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https://www.readbyqxmd.com/read/29768917/how-native-and-non-native-cations-bind-and-modulate-the-properties-of-gtp-atp
#1
Todor Dudev, Cedric Grauffel, Shang-Te Danny Hsu, Carmay Lim
Adenosine triphosphate (ATP) and guanosine triphosphate (GTP) exist in physiological solution mostly bound to cations. Interestingly, their cellular Mg2+ -bound forms have been shown to bind Li+ , a first-line drug for bipolar disorder. However, solution structures of NTP/NDP (N = A or G) bound to Li+ and/or Mg2+ have not been solved, thus precluding knowledge of how the native Mg2+ -bound cofactor conformation changes upon binding non-native Li+ and/or switching its environment from aqueous solution to proteins...
May 16, 2018: Journal of Chemical Theory and Computation
https://www.readbyqxmd.com/read/29766811/p2x7-receptor-associated-programmed-cell-death-in-the-pathophysiology-of-hemorrhagic-stroke
#2
Hengli Zhao, Yujie Chen, Hua Feng
Hemorrhagic stroke is a life-threatening disease characterized by a sudden rupture of cerebral blood vessels, and cell death is widely believed to occur after exposure to blood metabolites or subsequently damaged cells. Recently, programmed cell death, such as apoptosis, autophagy, necroptosis, pyroptosis, and ferroptosis, has been demonstrated to play crucial roles in the pathophysiology of stroke. However, the detailed mechanisms of these novel kinds of cell death are still unclear. The P2X7 receptor, previously known for its cytotoxic activity, is an ATP-gated, non-selective cation channel that belongs to the family of ionotropic P2X receptors...
May 15, 2018: Current Neuropharmacology
https://www.readbyqxmd.com/read/29731674/electrophysiological-evidence-for-functional-astrocytic-p2x-3-receptors-in-the-mouse-trigeminal-caudal-nucleus
#3
Jaekwang Lee, Jin Young Bae, C Justin Lee, Yong Chul Bae
Recently, we reported that astrocytes in the trigeminal caudal nucleus (Vc) of the brain stem express a purinergic receptor P2X3 , which is involved in the craniofacial pathologic pain. Although we observed protein expression of P2X3 receptors (P2X3 Rs) in the astrocyte of the Vc, it is still unclear that astrocyte has functional P2X3 Rs in Vc. To address this issue, we recorded asrtocytic P2X3 Rs by using whole cell voltage-clamp recording in the Vc of the GFAP-GFP mice, which was used as a guide to astrocytes with green fluorescence...
April 2018: Experimental Neurobiology
https://www.readbyqxmd.com/read/29729039/effects-of-calcium-and-sodium-on-atp-induced-vasopressin-release-from-rat-isolated-neurohypophysial-terminals
#4
E E Custer, T K Knott, S Ortiz-Miranda, J R Lemos
ATP-receptors (P2X2, P2X3, P2X4 & P2X7) are found in neurohypophysial terminals (NHT). These purinergic receptor subtypes are known to be cation selective. Here we confirm that both sodium (Na+ ) and calcium (Ca2+ ) are permeable through these NHT purinergic receptors, but to varying degrees (91% vs. 9%, respectively). Furthermore, extracellular calcium inhibits the ATP-current magnitude. Thus, the objective of this study was to determine the effects of extracellular Na+ vs. Ca2+ on ATP-induced vasopressin (AVP) release from populations of rat isolated NHT...
May 4, 2018: Journal of Neuroendocrinology
https://www.readbyqxmd.com/read/29713181/minodronate-for-the-treatment-of-osteoporosis
#5
REVIEW
Tsuyoshi Ohishi, Yukihiro Matsuyama
Minodronate is a third-generation bisphosphonate that was developed and approved for clinical use in osteoporosis therapy in Japan. The mechanism of action for suppressing bone resorption is the inhibition of farnesyl pyrophosphate synthase, a key enzyme in the mevalonic acid metabolic pathway of osteoclasts, to induce apoptosis of the cells. Minodronate is the strongest inhibitor of bone resorption among the currently available oral bisphosphonates. Large randomized, placebo-controlled, double-blind clinical trials have revealed an increase in bone mineral density of both the lumbar spine and femoral neck over 3 years of daily minodronate therapy and risk reduction in vertebral fractures over 2 years of therapy...
2018: Therapeutics and Clinical Risk Management
https://www.readbyqxmd.com/read/29700413/identification-of-the-allosteric-p2x-7-receptor-antagonist-11-c-smw139-as-a-pet-tracer-of-microglial-activation
#6
Bieneke Janssen, Danielle J Vugts, Shane M Wilkinson, Dieter Ory, Sylvie Chalon, Jeroen J M Hoozemans, Robert C Schuit, Wissam Beaino, Esther J M Kooijman, Johan van den Hoek, Mansoor Chishty, Aurélie Doméné, Anke Van der Perren, Alessandro Villa, Adriana Maggi, Ger T Molenaar, Uta Funke, Rostislav V Shevchenko, Veerle Baekelandt, Guy Bormans, Adriaan A Lammertsma, Michael Kassiou, Albert D Windhorst
The P2X7 receptor plays a significant role in microglial activation, and as a potential drug target, the P2X7 receptor is also an interesting target in positron emission tomography. The current study aimed at the development and evaluation of a potent tracer targeting the P2X7 receptor, to which end four adamantanyl benzamide analogues with high affinity for the human P2X7 receptor were labelled with carbon-11. All four analogues could be obtained in excellent radiochemical yield and high radiochemical purity and molar activity, and all analogues entered the rat brain...
April 26, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29676177/acetylcholine-induced-ciliary-beat-of-the-human-nasal-mucosa-is-regulated-by-the-pannexin-1-channel-and-purinergic-p2x-receptor
#7
Ba H Do, Toyoaki Ohbuchi, Tetsuro Wakasugi, Hiroki Koizumi, Mitsuru Yokoyama, Nobusuke Hohchi, Hideaki Suzuki
Background Airway mucociliary transport is an important function for the clearance of inhaled foreign particulates in the respiratory tract. The present study aimed at investigating the regulatory mechanism of acetylcholine (Ach)-induced ciliary beat of the human nasal mucosa in ex vivo. Methods The inferior turbinate mucosa was collected from patients with chronic hypertrophic rhinitis during endoscopic surgery. The mucosa was cut into thin strips, and ciliary movement was observed under a phase-contrast light microscope with a high-speed digital video camera...
January 1, 2018: American Journal of Rhinology & Allergy
https://www.readbyqxmd.com/read/29674445/druggable-negative-allosteric-site-of-p2x3-receptors
#8
Jin Wang, Yao Wang, Wen-Wen Cui, Yichen Huang, Yang Yang, Yan Liu, Wen-Shan Zhao, Xiao-Yang Cheng, Wang-Sheng Sun, Peng Cao, Michael X Zhu, Rui Wang, Motoyuki Hattori, Ye Yu
Allosteric modulation provides exciting opportunities for drug discovery of enzymes, ion channels, and G protein-coupled receptors. As cation channels gated by extracellular ATP, P2X receptors have attracted wide attention as new drug targets. Although small molecules targeting P2X receptors have entered into clinical trials for rheumatoid arthritis, cough, and pain, negative allosteric modulation of these receptors remains largely unexplored. Here, combining X-ray crystallography, computational modeling, and functional studies of channel mutants, we identified a negative allosteric site on P2X3 receptors, fostered by the left flipper (LF), lower body (LB), and dorsal fin (DF) domains...
April 19, 2018: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/29619754/the-involvement-of-purinergic-signalling-in-obesity
#9
REVIEW
Geoffrey Burnstock, Daniela Gentile
Obesity is a growing worldwide health problem, with an alarming increasing prevalence in developed countries, caused by a dysregulation of energy balance. Currently, no wholly successful pharmacological treatments are available for obesity and related adverse consequences. In recent years, hints obtained from several experimental animal models support the notion that purinergic signalling, acting through ATP-gated ion channels (P2X), G protein-coupled receptors (P2Y) and adenosine receptors (P1), is involved in obesity, both at peripheral and central levels...
April 4, 2018: Purinergic Signalling
https://www.readbyqxmd.com/read/29616195/the-atp-p2x-7-signaling-axis-is-an-essential-sentinel-for-intracellular-clostridium-difficile-pathogen-induced-inflammasome-activation
#10
Ya-Hui Liu, Yung-Chi Chang, Liang-Kuei Chen, Po-An Su, Wen-Chien Ko, Yau-Sheng Tsai, Yi-Hsuan Chen, Hsin-Chih Lai, Cheng-Yeu Wu, Yuan-Pin Hung, Pei-Jane Tsai
Clostridium difficile infection (CDI) is the leading cause of nosocomial infection in hospitalized patients receiving long-term antibiotic treatment. An excessive host inflammatory response is believed to be the major mechanism underlying the pathogenesis of C. difficile infection, and various proinflammatory cytokines such as IL-1β are detected in patients with C. difficile infection. IL-1β is known to be processed by caspase-1, a cysteine protease that is regulated by a protein complex called the inflammasome, which leads to a specialized form of cell death called pyroptosis...
2018: Frontiers in Cellular and Infection Microbiology
https://www.readbyqxmd.com/read/29615870/atp-and-odor-mixture-activate-trpm5-expressing-microvillous-cells-and-potentially-induce-acetylcholine-release-to-enhance-supporting-cell-endocytosis-in-mouse-main-olfactory-epithelium
#11
Ziying Fu, Tatsuya Ogura, Wangmei Luo, Weihong Lin
The main olfactory epithelium (MOE) functions to detect odor molecules, provide an epithelial surface barrier, and remove xenobiotics from inhaled air. Mechanisms coordinating the activities of different cell types within the MOE to maintain these functions are poorly understood. Previously, we showed that superficially located microvillous cells (MCs) in the MOE expressing transient receptor potential channel M5 (TRPM5) are cholinergic and chemoresponsive and that they play an important role in maintaining odor responses and olfactory-guided behavior under challenging chemical environment...
2018: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29611030/exploring-conformational-states-and-helical-packings-in-the-p2x-receptor-transmembrane-domain-by-molecular-dynamics-simulation
#12
Guo-Hua Li
The P2X receptor is a trimeric transmembrane protein that acts as an ATP-gated ion channel. Its transmembrane domain (TMD) contains only six helices and three of them, the M2 helices, line the ion conduction pathway. Here, using molecular dynamics simulation, I identify four conformational states of the TMD that are associated with four types of packing between M2 helices. Packing in the extracellular half of the M2 helix produces closed conformations, while packing in the intracellular half produces both open and closed conformations...
April 2, 2018: Journal of Biological Physics
https://www.readbyqxmd.com/read/29596152/upregulation-of-p2x2-and-p2x3-receptors-in-rats-with-hyperalgesia-induced-by-heroin-withdrawal
#13
Changlong Leng, Lin Chen, Xiaokang Gong, Baomiao Ma, Weimin Gan, Yuanren Si, Huaqiao Xiao, Chaoying Li
Drug dependence and withdrawal syndrome induced by abrupt cessation of opioid administration remain a severe obstacle in the clinical treatment of chronic pain and opioid drug addiction. One of the key symptoms during opioid withdrawal is hyperalgesia. The mechanism of opioid withdrawal-induced hyperalgesia remains unclear. P2X2 and P2X3 receptors, members of P2X receptor subunits, act as the integrator of multiple forms of noxious stimuli and play an important role in nociception transduction of chronic neuropathic and inflammatory pain...
March 28, 2018: Neuroreport
https://www.readbyqxmd.com/read/29590590/modulation-of-deg-enacs-by-amphiphiles-suggests-sensitivity-to-membrane-alterations
#14
Axel Schmidt, Rick J Alsop, Rahul Rimal, Pia Lenzig, Sylvia Joussen, Natalie N Gervasi, Adree Khondker, Stefan Gründer, Maikel C Rheinstädter, Dominik Wiemuth
The bile acid-sensitive ion channel is activated by amphiphilic substances such as bile acids or artificial detergents via membrane alterations; however, the mechanism of membrane sensitivity of the bile acid-sensitive ion channel is not known. It has also not been systematically investigated whether other members of the degenerin/epithelial Na+ channel (DEG/ENaC) gene family are affected by amphiphilic compounds. Here, we show that DEG/ENaCs ASIC1a, ASIC3, ENaC, and the purinergic receptor P2X2 are modulated by a large number of different, structurally unrelated amphiphilic substances, namely the detergents N-lauroylsarcosine, Triton X-100, and β-octylglucoside; the fenamate flufenamic acid; the antipsychotic drug chlorpromazine; the natural phenol resveratrol; the chili pepper compound capsaicin; the loop diuretic furosemide; and the antiarrythmic agent verapamil...
March 27, 2018: Biophysical Journal
https://www.readbyqxmd.com/read/29581742/methylene-blue-relieves-the-development-of-osteoarthritis-by-upregulating-lncrna-meg3
#15
Xinyi Li, Chaoliang Tang, Jin Wang, Peipei Guo, Chengyao Wang, Yanlin Wang, Zongze Zhang, Huisheng Wu
Methylene blue (MB) is a long-term inhibitor of peripheral nerve axons, thereby alleviating or permanently eliminating pain. However, it remains unknown whether MB is safe and effective method of treating osteoarthritis (OA). MB was injected into the knee joints of rabbits and they were monitored for any histological structural changes. The results revealed no evident changes in the histological structure of the normal knee joint following injection of 1 mg/kg MB at 1, 4, 8 and 24 weeks post-injection. Compared with the vehicle control, MB treatment significantly enhanced the weight distribution and significantly decreased the swelling ratio of the rabbits...
April 2018: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/29572578/crucial-role-of-p2x-7-receptor-for-effector-t-cell-activation-in-experimental-autoimmune-uveitis
#16
Atsunobu Takeda, Hisakata Yamada, Eiichi Hasegawa, Mitsuru Arima, Shoji Notomi, Sayaka Myojin, Takeru Yoshimura, Toshio Hisatomi, Hiroshi Enaida, Ryoji Yanai, Kazuhiro Kimura, Tatsuro Ishibashi, Koh-Hei Sonoda
PURPOSE: To investigate the roles of P2X7 receptors (P2RX7) in the pathogenesis of experimental autoimmune uveoretinitis (EAU). STUDY DESIGN: Experimental. METHODS: Either wild-type (P2rx7+/+ ) or P2rx7-deficient (P2rx7-∕- ) mice were immunized with interphotoreceptor retinoid-binding protein (IRBP) peptide 1-20. Severity of EAU was evaluated clinically and histopathologically. The induction of IRBP-specific proliferation and cytokines in draining lymph nodes was assessed by enzyme-linked immunosorbent assays (ELISA)...
March 23, 2018: Japanese Journal of Ophthalmology
https://www.readbyqxmd.com/read/29570626/angiotensin-ii-induced-mesangial-cell-damaged-is-preceded-by-cell-membrane-permeabilization-due-to-upregulation-of-non-selective-channels
#17
Gonzalo I Gómez, Paola Fernández, Victoria Velarde, Juan C Sáez
Connexin43 (Cx43), pannexin1 (Panx1) and P2X₇ receptor (P2X₇R) are expressed in kidneys and are known to constitute a feedforward mechanism leading to inflammation in other tissues. However, the possible functional relationship between these membrane channels and their role in damaged renal cells remain unknown. In the present work, we found that MES-13 cells, from a cell line derived from mesangial cells, stimulated with angiotensin II (AngII) developed oxidative stress (OS, thiobarbituric acid reactive species (TBARS) and generated pro-inflammatory cytokines (ELISA; IL-1β and TNF-α)...
March 23, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29563872/the-metabotropic-purinergic-p2y-receptor-family-as-novel-drug-target-in-epilepsy
#18
REVIEW
Mariana Alves, Edward Beamer, Tobias Engel
Epilepsy encompasses a heterogeneous group of neurological syndromes which are characterized by recurrent seizures affecting over 60 million people worldwide. Current anti-epileptic drugs (AEDs) are mainly designed to target ion channels and/or GABA or glutamate receptors. Despite recent advances in drug development, however, pharmacoresistance in epilepsy remains as high as 30%, suggesting the need for the development of new AEDs with a non-classical mechanism of action. Neuroinflammation is increasingly recognized as one of the key players in seizure generation and in the maintenance of the epileptic phenotype...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29561954/nitric-oxide-modulates-atp-evoked-currents-in-mouse-leydig-cells
#19
J L de Deus, A L A Dagostin, W A Varanda
Testosterone synthesis within Leydig cells is a calcium-dependent process. Intracellular calcium levels are regulated by different processes including ATP-activated P2X purinergic receptors, T-type Ca2+ channels modulated by the luteinizing hormone, and intracellular calcium storages recruited by a calcium-induced calcium release mechanism. On the other hand, nitric oxide (NO) is reported to have an inhibitory role in testosterone production. Based on these observations, we investigated the interaction between the purinergic and nitrergic systems in Leydig cells of adult mice...
March 15, 2018: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
https://www.readbyqxmd.com/read/29546069/involvement-of-p2x-7-receptor-in-proliferation-and-migration-of-human-glioma-cells
#20
Zhenhua Ji, Yuting Xie, Yu Guan, Yujian Zhang, Kin-Sang Cho, Min Ji, Yongping You
Previous studies have demonstrated that activation of P2X7 receptors (P2X7 R) results in the proliferation and migration of some types of tumor. Here, we asked whether and how the activated P2X7 R contribute to proliferation and migration of human glioma cells. Results showed that the number of P2X7 R positive cells was increasing with grade of tumor. In U87 and U251 human glioma cell lines, both expressed P2X7 R and the expression was enhanced by 3'-O-(4-benzoylbenzoyl) ATP (BzATP), the agonist of P2X7 R, and siRNA...
2018: BioMed Research International
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