scholarly journals Display of Potassium Channel–Blocking Tertiapin‐Q Peptides on Gold Nanoparticles Enhances Depolarization of Cellular Membrane Potential

2019 ◽  
Vol 36 (3) ◽  
pp. 1800493 ◽  
Author(s):  
Megan E. Muroski ◽  
Eunkeu Oh ◽  
JeffreyR. Deschamps ◽  
James B. Delehanty
Keyword(s):  
Gold Nanoparticles ◽  
Membrane Potential ◽  
Potassium Channel ◽  
Cellular Membrane ◽  
Channel Blocking

scholarly journals Beyond hemostasis: a snake venom serine protease with potassium channel blocking and potential antitumor activities

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Johara Boldrini-França ◽  
Ernesto Lopes Pinheiro-Junior ◽  
Steve Peigneur ◽  
Manuela Berto Pucca ◽  
Felipe Augusto Cerni ◽  
...  
Keyword(s):  
Potassium Channel ◽  
Serine Protease ◽  
Snake Venom ◽  
Antitumor Activities ◽  
Channel Blocking ◽  
Potential Antitumor

scholarly journals Voltage-gated potassium channel Kv1.3 in rabbit ciliary epithelium regulates the membrane potential via coupling intracellular calcium

2008 ◽  
Vol 121 (22) ◽  
pp. 2272-2277 ◽  
Author(s):  
Yan-feng LI ◽  
Ye-hong ZHUO ◽  
Wei-na BI ◽  
Yu-jing BAI ◽  
Yan-na LI ◽  
...  
Keyword(s):  
Membrane Potential ◽  
Potassium Channel ◽  
Intracellular Calcium ◽  
Ciliary Epithelium ◽  
Voltage Gated

scholarly journals A High-Throughput Electrophysiology Assay Identifies Inhibitors of the Inwardly Rectifying Potassium Channel Kir7.1

2015 ◽  
Vol 20 (6) ◽  
pp. 739-747 ◽  
Author(s):  
Paul D. Wright ◽  
Srinivasan Kanumilli ◽  
David Tickle ◽  
Jamie Cartland ◽  
Nathalie Bouloc ◽  
...  
Keyword(s):  
Membrane Potential ◽  
Potassium Channel ◽  
Screening Strategy ◽  
Resting Membrane Potential ◽  
Pharmacological Characterization ◽  
Inwardly Rectifying Potassium Channel ◽  
A Cell ◽  
Automated Patch Clamp ◽  
Patch Clamp Electrophysiology ◽  
Inwardly Rectifying

Kir7.1 is an inwardly rectifying potassium channel that has been implicated in controlling the resting membrane potential of the myometrium. Abnormal uterine activity in pregnancy plays an important role in postpartum hemorrhage, and novel therapies for this condition may lie in manipulation of membrane potential. This work presents an assay development and screening strategy for identifying novel inhibitors of Kir7.1. A cell-based automated patch-clamp electrophysiology assay was developed using the IonWorks Quattro (Molecular Devices, Sunnyvale, CA) system, and the iterative optimization is described. In total, 7087 compounds were tested, with a hit rate (>40% inhibition) of 3.09%. During screening, average Z′ values of 0.63 ± 0.09 were observed. After chemistry triage, lead compounds were resynthesized and activity confirmed by IC50 determinations. The most potent compound identified (MRT00200769) gave rise to an IC50 of 1.3 µM at Kir7.1. Compounds were assessed for selectivity using the inwardly rectifying potassium channel Kir1.1 (ROMK) and hERG (human Ether-à-go-go Related Gene). Pharmacological characterization of known Kir7.1 inhibitors was also carried out and analogues of VU590 tested to assess selectivity at Kir7.1.

Investigation of the effect of magnetite iron oxide particles size on cytotoxicity in A549 cell line

2019 ◽  
Vol 35 (11-12) ◽  
pp. 703-713 ◽  
Author(s):  
Athena Rafieepour ◽  
Mansour R Azari ◽  
Habibollah Peirovi ◽  
Fariba Khodagholi ◽  
Jalal Pourahmad Jaktaji ◽  
...  
Keyword(s):  
Membrane Potential ◽  
Iron Oxide ◽  
Cell Line ◽  
Cellular Membrane ◽  
Human Cell Line ◽  
Control Measures ◽  
Iron Oxide Particles ◽  
Magnetite Particles ◽  
Oxide Particles ◽  
Reduced Rate

Introduction: Magnetite as iron oxide is widely used in various industries, in the pharmaceutical industry in particular where it is used for its magnetic properties. The environmental and occupational exposure to airborne nanoparticles and microparticles of iron oxide compounds have been reported. Since authors have reported contradictory results, the objective of this study was to investigate the effect of particles’ size in their toxicities. Methods: The human cell line A549 was exposed with magnetite iron oxide in two size categories of micro (≥5 µm) and nano (<100 nm), with four concentrations of 10, 50, 100, and 250 µg/ml at two time periods of 24 and 72 h. The cell viability, reactive oxygen species (ROS), changes in mitochondrial membrane potential, and incidence of apoptosis were studied. Results: Nano and micro magnetite particles demonstrated diverse toxicity effects on the A549 cell line at the 24- and 72-h exposure periods; however, the effects produced were time- and concentration-dependent. Nano magnetite particles produced greater cellular toxicities in forms of decreased viabilities at concentration exposures greater than 50 µg/ml ( p < 0.05), along with increased ROS ( p < 0.05), decreased cellular membrane potential ( p < 0.05), and reduced rate of apoptosis ( p < 0.05). Discussion: The results of this study demonstrated that magnetite iron in nano-range sizes had a greater absorbability for the A549 cell line compared to micro sizes, and at the same time, nanoparticles were more toxic than microparticles, demonstrating higher production of ROS and decreased viabilities. Considering the greater toxicity of nanoparticles of magnetite iron in this study, thorough precautionary control measures must be taken before they can be used in various industries.

A Novel Potassium Channel Blocking Toxin from the ScorpionPandinus imperator:  A1H NMR Analysis Using a Nano-NMR Probe†

Biochemistry ◽  
1997 ◽  
Vol 36 (9) ◽  
pp. 2649-2658 ◽  
Author(s):  
M. Delepierre ◽  
A. Prochnicka-Chalufour ◽  
L. D. Possani
Keyword(s):  
Potassium Channel ◽  
Nmr Analysis ◽  
Channel Blocking
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