 more
doaj +1 more source
ChemistryOpen, EarlyView.This study employed density functional theory (DFT) and conceptual DFT (CDFT) to calculate the structures and properties of potential antibacterial compounds derived from 16‐membered lactone ring‐containing secondary metabolites of extremophiles, as well as midecamycin.
Dilong Li +6 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 +4 more
doaj +1 more source
Analysis and prediction of injury severity in single micromobility crashes with Random Forest
Heliyon, 2023 Urban micromobility represents a significant shift towards sustainable cities, underscoring the paramount importance of its safety. With the surge in micromobility adoption, collisions involving micromobility devices, such as bicycles and e-scooters ...
Almudena Sanjurjo-de-No +2 more
doaj +1 more source