Results 41 to 50 of about 12,393 (207)

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

hERG potassium channel inhibition by ivabradine requires channel gating

Journal of Molecular and Cellular Cardiology, 2015
The file associated with this record is under a 12-month embargo from publication in accordance with the publisher's self-archiving policy, available at http://www.elsevier.com/about/company-information/policies/sharing. The full text may be available in the publisher links provided above.
Melgari, Dario, Brack, Kieran E, Zhang, Yihong, El Harchi, Aziza, Mitcheson, John S, Dempsey, Christopher E, Ng, G André, Hancox, Jules C   +7 more
openaire   +3 more sources

Role of hERG potassium channel assays in drug development [PDF]

Channels, 2008
Numerous structurally and functionally unrelated drugs block the hERG potassium channel. HERG channels are involved in cardiac action potential repolarization, and reduced function of hERG lengthens ventricular action potentials, prolongs the QT interval in an electrocardiogram, and increases the risk for potentially fatal ventricular arrhythmias.
Birgit T, Priest, Ian M, Bell, Maria L, Garcia   +2 more
openaire   +2 more sources

Diabetes mellitus attenuates the repolarization reserve in mammalian heart [PDF]

, 2007
Objective: In diabetes mellitus several cardiac electrophysiological parameters are known to be affected. In rodent experimental diabetes models changes in these parameters were reported, but no such data are available in other mammalian species ...
Biliczki, Péter, Bíró, Tamás, Jost, Norbert, Kecskeméti, Valéria, Kocsis, Erzsébet, Lengyel, Csaba Attila, Magyar, János, Nánási, Péter Pál, Papp, Julius Gyula, Skoumal, Réka, Tóth, Miklós, Varró, András, Virág, László   +12 more
core   +1 more source

Hsp40 Chaperones Promote Degradation of the hERG Potassium Channel [PDF]

Journal of Biological Chemistry, 2010
Loss of function mutations in the hERG (human ether-a-go-go related gene or KCNH2) potassium channel underlie the proarrhythmic cardiac long QT syndrome type 2. Most often this is a consequence of defective trafficking of hERG mutants to the cell surface, with channel retention and degradation at the endoplasmic reticulum.
Valerie E, Walker, Michael J H, Wong, Roxana, Atanasiu, Christine, Hantouche, Jason C, Young, Alvin, Shrier   +5 more
openaire   +2 more sources

hERG potassium channel blockade by the HCN channel inhibitor bradycardic agent ivabradine. [PDF]

J Am Heart Assoc, 2015
BackgroundIvabradine is a specific bradycardic agent used in coronary artery disease and heart failure, lowering heart rate through inhibition of sinoatrial nodalHCN‐channels. This study investigated the propensity of ivabradine to interact withKCNH2‐encoded human Ether‐à‐go‐go–Related Gene (hERG) potassium channels, which strongly influence ...
Melgari D, Brack KE, Zhang C, Zhang Y, El Harchi A, Mitcheson JS, Dempsey CE, Ng GA, Hancox JC.   +8 more
europepmc   +5 more sources

Design, synthesis and antibacterial activity of minor groove binders: the role of non-cationic tail groups [PDF]

, 2012
he design and synthesis of a new class of minor groove binder (MGBs) in which, the cationic tail group has been replaced by a neutral, polar variant including cyanoguanidine, nitroalkene, and trifluoroacetamide groups.
Bourdin, Claire, Breen, David, Clements, Carol, Donoghue, Gavin, Fox, Keith, Khalaf, Abedawn, MacMillan, Donna, Scott, Fraser, Sekibo, Doreen, Suckling, Colin   +9 more
core   +1 more source

Hypoxia induced hERG trafficking defect linked to cell cycle arrest in SH-SY5Y cells.

PLoS ONE, 2019
The alpha subunit of the voltage gated human ether-a-go-go-related (hERG) potassium channel regulates cell excitability in a broad range of cell lines.
Damodara Reddy Vaddi, Lin Piao, Shakil A Khan, Ning Wang, Nanduri R Prabhakar, Jayasri Nanduri   +5 more
doaj   +1 more source

Stereoselective Block of hERG Channel by Bupivacaine Scrutinized at Molecular Level

CHIMIA, 2010
In the heart, the hERG voltage-gated potassium channel mediates the IKr current, which is crucial for the duration of cardiac action potential.
Liliana Sintra Grilo, Pierre-Alain Carrupt, Antoine Daina   +2 more
doaj   +1 more source

Potassium dependent structural changes in the selectivity filter of HERG potassium channels

Nature Communications, 2023
AbstractThe fine tuning of biological electrical signaling is mediated by variations in the rates of opening and closing of gates that control ion flux through different ion channels. Human ether-a-go-go related gene (HERG) potassium channels have uniquely rapid inactivation kinetics which are critical to the role they play in regulating cardiac ...
Carus H. Y. Lau, Emelie Flood, Mark J. Hunter, Billy J. Williams-Noonan, Karen M. Corbett, Chai-Ann Ng, James C. Bouwer, Alastair G. Stewart, Eduardo Perozo, Toby W. Allen, Jamie I. Vandenberg   +10 more
openaire   +4 more sources