Article
Chemistry, Multidisciplinary
Zixuan Lu, Chiara Barberio, Ana Fernandez-Villegas, Aimee Withers, Alexandra Wheeler, Konstantinos Kallitsis, Eleonora Martinelli, Achilleas Savva, Becky M. Hess, Anna-Maria Pappa, Gabriele S. Kaminski Schierle, Roisin M. Owens
Summary: This work reports a new system that integrates neuron membranes with organic microelectrode arrays for drug studies targeting neuronal ion channels. The system overcomes the challenges of traditional methods and provides an easy-to-test, rapid, ultra-sensitive, cell-free, and high-throughput platform to monitor dose-dependent ion-channel blocking effects on native neuronal membranes.
Review
Biochemistry & Molecular Biology
Silvia Cassinelli, Carla Vinola-Renart, Anna Benavente-Garcia, Maria Navarro-Perez, Jesusa Capera, Antonio Felipe
Summary: Protein lipidation is a common form of posttranslational modification that regulates various aspects of a protein's physiology, including its structure, stability, and interaction with cellular membranes. Palmitoylation, the addition of long saturated fatty acid chains to proteins, is a key form of lipidation. Enzymes called acyltransferases and thioesterases control the behavior of palmitoylated proteins through a series of acylation and deacylation cycles. Palmitoylation plays a pleiotropic role in regulating the trafficking, spatial organization, and electrophysiological properties of ion channels, particularly voltage-gated ion channels (VGICs). Dysregulation of palmitoylation in VGICs and associated subunits is linked to the development of diseases such as cancer and mental disorders. Therefore, protein palmitoylation is emerging as an important factor in cellular protein regulation and human health.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Physiology
Rabab Rashwan, David M. Hunt, Livia S. Carvalho
Summary: Photoreceptors exhibit remarkable adaptability by adjusting gain to respond to different levels of ambient light intensity. The dynamic operating range of photoreceptors is maintained by a balance of inward and outward currents modulated by various ion channels. Potassium and calcium voltage-gated channels play crucial roles in setting the dark resting potential and synaptic signal processing, contributing significantly to visual processing.
PFLUGERS ARCHIV-EUROPEAN JOURNAL OF PHYSIOLOGY
(2021)
Article
Medicine, General & Internal
Kai-Feng Shen, Xiao-Lin Yang, Guo-Long Liu, Gang Zhu, Zhong-Ke Wang, Xian-Jun Shi, Ting-Ting Wang, Zhi-Feng Wu, Sheng-Qing Lv, Shi-Yong Liu, Hui Yang, Chun-Qing Zhang
Summary: The study revealed that ClC-mediated current was increased in the hippocampal neurons of chronic TLE mice. Application of chloride channel blockers NPPB and DIDS reduced the current and increased inhibitory synaptic transmission in TLE mice. These drugs also decreased seizure frequency and the average power of ictal high-frequency oscillations in TLE mice.
Article
Pharmacology & Pharmacy
Christopher Katnik, Javier Cuevas
Summary: The study focuses on intracellular ionic imbalance resulting from ischemic stroke, and the impact of NKCC1 antagonists on Na+ and Ca2+ overload. Loop diuretics BMN and EA inhibited ischemia-acidosis induced Ca2+ overload, but did not reduce Na+ increases.
FRONTIERS IN PHARMACOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Valerij S. Sokolov, Vladimir V. Cherny, Artem G. Ayuyan, Thomas E. DeCoursey
Summary: H(V)1 channels, resembling the voltage-sensing domain of other voltage-gated ion channels, feature a unique Delta pH dependent gating mechanism that regulates channel opening by pH on both sides of the membrane. Two mechanisms, the countercharge mechanism and the electrostatic mechanism, are proposed to contribute to this Delta pH dependent gating. Both mechanisms are likely to operate together to regulate the gating of H(V)1 channels.
BIOCHIMICA ET BIOPHYSICA ACTA-BIOENERGETICS
(2021)
Article
Chemistry, Multidisciplinary
Shuai Gao, Nieng Yan
Summary: This study reports the structures of Ca(v)1.1 bound with different drugs, revealing the molecular basis for their effects. The structures show that amlodipine and nifedipine have different impacts on Ca(v)1.1, while the two enantiomers of Bay K8644 as agonists are insufficient to maintain the activated state of the channel.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Biochemistry & Molecular Biology
Marta Martini, Giorgio Rispoli
Summary: Some sensory disorders in hearing, vestibular, and vision can be attributed to voltage-gated Ca2+ channels in sensory cells. In this study, the Na+ current flowing through L- and R-type Ca2+ channels in labyrinth hair cells was investigated. The activation and deactivation of the Na+ current in L-type channels were affected by low Ca2+ concentration, resulting in increased current amplitude. The R-type Na+ current was partially blocked by nifedipine and its current amplitude increased in low Ca2+ condition. Furthermore, the selectivity filter of R channels was less affected by external Ca2+ compared to L channels.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Paz Duran, Santiago Loya-Lopez, Dongzhi Ran, Cheng Tang, Aida Calderon-Rivera, Kimberly Gomez, Harrison J. Stratton, Sun Huang, Ya-ming Xu, E. M. Kithsiri Wijeratne, Samantha Perez-Miller, Zhiming Shan, Song Cai, Anna T. Gabrielsen, Angie Dorame, Kyleigh A. Masterson, Omar Alsbiei, Cynthia L. Madura, Guoqin Luo, Aubin Moutal, John Streicher, Gerald W. Zamponi, A. A. Leslie Gunatilaka, Rajesh Khanna
Summary: This study identified argentatin C, a compound derived from the Native American medicinal plant Parthenium incanum, which can block the activity of voltage-gated sodium and calcium channels and has potential as a novel treatment for painful conditions. Experimental results demonstrated that argentatin C decreased ion currents and excitability in sensory neurons and relieved postsurgical pain in a mouse model. Therefore, argentatin C may serve as an alternative therapy for chronic pain management.
BRITISH JOURNAL OF PHARMACOLOGY
(2023)
Review
Physiology
Murat Oz, Keun-Hang Susan Yang, Mohamed Omer Mahgoub
Summary: This report reviews and discusses the direct effects of endogenous, phytogenic, and synthetic cannabinoids on the functional properties of ligand-gated ion channels, as well as the possible mechanisms mediating these effects.
FRONTIERS IN PHYSIOLOGY
(2022)
Article
Neurosciences
Rahul Kumar Rathour, Hanoch Kaphzan
Summary: This study investigates the impact of variability in voltage-gated ion channels (VGICs) expression on information transfer. The results show that the expression variability of VGICs leads to variability in mutual information transfer and affects output firing frequencies. Virtual knockout experiments demonstrate that the A-type K+ channel plays a major role in information processing and transfer.
FRONTIERS IN CELLULAR NEUROSCIENCE
(2022)
Article
Biochemistry & Molecular Biology
Denis P. Laryushkin, Sergei A. Maiorov, Valery P. Zinchenko, Sergei G. Gaidin, Artem M. Kosenkov
Summary: The study demonstrates that blockade of L-type VGCC can reduce the half-width and amplitude of bicuculline-induced [Ca2+](i) oscillations, decrease the number of PDSs in a cluster, and shorten the cluster duration, while insignificantly affecting the pattern of individual PDSs and the frequency of cluster occurrence.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Multidisciplinary Sciences
Muhammad Imran Arshaad, Magdalena Elisabeth Siwek, Christina Henseler, Johanna Daubner, Dan Ehninger, Juergen Hescheler, Agapios Sachinidis, Karl Broich, Anna Papazoglou, Marco Weiergraeber
Summary: The study revealed the significant role of Ca(v)3.2 Ca2+ channels in hippocampal theta oscillations, showing increased power in the theta frequency range and altered theta activity and architecture following Ca(v)3.2 ablation. qPCR evaluation identified changes in key genes in Ca(v)3.2(-/-) mice, particularly in the GABAergic system. These transcriptional changes may be functionally linked to the observed electrophysiological phenotype.
SCIENTIFIC REPORTS
(2021)
Review
Multidisciplinary Sciences
Xinwei Wang, Xueping Li
Summary: Voltage-gated ion channels play an important role in the metabolism of chondrocytes and extracellular matrix, regulating pain neurotransmitters between cartilage and the central nervous system. Abnormal ion channel transport and increased calcium influx in the osteoarthritis model lead to heightened neuronal excitability. The changes in ion channels are closely associated with the development of osteoarthritis and individual risk factors. Further research should explore the impact of voltage-gated ion channels on the metabolism of chondrocytes and surrounding tissues, aiding in the development of effective targeted drugs to alleviate the progression of osteoarthritis.
Article
Multidisciplinary Sciences
Tetsuya Yamada, Shoi Shi, Hiroki R. Ueda
Summary: Neural oscillations are regulated by molecular mechanisms and network connectivity of neurons. Recent research has found that slowly inactivating potassium channels play a crucial role in the firing pattern of spindle oscillations, while leak sodium and potassium channels competitively regulate the base value and time constant of spindle oscillations.
