Ancillary subunits KChIP2c and DPP6 differentially modulate the inhibition of Kv4.2 channels by riluzole.

In native tissue, Kv4.2 channels associate with the ancillary subunits Kv channels interacting proteins (KChIPs) and dipeptidyl peptidase-related proteins (DPPs) to evoke rapidly activating/inactivating currents in the heart (I) and brain (I). Despite extensive knowledge of Kv4.

Inhibition of Kv2.1 potassium channels by the antidepressant drug sertraline.

Sertraline is a commonly used antidepressant of the selective serotonin reuptake inhibitors (SSRIs) class. In this study, we have used the patch-clamp technique to assess the effects of sertraline on Kv2.1 channels heterologously expressed in HEK-293 cells and on the voltage-gated potassium currents (I) of Neuro 2a cells, which are predominantly mediated by Kv2.

Crosstalk between cholesterol and PIP in the regulation of Kv7.2/Kv7.3 channels.

The activity of neuronal Kv7.2/Kv7.3 channels is critically dependent on PIP and finely modulated by cholesterol.

Riluzole inhibits Kv4.2 channels acting on the closed and closed inactivated states.

Riluzole is an anticonvulsant drug also used to treat the amyotrophic lateral sclerosis and major depressive disorder. This compound has antiglutamatergic activity and is an important multichannel blocker. However, little is known about its actions on the Kv4.

Inhibitory effect of terfenadine on Kir2.1 and Kir2.3 channels.

Terfenadine is a second-generation H1-antihistamine that despite potentially can produce severe side effects it has recently gained attention due to its anticancer properties. Lately, the subfamily 2 of inward rectifier potassium channels (Kir2) has been implicated in the progression of some tumoral processes. Hence, we characterized the effects of terfenadine on Kir2.

In vitro and in silico characterization of the inhibition of Kir4.1 channels by aminoglycoside antibiotics.

Background And Purpose: Aminoglycoside antibiotics are positively charged molecules that are known to inhibit several ion channels. In this study, we have shown that aminoglycosides also inhibit the activity of Kir4.1 channels.

Functional marriage in plasma membrane: Critical cholesterol level-optimal protein activity.

In physiology, homeostasis refers to the condition where a system exhibits an optimum functional level. In contrast, any variation from this optimum is considered as a dysfunctional or pathological state. In this review, we address the proposal that a critical cholesterol level in the plasma membrane is required for the proper functioning of transmembrane proteins.

Cytoskeleton disruption affects Kv2.1 channel function and its modulation by PIP.

Voltage-gated potassium channels are expressed in a wide variety of excitable and non-excitable cells and regulate numerous cellular functions. The activity of ion channels can be modulated by direct interaction or/and functional coupling with other proteins including auxiliary subunits, scaffold proteins and the cytoskeleton. Here, we evaluated the influence of the actin-based cytoskeleton on the Kv2.

Dual regulation of hEAG1 channels by phosphatidylinositol 4,5-bisphosphate.

The ether-à-go-go1 (EAG1, Kv10.1) K channel is a member of the voltage-gated K channel family mainly expressed in the central nervous system and cancer cells. Membrane lipids regulate several voltage-gated K channels but their influence on EAG1 channels has been poorly explored.

Regulation of Kv7.2/Kv7.3 channels by cholesterol: Relevance of an optimum plasma membrane cholesterol content.

Kv7.2/Kv7.3 channels are the molecular correlate of the M-current, which stabilizes the membrane potential and controls neuronal excitability.

Regulation of Kv2.1 channel inactivation by phosphatidylinositol 4,5-bisphosphate.

Phosphatidylinositol 4,5-bisphosphate (PIP) is a membrane phospholipid that regulates the function of multiple ion channels, including some members of the voltage-gated potassium (Kv) channel superfamily. The PIP sensitivity of Kv channels is well established for all five members of the Kv7 family and for Kv1.2 channels; however, regulation of other Kv channels by PIP remains unclear.

Phytochemicals genistein and capsaicin modulate Kv2.1 channel gating.

Background: Phytochemicals are a large group of plant-derived compounds that have a broad range of pharmacological effects. Some of these effects are derived from their action on transport proteins, including ion channels. The present study investigates the effects of the phytochemicals genistein and capsaicin on voltage-gated potassium Kv2.

High-potency block of Kir4.1 channels by pentamidine: Molecular basis.

Inward rectifier potassium (Kir) channels are expressed in almost all mammalian tissues and contribute to a wide range of physiological processes. Kir4.1 channel expression is found in the brain, inner ear, eye, and kidney.

Modulation of the voltage-gated potassium channel Kv2.1 by the anti-tumor alkylphospholipid perifosine.

Background: The aim of the present study was to assess the effects of perifosine-a third generation alkylphospholipid analog with anti-tumor properties-on the activity of Kv2.1 channels.

Methods: The whole-cell patch clamp technique was applied to follow the modulatory effect of perifosine on Kv2.

Modulation of Kv2.1 channels inactivation by curcumin.

Background: The aim of the present study was to assess the effects of curcumin on the voltage-dependent Kv2.1 potassium channel.

Methods: The whole-cell patch-clamp technique was used to explore the regulation of Kv2.

Infection by Trypanosoma cruzi enhances anion conductance in rat neonatal ventricular cardiomyocytes.

Recent studies on malaria-infected erythrocytes have shown increased anion channel activity in the host cell membrane, increasing the exchange of solutes between the cytoplasm and exterior. In the present work, we addressed the question of whether another intracellular protozoan parasite, Trypanosoma cruzi, alters membrane transport systems in the host cardiac cell. Neonatal rat cardiomyocytes were cultured and infected with T.