Article
Chemistry, Physical
Mehdi Yoosefian, Batool Tajaddini, Saeid Ahmadzadeh, Maryam Zeraati-Moghani, Zahra Pakdin-Parizi
Summary: Drinking excessive alcohol can cause chronic diseases and serious problems such as heart disease, high blood pressure, stroke, digestive problems, and liver disease. A molecular dynamics simulation study found that ethanol blocks calcium channels and interferes with calcium ion passage. Furthermore, calcium ions have a greater tendency to interact with residues inside the protein channel in the presence of ethanol.
JOURNAL OF MOLECULAR LIQUIDS
(2023)
Article
Multidisciplinary Sciences
Tadashi Nakajima, Reika Kawabata-Iwakawa, Shuntaro Tamura, Hiroshi Hasegawa, Takashi Kobari, Hideki Itoh, Minoru Horie, Masahiko Nishiyama, Masahiko Kurabayashi, Yoshiaki Kaneko, Hideki Ishii
Summary: Gain-of-function mutations in the CACNA1C gene cause long QT syndrome. A novel mutation in CACNA1C was identified in this study, which was associated with non-syndromic long QT syndrome. The study provides insights into the biophysical defects and pathophysiological roles of the mutation.
Article
Chemistry, Medicinal
Eleni Kaisis, Laura J. J. Thei, Gary J. J. Stephens, Mark L. L. Dallas
Summary: Cav2.2 channels are modulated by Ab(1-42) peptides, and this modulation has different effects at different concentrations. This study reveals a potential mechanistic link between amyloid accumulation and Cav2.2 channel modulation.
Article
Biochemistry & Molecular Biology
Julien Giribaldi, Jean Chemin, Marie Tuifua, Jennifer R. Deuis, Rosanna Mary, Irina Vetter, David T. Wilson, Norelle L. Daly, Christina I. Schroeder, Emmanuel Bourinet, Sebastien Dutertre
Summary: A novel spider toxin, named Pmu1a, was discovered from the venom of Pterinochilus murinus. It has inhibitory activity on both hNa(V)1.7 and hCa(V)3.2 channels, which are therapeutic targets involved in pain pathways. This finding may lead to the development of compounds targeting these channels for chronic pain treatment.
Article
Biochemistry & Molecular Biology
Chin-Meng Ko, Chee-Kin Then, Yen-Kuang Lin, Yu-Ming Kuo, Shing-Chuan Shen
Summary: This study investigated the effects of far-infrared (FIR) on lead-induced renal damage and found that FIR mitigated the damage by modulating calcium influx and optimizing mitochondrial function, suggesting its potential as a therapeutic approach for lead toxicity in the kidneys.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Multidisciplinary
Yangmei Li, Chao Chang, Zhi Zhu, Lan Sun, Chunhai Fan
Summary: The dysfunction of voltage-gated calcium channels leading to a deficiency in Ca2+ fluxes is associated with calcium channelopathies such as epilepsy and periodic paralysis. By using resonant terahertz waves, researchers have demonstrated enhanced selectivity and conductance of Ca2+, potentially offering therapeutic interventions in correcting calcium channel deficiencies and inducing apoptosis in tumor cells.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2021)
Article
Nanoscience & Nanotechnology
Meimei Wang, Zhenzhen Zhang, Ning Sun, Baolin Yang, Jihao Mo, Daping Wang, Mingqin Su, Jian Hu, Miaomiao Wang, Lei Wang
Summary: The study found that exposure to Au NPs may have adverse effects on the nervous system, specifically affecting the feeding behavior and olfactory perception of C. elegans. These findings can provide guidance for the use of Au NPs in the medical field.
INTERNATIONAL JOURNAL OF NANOMEDICINE
(2023)
Article
Cell Biology
Wietske E. Tuinte, Eniko Torok, Irene Mahlknecht, Petronel Tuluc, Bernhard E. Flucher, Marta Campiglio
Summary: The adaptor protein STAC3 is essential for the functional expression and excitation-contraction coupling of the skeletal muscle Ca(V)1.1 channel. STAC3 can inhibit the voltage-dependent inactivation (VDI) of Ca(V)1.1 currents but not the calcium-dependent inactivation (CDI). Mutant STAC3-ETLAAA supports Ca(V)1.1 functional expression and EC coupling but accelerates the kinetics of activation and inactivation of Ca(V)1.1 currents. STAC3 is determined to be a crucial determinant for the slow activation kinetics of Ca(V)1.1 currents.
JOURNAL OF CELLULAR PHYSIOLOGY
(2022)
Review
Cardiac & Cardiovascular Systems
Kelvin Wei Zhern Loh, Cong Liu, Tuck Wah Soong, Zhenyu Hu
Summary: Calcium signaling plays a crucial role in essential bodily functions such as muscle contractions and neuronal communications. Voltage-gated calcium channels (VGCCs) are transmembrane protein complexes that allow for the selective entry of calcium ions into cells. The alpha 1 subunit constitutes the main pore-forming subunit and is regulated by various auxiliary subunits. Understanding the role of the beta subunit and its post-translational modifications is essential for developing therapeutic interventions for cardiovascular diseases.
FRONTIERS IN CARDIOVASCULAR MEDICINE
(2023)
Article
Pharmacology & Pharmacy
Liqiong Ding, Ping Jiang, Xinfeng Xu, Wanzhen Lu, Chan Yang, Lin Li, Pingzheng Zhou, Shuwen Liu
Summary: The study identified T-type calcium channel blockers as potential inhibitors of HSV-2 infection, while L-type calcium channel blockers showed no significant effect. Additionally, benidipine exerted antiviral effects by suppressing viral gene expression in the late stage of infection.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2021)
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)
Article
Chemistry, Medicinal
Nace Zidar, Tihomir Tomasic, Danijel Kikelj, Martina Durcik, Jan Tytgat, Steve Peigneur, Marc Rogers, Alexander Haworth, Robert W. Kirby
Summary: Voltage-gated sodium channels (Navs) play a crucial role in neurotransmission and their dysfunction is associated with various neurological disorders. In this study, a new series of aryl and acylsulfonamides were discovered as state-dependent inhibitors of Nav1.3 channels. These compounds displayed strong selective activity against the inactivated state of the Nav1.3 channel, with weaker activity against Nav1.5 and Nav1.7 channels. These findings provide a valuable tool for further evaluation of Nav1.3 channel as a potential drug target.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Pharmacology & Pharmacy
Siddesh Kelkar, Namrata Nailwal, Nirav Yogesh Bhatia, Gaurav Doshi, Sadhana Sathaye, Angel Pavalu Godad
Summary: Inflammation is a mechanism of the body to activate the immune system and prevent bacteria and viruses from causing toxic effects. Voltage-gated ion channel blockers can be an important alternative to deal with the side effects of current drugs.
CURRENT DRUG TARGETS
(2022)
Article
Neurosciences
Daniel M. DuBreuil, Eduardo Javier Lopez Soto, Simon Daste, Remy Meir, Daniel Li, Brian Wainger, Alexander Fleischmann, Diane Lipscombe
Summary: Functional Ca(V)2.2 channels in peripheral axons innervating skin are required for capsaicin-induced heat hypersensitivity, which may be an important therapeutic target for certain forms of chronic pain.
JOURNAL OF NEUROSCIENCE
(2021)
Review
Chemistry, Medicinal
Elisabetta Tosti, Raffaele Boni, Alessandra Gallo
Summary: Voltage-gated ion channels are membrane proteins that generate electrical signals, and their dysfunction can lead to diseases and pain. Conotoxins, bioactive peptides extracted from marine mollusk venom, have therapeutic effects and can relieve pain, but they may also cause pathological states.