Results 71 to 80 of about 1,218,415 (224)

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

An Update on the Structure of hERG

Frontiers in Pharmacology, 2020
The human voltage-sensitive K+ channel hERG plays a fundamental role in cardiac action potential repolarization, effectively controlling the QT interval of the electrocardiogram.
Andrew Butler, Matthew V. Helliwell, Yihong Zhang, Jules C. Hancox, Christopher E. Dempsey   +4 more
doaj   +1 more source

Developing the Dopamine D3 Receptor (D3R) Antagonist, (R)‐VK4‐116, as a Non‐Opioid Medication for the Treatment of Opioid Use Disorder

Medicinal Research Reviews, EarlyView.
ABSTRACT Opioid use disorder (OUD) remains a major global health challenge, and currently approved treatments (methadone, buprenorphine, and naltrexone) are all opioid receptor‐targeting drugs with limitations in access, adherence, stigma, and use in polysubstance use disorders. Because the dopamine D3 receptor (D3R) is enriched in limbic brain regions
Chia‐Kuei Wu, Yu‐Chih Lin, Junfeng Huang, Bangwei Ding, Pramod Terse, Rahul Nandre, Haksong Jin, Molly Congdon, Kun Shen, Philip Sanderson, Gregory Tawa, Stephanie Mounaud, Marta De Santis, Donald Lo, Elizabeth A. Ottinger, Amy Hauck Newman   +15 more
wiley   +1 more source

Assessing hERG Channel Inhibition Using PatchXpress [PDF]

Clinics in Laboratory Medicine, 2005
PatchXpress, an automated 16-channel parallel patch clamp system, was used to determine inhibition of human ether-a-go-go related gene (hERG) potassium channels by known blockers. A monoclonal cell line stably expressing hERG potassium channels was generated in CHO-KI cells.
Justin Q, Ly, Gordon, Shyy, Dinah L, Misner   +2 more
openaire   +2 more sources

Integrative Approaches in Cardiovascular Disease: The Role of Nutraceuticals in Heart Failure, Atrial Fibrillation, and Related Conditions

Phytotherapy Research, EarlyView.
Schematic representation of the shared pathophysiological mechanisms underlying heart failure (HF) and atrial fibrillation (AF), including inflammation, oxidative stress, endothelial dysfunction, and fibrosis. The figure highlights the clinical and mechanistic convergence of conventional pharmacological therapies and selected nutraceuticals in ...
Laura Beatrice Mattioli, Ivan Corazza, Roberta Budriesi, Luca Camarda, Maria Carelli, Alberto Spadotto, Igor Diemberger   +6 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  

Action potential clamp and pharmacology of the variant 1 Short QT Syndrome T618I hERG K⁺ channel.

PLoS ONE, 2012
BackgroundThe familial Short QT Syndrome (SQTS) is associated with an increased risk of cardiac arrhythmia and sudden death. Gain-of-function mutations in the hERG K(+) channel protein have been linked to variant 1 of the SQTS. A hERG channel pore (T618I)
Aziza El Harchi, Dario Melgari, Yi Hong Zhang, Henggui Zhang, Jules C Hancox   +4 more
doaj   +1 more source

Multi‐Target Pharmacological Mechanisms of Salvia miltiorrhiza Bunge in Metabolic Syndrome and Cardiovascular Diseases: A Comprehensive Review Based on the Theory of “Same Treatment for Different Diseases”

Phytotherapy Research, EarlyView.
Salvia miltiorrhiza Bunge in metabolic syndrome and cardiovascular diseases: multi‐target actions on shared signaling pathways. ABSTRACT Metabolic syndrome (MetS) represents a clinical disorder characterized by the clustering of conditions including obesity, elevated blood sugar levels, and high lipid levels, which are intricately linked to the onset ...
Zhiyi Jia, Kaiyi Wu, Jiaying Qi, Nana Huang, Yusheng Liu, Xiumei Gao, Rong Sun   +6 more
wiley   +1 more source

Artificial intelligence empowers targeted protein degradation: Core technological innovations, multi‐scenario applications, and translational prospects

Smart Molecules, EarlyView.
AI is transforming TPD by improving the design, prediction, and optimization of degraders such as PROTACs, molecular glues, and LYTACs. This review summarizes key AI‐driven advances, highlights applications across drug discovery stages, and discusses remaining challenges and future directions for accelerating the development of therapies against ...
Shuanglin Qin, Rui Peng, Guangshuai Zhang, Si Yan, Jin Xiao, Zishu Liu, Ziyu Tan, Qingqing Xie, Shangjie Li, Wei Luo, Xiaohe Xiao   +10 more
wiley   +1 more source

Effects of hERG K+ channel beyond prolonged QT syndrome

, 2022
The human ether -a -go-go - related gene (hERG) potassium channel assumes the focal part for directing cardiac sensitivity; heart activity like repolarization adequately controlling the QT time interval electrocardiogram, that is communicated within our ...
Arghya Bhattacharya, Meghna Santra, Sahim Mondal, Debraj Mukhopadhyay, Soumik Bhattacharjee, Vinay Sai Lankipalli, Sumit Nandi, Dattatreya Mukherjee, Shibam Kundagrami, Bikram Dhara   +9 more
core   +1 more source