Results 71 to 80 of about 33,807 (258)
Drug trapping in hERG K+ channels: (not) a matter of drug size?
MedChemComm, 2015 The hERG cavity can trap very bulky compounds, without perturbing normal gate closure.
T. Linder +7 more
semanticscholar +1 more source
Independent derivations of the axis of arrhythmia for predicting drug‐induced torsades de pointes
British Journal of Pharmacology, EarlyView.Abstract Background and Purpose: Torsades de pointes is a potentially lethal ventricular arrhythmia that can be induced by many classes of drugs. The risk for a given drug depends upon the combination of cardiac ion channels that it targets. The axis of arrhythmia quantifies that risk. It is a conceptual line in the electrophysiology that describes the
Stewart Heitmann +2 more
wiley +1 more source
Digging into Lipid Membrane Permeation for Cardiac Ion Channel Blocker d-Sotalol with All-Atom Simulations. [PDF]
, 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
British Journal of Pharmacology, EarlyView.Background and purpose Traumatic brain injury (TBI) is considered to be a leading cause of mortality and disability worldwide. After TBI, innate immunity is rapidly activated in response to damage‐associated molecular patterns, such as ATP release, recognised by P2X7 receptors.
Inés Valencia +15 more
wiley +1 more source
MicroRNA 362-3p Reduces hERG-related Current and Inhibits Breast Cancer Cells Proliferation
Cancer Genomics & Proteomics, 2019 Background/Aim: hERG potassium channels enhance tumor invasiveness and breast cancer proliferation. MicroRNA (miRNA) dysregulation during cancer controls gene regulation. The objective of this study was to identify miRNAs that regulate hERG expression in
Abdullah A Assiri +6 more
semanticscholar +1 more source
Structure‐based discovery of thiamine uptake inhibitors
British Journal of Pharmacology, EarlyView.Background and Purpose Thiamine (vitamin B1) is an essential coenzyme and catalyses various reactions in central metabolic pathways. Since mammals have lost the ability to synthesise thiamine de novo, this micronutrient has to be imported via the high affinity solute carriers SLC19A2 and A3 across the plasma membrane.
Florian Gabriel +2 more
wiley +1 more source
Effects of cariprazine on hERG 1A and hERG 1A/3.1 potassium channels
European Journal of Pharmacology, 2019 Cariprazine is a novel atypical antipsychotic drug that is widely used for the treatment of schizophrenia and bipolar mania/mixed disorder. We used the whole-cell patch-clamp technique to investigate the effects of cariprazine on hERG channels that are stably expressed in HEK cells. Cariprazine inhibited the hERG 1A and hERG 1A/3.1 tail currents at -50
Hong Joon Lee +3 more
openaire +3 more sources
Gain of function mutants: Ion channels and G protein-coupled receptors [PDF]
, 2000 Many ion channels and receptors display striking phenotypes for gain-of-function mutations but milder phenotypes for null mutations. Gain of molecular function can have several mechanistic bases: selectivity changes, gating changes including constitutive
Karschin, Andreas, Lester, Henry A.
core +1 more source
British Journal of Pharmacology, EarlyView.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
, 2017 Blockage of some ion channels and in particular, the hERG cardiac potassium channel delays cardiac repolarization and can induce arrhythmia. In some cases it leads to a potentially life-threatening arrhythmia known as Torsade de Pointes (TdP).
Buzatu, Dan +3 more
core +1 more source