Results 91 to 100 of about 1,218,415 (224)

Modulation of hERG K+ Channel Deactivation by Voltage Sensor Relaxation

Frontiers in Pharmacology, 2020
The hERG (human-ether-à-go-go-related gene) channel underlies the rapid delayed rectifier current, Ikr, in the heart, which is essential for normal cardiac electrical activity and rhythm.
Yu Patrick Shi, Samrat Thouta, Thomas W. Claydon   +2 more
doaj   +1 more source

Pediatric Developmental Safety Assessment and New Approach Methodologies: US FDA/Triangle CERSI Workshop Report

Clinical Pharmacology &Therapeutics, Volume 120, Issue 5, Page 1240-1249, November 2026.
Pediatric developmental safety assessment presents distinct challenges in drug development. Children undergo dynamic changes in organ systems and drug disposition pathways during development, and drug‐related effects may be delayed or manifested differently than in adults.
Gilbert J. Burckart, Gelareh Abulwerdi, Christin L. Daniels, Calib Choi, Rebecca Racz, Jean‐Pierre Valentin, Kristin Ardlie, Nicholas Tatonetti, Susan Laffan, Marjory Moreau, Will Redfern, Lang Li, James J. Hickman, Rajanikanth Madabushi, Bhagwat Prasad, Lynne Yao, Paul B. Watkins   +16 more
wiley   +1 more source

Ion Conduction through the hERG Potassium Channel

PLoS ONE, 2012
The inward rectifier voltage-gated potassium channel hERG is of primary importance for the regulation of the membrane potential of cardiomyocytes. Unlike most voltage-gated K(+)-channels, hERG shows a low elementary conductance at physiological voltage and potassium concentration.
Ceccarini L., MASETTI, MATTEO, CAVALLI, ANDREA, RECANATINI, MAURIZIO   +3 more
openaire   +5 more sources

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

Plasmepsins as Antimalarial Drug Targets—Then, Now, and the Future

Medicinal Research Reviews, Volume 46, Issue 6, Page 1574-1602, November 2026.
ABSTRACT Malaria is a devastating disease caused by Plasmodium parasites. Plasmodium parasites express ten cathepsin D‐like aspartyl proteases, called plasmepsins (PMs). These PMs have diverse roles fulfill diverse functions throughout the parasite's lifecycle, though several exhibit functional redundancies. Among them, PMV, PMIV, and PMX are essential
Brad E. Sleebs
wiley   +1 more source

Redefining CHI3L1: Therapeutic Opportunities at the Crossroads of Immune Suppression and Disease Progression

Medicinal Research Reviews, Volume 46, Issue 6, Page 1897-1921, November 2026.
ABSTRACT Chitinase‐3‐like‐1 (CHI3L1, also known as YKL‐40) has been recognized as a biomarker of inflammation and tissue remodeling and has now emerged as a pseudoenzymatic immune checkpoint. Recent structural, immunological, and translational studies redefine it as an active regulator of immune suppression rather than a passive disease marker. Despite
Kirti Upmanyu, Saurabh Upadhyay, Moustafa T. Gabr   +2 more
wiley   +1 more source

Combating Campylobacter Resistance in Moroccan Poultry Using Essential Oil–Ciprofloxacin Combination

Veterinary Medicine and Science, Volume 12, Issue 6, November 2026.
With an estimated prevalence of 15.52% in Moroccan poultry, Campylobacter species pose a significant food safety concern. We investigated whether essential oils (EOs) could restore the efficacy of ciprofloxacin against multidrug‐resistant (MDR) strains.
Zineb Soubai, Nadia Ziyate, Rim Rais, Hamza Elhrech, Oumayma Aguerd, Abdelhakim Bouyahya, Taoufiq Benali, Mohamed Akhazzane, Hiba Mahir, Siham Fellahi, Waleed Al Abdulmonem, Imane El Houssni, Benaissa Attarassi, Nabila Auajjar   +13 more
wiley   +1 more source

Diethylene Glycol‐Linked Ring‐Fused Bis‐Azoles: Target‐Oriented Synthesis, In Silico Screening, and Antitumor Activity

ChemMedChem, Volume 21, Issue 19, 14 October 2026.
A series of diethylene glycol‐linked cyclic derivatives with diversity in the heterocyclic motif have been synthesized and screened for antitumor activity. Two bis‐thiazolo[3,2‐a]pyrimidinone derivatives displayed moderate cytotoxicity, high selectivity against hepatocellular carcinoma cells, promising VEGFR2, and remarkable FGFR2 inhibitory activities
Sami A. Al‐Hussain, Abdulrahman S. Alharbi, Zeinab A. Muhammad, Alyaa S. Abdel Halim, Magdi E. A. Zaki, Mark C. Bagley, Refaie M. Kassab   +6 more
wiley   +1 more source

Regulation of HERG (KCNH2) potassium channel surface expression by diacylglycerol

, 2010
The HERG (KCNH2) channel is a voltage-sensitive potassium channel mainly expressed in cardiac tissue, but has also been identified in other tissues like neuronal and smooth muscle tissue, and in various tumours and tumour cell lines. The function of HERG
Korhonen, Laura,, Soini, Sanna,, Ramstrom, Cia,, Kivela, Johanna,, Chapman, Hugh,, Viitanen, Tero,, Afrasiabi, Emad,, Lindholm, Dan,, Tornquist, Kid,, Fox, Heli,, Pasternack, Michael,   +10 more
core   +1 more source

Computer simulations of structure-activity relationships for hERG channel blockers. [PDF]

, 2011
The hERG potassium channel is of major pharmaceutical importance, and its blockade by various compounds, potentially causing serious cardiac side effects, is a major problem in drug development.
Bert L. de Groot, Wallin, Göran,, Keranen, H., de Groot, B., Anna Stary-Weinzinger, Göran Wallin, Keränen, Henrik,, Boukharta, L., Åqvist, Johan,, Aqvist, J., Henrik Keränen, Stary-Weinzinger, Anna, Stary-Weinzinger, A., Wallin, G., Lars Boukharta, Boukharta, Lars, Wallin, Göran, Johan Åqvist, Keränen, Henrik, Boukharta, Lars,, de Groot, B. L., Keraenen, H., Åqvist, Johan, de Groot, Bert L.   +23 more
core   +1 more source