Results 61 to 70 of about 1,529,868 (197)

Pediatric Developmental Safety Assessment and New Approach Methodologies: US FDA/Triangle CERSI Workshop Report

Clinical Pharmacology &Therapeutics, Volume 120, Issue 5, Page 1240-1249, November 2026.
Pediatric developmental safety assessment presents distinct challenges in drug development. Children undergo dynamic changes in organ systems and drug disposition pathways during development, and drug‐related effects may be delayed or manifested differently than in adults.
Gilbert J. Burckart, Gelareh Abulwerdi, Christin L. Daniels, Calib Choi, Rebecca Racz, Jean‐Pierre Valentin, Kristin Ardlie, Nicholas Tatonetti, Susan Laffan, Marjory Moreau, Will Redfern, Lang Li, James J. Hickman, Rajanikanth Madabushi, Bhagwat Prasad, Lynne Yao, Paul B. Watkins   +16 more
wiley   +1 more source

Two Types of K⁺ Channel Subunit, Erg1 and KCNQ2/3, Contribute to the M-Like Current in a Mammalian Neuronal Cell [PDF]

, 1999
The potassium M current was originally identified in sympathetic ganglion cells, and analogous currents have been reported in some central neurons and also in some neural cell lines.
Abogadie, FC, Wood, IC, London, B, Buckley, NJ, Brown, DA, Hadley, JK, Delmas, P, Selyanko, AA   +7 more
core  

Inhibition of HERG potassium channels by the antimalarial agent halofantrine [PDF]

British Journal of Pharmacology, 2000
Halofantrine is a widely used antimalarial agent which has been associated with prolongation of the ‘QT interval’ of the electrocardiogram (ECG), torsades de pointes and sudden death. Whilst QT prolongation is consistent with halofantrine‐induced increases in cardiac ventricular action potential duration, the cellular mechanism for these observations
H, Tie, B D, Walker, C B, Singleton, S M, Valenzuela, J A, Bursill, K R, Wyse, S N, Breit, T J, Campbell   +7 more
openaire   +2 more sources

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

Nature Communications, 2023
Abstract The 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 ...
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   +6 more sources

Multitarget Drug Design for Cardiovascular Disease: Bridging Chemistry and Medicine

ChemMedChem, Volume 21, Issue 19, 14 October 2026.
Many pathophysiological pathways associated with cardiovascular diseases involve multiple drug targets. This article reviews recent advances in the development of pharmacological compounds capable of simultaneously modulating multiple mechanisms. Multitarget drugs offer a promising therapeutic approach for complex cardiovascular disorders, including ...
Gyuzel Y. Mitronova, Vladimir N. Belov, Constanze Schmidt, Stephan E. Lehnart   +3 more
wiley   +1 more source

Functional consequences of methionine oxidation of hERG potassium channels [PDF]

Biochemical Pharmacology, 2007
Reactive species oxidatively modify numerous proteins including ion channels. Oxidative sensitivity of ion channels is often conferred by amino acids containing sulfur atoms, such as cysteine and methionine. Functional consequences of oxidative modification of methionine in human ether à go-go related gene 1 (hERG1), which encodes cardiac I(Kr ...
Zhi, Su, James, Limberis, Ruth L, Martin, Rong, Xu, Katrin, Kolbe, Stefan H, Heinemann, Toshinori, Hoshi, Bryan F, Cox, Gary A, Gintant   +8 more
openaire   +2 more sources

Characterization of the novel mutant A78T-HERG from a long QT syndrome type 2 patient: Instability of the mutant protein and stabilization by heat shock factor 1

Journal of Arrhythmia, 2016
Background: The human ether-a-go-go-related gene (HERG) encodes the α-subunit of rapidly activating delayed-rectifier potassium channels. Mutations in this gene cause long QT syndrome type 2 (LQT2).
Takehito Kondo, Ichiro Hisatome, Shouichi Yoshimura, Endang Mahati, Tomomi Notsu, Peili Li, Kazuhiko Iitsuka, Masaru Kato, Kazuyoshi Ogura, Junichiro Miake, Takeshi Aiba, Wataru Shimizu, Yasutaka Kurata, Shinji Sakata, Naoe Nakasone, Haruaki Ninomiya, Akira Nakai, Katsumi Higaki, Yasushi Kawata, Yasuaki Shirayoshi, Akio Yoshida, Kazuhiro Yamamoto   +21 more
doaj   +1 more source

Trafficking Deficiency of TMEM175 Variants in Parkinson's Disease Pathogenesis and the Prospects of Precision Medicine

Advanced Science, Volume 13, Issue 57, 14 October 2026.
This study identifies that the PD‐associated TMEM175‐L156P variant disrupts lysosomal ion channel trafficking by causing aberrant endoplasmic reticulum retention. A “chaperone–agonist” bifunctional small molecule restores TMEM175‐L156P lysosomal localization and channel function, thereby alleviating PD‐relevant cellular phenotypes and highlighting a ...
Ting Luo, Yu He, Shuyao Li, Haoyu Guan, Ruili Cui, Yu Shi, Zhongwen Jiang, Siyu Wang, Xuan Li, Jiyuan Li, Mei Hu, Yupeng Zhou, Beisha Tang, Yanyan Zhang, Zhaobing Gao, Yu Zhou, Zhenhua Liu, Ping Li   +17 more
wiley   +1 more source

The Real‐World Safety Profile of Haloperidol: A Comprehensive Pharmacovigilance Analysis Using the Large‐Scale FAERS Database

CNS Neuroscience &Therapeutics, Volume 32, Issue 10, October 2026.
This first comprehensive FAERS‐based pharmacovigilance analysis of haloperidol over two decades characterized the real‐world safety profile across 9916 reports. Strong signals were found for nervous, psychiatric, and cardiac disorders. Known risks were confirmed and novel signals revealed. Sex‐ and age‐specific vulnerabilities were identified. Findings
Nengping Luo, Lu Xiao, Ying Liu, Xiang Liu   +3 more
wiley   +1 more source

Modulation of HERG potassium channel function by drug action

Annals of Medicine, 2004
Repolarization of cardiomyocytes is mainly performed by the rapid component of the delayed rectifier potassium current, I(Kr), which is encoded by the human ether-a-go-go-related gene (HERG). Inhibition of HERG potassium currents by class III antiarrhythmic drugs causes lengthening of the cardiac action potential, which produces a beneficial ...
Dierk, Thomas, Christoph A, Karle, Johann, Kiehn   +2 more
openaire   +2 more sources