Article
Biology
Peter R. Strege, Luke M. Cowan, Constanza Alcaino, Amelia Mazzone, Christopher A. Ahern, Lorin S. Milescu, Gianrico Farrugia, Arthur Beyder
Summary: Shear stress and patch suction can reversibly alter the kinetic properties and maximum current of NaChBac, suggesting it is mechanosensitive. Structural analysis reveals a large displacement of the intracellular gate, supporting the proposed mechanosensitive mechanism.
Review
Pharmacology & Pharmacy
Fritz Markwardt
Summary: Patch clamp investigations help understand the molecular function of single ion channels. The human P2X7 receptor is an ATP-gated ion channel involved in inflammatory and nociceptive reactions. Specific residues and domains play crucial roles in ion channel function.
BIOCHEMICAL PHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Karl Josef Foehr, Michael Rapp, Michael Fauler, Thomas Zimmer, Bettina Jungwirth, David Alexander Christian Messerer
Summary: Aripiprazole has been identified as a potent blocker of the dominant voltage-gated sodium channel of heart muscle. Its interactions with the channel differ depending on the state, with weaker affinity for the resting state and stronger affinity for the inactivated state.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biology
Jan L. Muench, Fabian Paul, Ralf Schmauder, Klaus Benndorf
Summary: Inferring appropriate kinetic models for ion channel gating from ensemble currents is a challenging task due to limited data. We propose a Bayesian filter approach that specifies hidden Markov models for current and fluorescence data, which shows flexibility and superior performance compared to traditional methods. The approach can handle different noise distributions and incorporate orthogonal fluorescence data, providing more accurate parameter estimates.
Article
Cell & Tissue Engineering
Lingyun Li, Huan Zhao, Haohuan Xie, Tasneem Akhtar, Yichuan Yao, Yuan Cai, Kai Dong, Yonghao Gu, Jin Bao, Jutao Chen, Mei Zhang, Kai Zhong, Weiping Xu, Tian Xue
Summary: This study comprehensively characterized the physiological maturation of photoreceptor-like cells derived from hiPSCs in ROs, revealing progressive maturation of ion channels associated with photoreceptor function during differentiation. The inward-outward current ratio was identified as a sensitive indicator of photoreceptor maturity and pathological state, providing a potential biomarker for quality control during RO differentiation.
Article
Developmental Biology
Elis Torrezan-Nitao, Sean G. Brown, Linda Lefievre, Jennifer Morris, Joao Correia, Claire Harper, Stephen Publicover
Summary: Exposure of human sperm to progesterone activates CatSper channels, leading to an increase in intracellular calcium concentration and oscillations. The inhibitor SKF96365 can enhance these oscillations. The presence of bovine serum albumin affects the ability of SKF to induce oscillations.
MOLECULAR HUMAN REPRODUCTION
(2023)
Article
Biology
Crescent L. Combe, Carol M. Upchurch, Carmen C. Canavier, Sonia Gasparini
Summary: A combination of in vitro electrophysiology and modeling identified TRPM4 channels as major drivers of cholinergic modulation of firing rate in rat CA1 pyramidal neurons. Cholinergic agonist carbachol reverses the spike rate adaptation caused by Na-V channel inactivation, resulting in more spikes on the down-ramp compared to the up-ramp. Pharmacological experiments and modeling suggest that TRPM4 channels play a role in the cholinergic shift of firing center of mass through Ca2+-activated nonspecific cation current ICAN.
Article
Pharmacology & Pharmacy
Young-Woo Nam, Meng Cui, Naglaa Salem El-Sayed, Razan Orfali, Misa Nguyen, Grace Yang, Mohammad Asikur Rahman, Judy Lee, Miao Zhang
Summary: The selectivity of CyPPA among K(Ca)2 and K(Ca)3.1 channel subtypes relies on the HA/HB helices.
BRITISH JOURNAL OF PHARMACOLOGY
(2022)
Article
Multidisciplinary Sciences
Bingxue Li, Songling Li, Honglan Zheng, Zhiqiang Yan
Summary: Research shows that in Drosophila larvae, the MET currents in Cho neurons are mediated by two TRPV channels, NAN and IAV, with the C-terminal residues 857 through 990 of IAV regulating the kinetics of MET currents. Additionally, the NompC channel contributes to the adaptation of auditory transduction currents.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2021)
Article
Pharmacology & Pharmacy
Chao Dong, Jiawei Li, Weiguang Ding, Rika Ueda, Xiaolu Xie, Jie Wu, Hiroshi Matsuura, Minoru Horie
Summary: Kv1.5 channels play an important role in atrial fibrillation and certain types of tumors. The symmetrical biphenyl derivative HMQ1611 has been found to effectively block the activity of hKv1.5 channels. We have identified potential binding sites for HMQ1611 within the hKv1.5 channel and demonstrated the voltage and time-dependent inhibitory effects of HMQ1611 on hKv1.5 currents.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Valeria Vasileva, Elena Morachevskaya, Anastasia Sudarikova, Yuri Negulyaev, Vladislav Chubinskiy-Nadezhdin
Summary: Yoda1, a synthetic Piezo1 agonist, has been shown to effectively stimulate Piezo1 channels in artificial systems, but its activating effect on native Piezo1 channels in living cell membranes remains unclear.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Pharmacology & Pharmacy
Miaomaio Liu, Yakun Yang, Muqing Zhang, Yucong Xue, Bin Zheng, Yuanyuan Zhang, Yu Liu, Xi Chu, Zhenqing Sun, Xue Han
Summary: The study revealed that 8-Gin is the most potent inhibitor of hERG K+ channels among gingerol components, offering a new approach for understanding and treating cancer.
JOURNAL OF PHARMACY AND PHARMACOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Anna N. Bukiya, Alex M. Dopico
Summary: The study shows that a high-CLR diet can protect cerebral arteries from alcohol-induced constriction by antagonizing the inhibition of BK channels and that this protection is dependent on cell integrity and a PKC-dependent mechanism.
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR AND CELL BIOLOGY OF LIPIDS
(2021)
Review
Pharmacology & Pharmacy
Shirin Ahmadi, Melisa Benard-Valle, Kim Boddum, Fernanda C. Cardoso, Glenn F. King, Andreas Hougaard Laustsen, Anne Ljungars
Summary: Ion channels are crucial for various physiological processes. Venomous creatures exploit ion channels by producing toxins that target them, leading to dysregulation which can cause severe complications in humans. However, the discovery of selective venom toxins has contributed to the development of drugs for envenoming and ion channel-related diseases.
FRONTIERS IN PHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Kaori Takahashi, Kentaro Araki, Hideo Miyamoto, Rikimaru Shirakawa, Takashi Yoshida, Minoru Wakamori
Summary: The TRPV1 channel plays a crucial role in pain sensation, being regulated by capsaicin and protons, showing strong voltage dependency, and having specific activation characteristics.
FRONTIERS IN PHARMACOLOGY
(2021)