Results 121 to 130 of about 208,986 (273)

Machine Learning‐Driven Discovery of Structurally Related Natural Products as Activators of the Cardiac Calcium Pump SERCA2a

open access: yesChemMedChem, EarlyView.
Heart failure involves reduced SERCA2a activity, crucial for calcium regulation in heart cells. This study reports machine learning screening of 57,423 natural products, identifying several structurally related SERCA2a activators. Three compounds enhance calcium transport in cardiac cells, despite off‐target effects, offering promising hits for ...
Carlos Cruz‐Cortés   +7 more
wiley   +1 more source

Leveraging Visibility Graphs for Enhanced Arrhythmia Classification with Graph Convolutional Networks [PDF]

open access: yesarXiv
Arrhythmias, detectable through electrocardiograms (ECGs), pose significant health risks, underscoring the need for accurate and efficient automated detection techniques. While recent advancements in graph-based methods have demonstrated potential to enhance arrhythmia classification, the challenge lies in effectively representing ECG signals as graphs.
arxiv  

Further SAR of GIRK1/2 activators: Synthesis and Biological Characterization of In Vitro Tool Compounds

open access: yesChemMedChem, Accepted Article.
The work presented herein outlines the ongoing structure‐activity relationship (SAR) studies centered around a potent, efficacious, and selective activators of the GIRK1/2 channel. Optimization studies centered around the pyrazole privileged scaffold, the N‐1‐position of the pyrazole and the right‐hand ether.
Sumaiya Nahid   +8 more
wiley   +1 more source

A Phase 1 Randomized Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single Escalating Oral Doses of Dordaviprone and the Effects of Food on the Bioavailability of Dordaviprone in Healthy Adult Subjects

open access: yesClinical Pharmacology in Drug Development, EarlyView.
Abstract Dordaviprone (ONC201) is a novel, small molecule imipridone with antitumor effects in glioma patients. This study evaluated the pharmacokinetics and safety of dordaviprone following single escalating doses (Part A), as a capsule content mixed with applesauce or Gatorade (sports drink) [Part B1]), and with or without food [Part B2].
Shamia L. Faison   +7 more
wiley   +1 more source

QTc Interval Changes in Preeclampsia vs. Normal Pregnancy: A Systematic Review and Meta‐Analysis

open access: yesClinical Pharmacology &Therapeutics, EarlyView.
Pregnancy induces significant adaptations in the cardio‐autonomic nervous system, with additional cardiac stress in preeclampsia potentially impacting ventricular repolarization. Despite the widespread use of QT‐prolonging drugs during pregnancy, the extent of heart rate (HR)‐corrected QT (QTc) interval changes during normal pregnancy and preeclampsia ...
Omar A. Aboshady   +4 more
wiley   +1 more source

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