Results 151 to 160 of about 36,434 (294)

Contribution of chloride channels to the action potential and contraction in human myometrium during labour

open access: yesBritish Journal of Pharmacology, Volume 182, Issue 23, Page 5748-5761, December 2025.
Background and purpose The action potential underpinning calcium delivery for contraction in human uterine smooth muscle (myometrium) consists of an initial spike(s) followed by a prolonged plateau of depolarization to ⁓ −25 mV. The plateau duration establishes contraction duration, especially important in labour.
Helena C. Parkington   +6 more
wiley   +1 more source

New Anticancer 4‐Aryldihydropyrimidinone‐5‐Carboxylates Targeting Hsp90

open access: yesChemical Biology &Drug Design, Volume 106, Issue 6, December 2025.
We report the computational design and early structure–activity relationship optimisation (SAR) studies on new anticancer 4‐aryldihydropyrimidinone‐5‐carboxylate derivatives as inhibitors of heat shock protein 90. Analogue 5d emerged as a useful hit compound, combining inhibition of colony formation in breast cancer cell lines with effective Hsp90 ...
Cinzia Bordoni   +4 more
wiley   +1 more source

X-test-herg

open access: green, 2022
Elina Shaniazova
openalex   +1 more source

Calculation of absolute binding free energies between the hERG channel and structurally diverse drugs

open access: yesScientific Reports, 2019
The human ether-a-go-go-related gene (hERG) encodes a voltage-gated potassium channel that plays an essential role in the repolarization of action potentials in cardiac muscle.
Tatsuki Negami   +3 more
semanticscholar   +1 more source

Electrophysiological characterization of a small molecule activator on human ether-a-go-go-related gene (hERG) potassium channel

open access: yesJournal of Pharmacological Sciences, 2019
The human ether-a-go-go-related gene (hERG) encodes the K+ channel that carries the rapid component of the delayed rectifier current in the human heart. Reduction of hERG activity induced by gene mutations or pharmacological inhibition is responsible for
Xiuming Dong   +6 more
doaj   +1 more source

Mutation-specific peripheral and ER quality control of hERG channel cell-surface expression

open access: yesScientific Reports, 2019
Impaired functional plasma membrane (PM) expression of the hERG K+-channel is associated with Long-QT syndrome type-2 (LQT2) and increased risk of cardiac arrhythmia. Reduced PM-expression is primarily attributed to retention and degradation of misfolded
Brian Foo   +5 more
semanticscholar   +1 more source

Digging into Lipid Membrane Permeation for Cardiac Ion Channel Blocker d-Sotalol with All-Atom Simulations. [PDF]

open access: yes, 2018
Interactions of drug molecules with lipid membranes play crucial role in their accessibility of cellular targets and can be an important predictor of their therapeutic and safety profiles.
Bekker, Slava   +4 more
core  

A new hERG allosteric modulator rescues genetic and drug‐induced long‐QT syndrome phenotypes in cardiomyocytes from isogenic pairs of patient induced pluripotent stem cells

open access: yesEMBO Molecular Medicine, 2016
Long‐QT syndrome (LQTS) is an arrhythmogenic disorder characterised by prolongation of the QT interval in the electrocardiogram, which can lead to sudden cardiac death.

semanticscholar   +1 more source

Disease-associated mutations in KCNE potassium channel subunits (MiRPs) reveal promiscuous disruption of multiple currents and conservation of mechanism. [PDF]

open access: yes, 2002
KCNE genes encode single transmembrane-domain subunits, the MinK-related peptides (MiRPs), which assemble with pore-forming alpha subunits to establish the attributes of potassium channels in vivo.
Abbott, Geoffrey W, Goldstein, Steve AN
core   +1 more source

Molecular Determinants of hERG Channel Block by Terfenadine and Cisapride

open access: yesJournal of Pharmacological Sciences, 2008
Block of cardiac hERG K+ channels by the antihistamine terfenadine and the prokinetic agent cisapride is associated with prolonged ventricular repolarization and an increased risk of ventricular arrhythmia.
Kaichiro Kamiya   +4 more
doaj   +1 more source

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