keyword
MENU ▼
Read by QxMD icon Read
search

Ion channels, cell calcium, pharmacology,

keyword
https://www.readbyqxmd.com/read/28130783/the-trpm7-channel-kinase-regulates-store-operated-calcium-entry
#1
Malika Faouzi, Tatiana Kilch, F David Horgen, Andrea Fleig, Reinhold Penner
The Transient receptor potential melastatin 7 (TRPM7) is a protein that combines an ion channel with an intrinsic kinase domain, enabling it to modulate cellular functions either by conducting ions through the pore or by phosphorylating downstream proteins through its kinase domain. In this study we present Store-Operated Calcium Entry (SOCE) as a novel target of TRPM7 kinase activity. TRPM7-deficient chicken DT40 B lymphocytes exhibit a strongly impaired SOCE compared to wild type cells due to reduced Calcium Release Activated Calcium (CRAC) currents and independent of potassium channel regulation, membrane potential changes or changes in cell-cycle distribution...
January 28, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28121009/molecular-biophysical-and-pharmacological-properties-of-calcium-activated-chloride-channels
#2
REVIEW
Mohammad Amin Kamaleddin
Calcium-activated chloride channels (CaCCs) are a family of anionic transmembrane ion channels. They are mainly responsible for the movement of Cl(-) and other anions across the biological membranes and are widely expressed in different tissues. Due to the fact that Cl(-) flow into or out of the cell plays a crucial role in hyperpolarizing or depolarizing the cells, respectively, the impact of intracellular Ca(2+) concentration on these channels is attracting a lot of attentions. After summarizing the molecular, biophysical, and pharmacological properties of CaCCs, the role of CaCCs in normal cellular functions will be discussed, and I will emphasize how dysregulation of CaCCs in pathological conditions can account for different diseases...
January 25, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28116717/measuring-t-type-calcium-channel-currents-in-isolated-vascular-smooth-muscle-cells
#3
Ivana Y Kuo, Caryl E Hill
Patch clamp electrophysiology is a powerful tool that has been important in isolating and characterizing the ion channels that govern cellular excitability under physiological and pathophysiological conditions. The ability to enzymatically dissociate blood vessels and acutely isolate vascular smooth muscle cells has enabled the application of patch clamp electrophysiology to the identification of diverse voltage dependent ion channels that ultimately control vasoconstriction and vasodilation. Since intraluminal pressure results in depolarization of vascular smooth muscle, the channels that control the voltage dependent influx of extracellular calcium are of particular interest...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/28077439/the-functional-expression-of-transient-receptor-potential-channels-in-the-mouse-endometrium
#4
Katrien De Clercq, Charlotte Van den Eynde, Aurélie Hennes, Rieta Van Bree, Thomas Voets, Joris Vriens
STUDY QUESTION: Does mouse endometrial epithelial cells and stromal cells have a similar transient receptor potential (TRP)-channel expression profile and to that found in the human endometrium? SUMMARY ANSWER: Mouse endometrial epithelial and stromal cells have a distinct TRP channel expression profile analogous to what has been found in human endometrium, and hence suggests the mouse a good model to investigate the role of TRP channels in reproduction. WHAT IS KNOWN ALREADY: An optimal intercellular communication between epithelial and stromal endometrial cells is crucial for successful reproduction...
January 6, 2017: Human Reproduction
https://www.readbyqxmd.com/read/27988421/voltage-gated-sodium-channels-viewed-through-a-structural-biology-lens
#5
REVIEW
Thomas Clairfeuille, Hui Xu, Christopher M Koth, Jian Payandeh
Voltage-gated sodium (Nav) channels initiate and propagate action potentials in excitable cells, and are frequently dysregulated or mutated in human disease. Despite decades of intense physiological and biophysical research, eukaryotic Nav channels have so far eluded high-resolution structure determination because of their biochemical complexity. Recently, simpler bacterial voltage-gated sodium (BacNav) channels have provided templates to understand the structural basis of voltage-dependent activation, inactivation, ion selectivity, and drug block in eukaryotic Nav and related voltage-gated calcium (Cav) channels...
December 15, 2016: Current Opinion in Structural Biology
https://www.readbyqxmd.com/read/27979597/inhibition-of-trpc6-channels-ameliorates-renal%C3%A2-fibrosis-and-contributes-to-renal-protection%C3%A2-by%C3%A2-soluble-klotho
#6
Yueh-Lin Wu, Jian Xie, Sung-Wan An, Noelynn Oliver, Nestor X Barrezueta, Mei-Hsiang Lin, Lutz Birnbaumer, Chou-Long Huang
Fibrosis is an exaggerated form of tissue repair that occurs with serious damage or repetitive injury and ultimately leads to organ failure due to the excessive scarring. Increased calcium ion entry through the TRPC6 channel has been associated with the pathogenesis of heart and glomerular diseases, but its role in renal interstitial fibrosis is unknown. We studied this by deletion of Trpc6 in mice and found it decreased unilateral ureteral obstruction-induced interstitial fibrosis and blunted increased mRNA expression of fibrosis-related genes in the ureteral obstructed kidney relative to that in the kidney of wild-type mice...
December 12, 2016: Kidney International
https://www.readbyqxmd.com/read/27901061/inter-individual-variability-and-modeling-of-electrical-activity-a-possible-new-approach-to-explore-cardiac-safety
#7
Jean-Yves Le Guennec, Jérôme Thireau, Aude Ouillé, Julien Roussel, Jérôme Roy, Serge Richard, Sylvain Richard, Eric Martel, Pascal Champéroux
Safety pharmacology aims to predict rare side effects of new drugs. We explored whether rare pro-arrhythmic effects could be linked to the variability of the effects of these drugs on ion currents and whether taking into consideration this variability in computational models could help to better detect and predict cardiac side effects. For this purpose, we evaluated how intra- and inter-individual variability influences the effect of hERG inhibition on both the action potential duration and the occurrence of arrhythmias...
November 30, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27891582/versatile-roles-of-intracellularly-located-trpv1-channel
#8
REVIEW
Rui Zhao, Suk Ying Tsang
The ubiquitous expression in many organs throughout the body and the ability to respond to a wide variety of physical and chemical stimuli have brought transient receptor potential (TRP) channels to the vanguards of our sensory systems. TRP vanilloid-1 (TRPV1) is the founding member of the TRPV subfamily. TRPV1 can be activated by noxious heat, protons and vanilloids. Previous studies have shown that TRPV1 is located on the plasma membrane, serving to non-selectively permeate calcium ion from the extracellular region to the cytoplasm...
November 27, 2016: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/27856238/evaluation-of-known-and-novel-inhibitors-of-orai1-mediated-store-operated-ca-2-entry-in-mda-mb-231-breast-cancer-cells-using-a-fluorescence-imaging-plate-reader-assay
#9
Iman Azimi, Jack U Flanagan, Ralph J Stevenson, Marco Inserra, Irina Vetter, Gregory R Monteith, William A Denny
The Orai1 Ca(2+) permeable ion channel is an important component of store operated Ca(2+) entry (SOCE) in cells. It's over-expression in basal molecular subtype breast cancers has been linked with poor prognosis, making it a potential target for drug development. We pharmacologically characterised a number of reported inhibitors of SOCE in MDA-MB-231 breast cancer cells using a convenient Fluorescence Imaging Plate Reader (FLIPR) assay, and show that the rank order of their potencies in this assay is the same as those reported in a wide range of published assays...
January 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27756874/mechanism-of-melanoma-cells-selective-apoptosis-induced-by-a-photoactive-nadph-analogue
#10
Florian Rouaud, Jean-Luc Boucher, Anny Slama-Schwok, Stéphane Rocchi
Melanoma is one of the most lethal cancers when it reaches a metastatic stage. Despite the spectacular achievements of targeted therapies (BRAF inhibitors) or immuno-therapies (anti-CTLA4 or anti-PD1), most patients with melanoma will need additional treatments. Here we used a photoactive NADPH analogue called NS1 to induce cell death by inhibition of NADPH oxidases NOX in melanoma cells, including melanoma cells isolated from patients. In contrast, healthy melanocytes growth was unaffected by NS1 treatment...
October 14, 2016: Oncotarget
https://www.readbyqxmd.com/read/27738742/n-acetyl-l-cysteine-inhibits-sulfur-mustard-induced-and-trpa1-dependent-calcium-influx
#11
Bernhard Stenger, Tanja Popp, Harald John, Markus Siegert, Amelie Tsoutsoulopoulos, Annette Schmidt, Harald Mückter, Thomas Gudermann, Horst Thiermann, Dirk Steinritz
Transient receptor potential family channels (TRPs) have been identified as relevant targets in many pharmacological as well as toxicological studies. TRP channels are ubiquitously expressed in different tissues and act among others as sensors for different external stimuli, such as mechanical stress or noxious impacts. Recent studies suggest that one member of this family, the transient receptor potential ankyrin 1 cation channel (TRPA1), is involved in pain, itch, and various diseases, suggesting TRPA1 as a potential therapeutic target...
October 13, 2016: Archives of Toxicology
https://www.readbyqxmd.com/read/27681336/trpm7-like-channels-are-functionally-expressed-in-oocytes-and-modulate-post-fertilization-embryo-development-in-mouse
#12
Ingrid Carvacho, Goli Ardestani, Hoi Chang Lee, Kaitlyn McGarvey, Rafael A Fissore, Karin Lykke-Hartmann
The Transient Receptor Potential (TRP) channels are a family of cationic ion channels widely distributed in mammalian tissues. In general, the global genetic disruption of individual TRP channels result in phenotypes associated with impairment of a particular tissue and/or organ function. An exception is the genetic ablation of the TRP channel TRPM7, which results in early embryonic lethality. Nevertheless, the function of TRPM7 in oocytes, eggs and pre-implantation embryos remains unknown. Here, we described an outward rectifying non-selective current mediated by a TRP ion channel in immature oocytes (germinal vesicle stage), matured oocytes (metaphase II eggs) and 2-cell stage embryos...
September 29, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27659111/selected-grin2a-mutations-in-melanoma-cause-oncogenic-effects-that-can-be-modulated-by-extracellular-glutamate
#13
Stacey Ann N D'mello, Wayne R Joseph, Taryn N Green, Euphemia Y Leung, Matthew J During, Graeme J Finlay, Bruce C Baguley, Maggie L Kalev-Zylinska
GRIN2A mutations are frequent in melanoma tumours but their role in disease is not well understood. GRIN2A encodes a modulatory subunit of the N-methyl-d-aspartate receptor (NMDAR). We hypothesized that certain GRIN2A mutations increase NMDAR function and support melanoma growth through oncogenic effects. This hypothesis was tested using 19 low-passage melanoma cell lines, four of which carried novel missense mutations in GRIN2A that we previously reported. We examined NMDAR expression, function of a calcium ion (Ca(2+)) channel and its contribution to cell growth using pharmacological modulators; findings were correlated with the presence or absence of GRIN2A mutations...
September 14, 2016: Cell Calcium
https://www.readbyqxmd.com/read/27535905/dysregulation-of-neuronal-ca2-channel-linked-to-heightened-sympathetic-phenotype-in-prohypertensive-states
#14
Hege E Larsen, Emma N Bardsley, Konstantinos Lefkimmiatis, David J Paterson
UNLABELLED: Hypertension is associated with impaired nitric oxide (NO)-cyclic nucleotide (CN)-coupled intracellular calcium (Ca(2+)) homeostasis that enhances cardiac sympathetic neurotransmission. Because neuronal membrane Ca(2+) currents are reduced by NO-activated S-nitrosylation, we tested whether CNs affect membrane channel conductance directly in neurons isolated from the stellate ganglia of spontaneously hypertensive rats (SHRs) and their normotensive controls. Using voltage-clamp and cAMP-protein kinase A (PKA) FRET sensors, we hypothesized that impaired CN regulation provides a direct link to abnormal signaling of neuronal calcium channels in the SHR and that targeting cGMP can restore the channel phenotype...
August 17, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27503387/identification-of-drug-drug-interactions-in-vitro-a-case-study-evaluating-the-effects-of-sofosbuvir-and-amiodarone-on-hipsc-derived-cardiomyocytes
#15
Daniel C Millard, Christopher J Strock, Coby B Carlson, Natsuyo Aoyama, Krisztina Juhasz, Tom A Goetze, Sonja Stoelzle-Feix, Nadine Becker, Niels Fertig, Craig T January, Blake D Anson, James D Ross
Drug-drug interactions pose a difficult drug safety problem, given the increasing number of individuals taking multiple medications and the relative complexity of assessing the potential for interactions. For example, sofosbuvir-based drug treatments have significantly advanced care for hepatitis C virus-infected patients, yet recent reports suggest interactions with amiodarone may cause severe symptomatic bradycardia and thus limit an otherwise extremely effective treatment. Here, we evaluated the ability of human induced pluripotent stem cell derived cardiomyocytes (hiPSC-CMs) to recapitulate the interaction between sofosbuvir and amiodarone in vitro, and more generally assessed the feasibility of hiPSC-CMs as a model system for drug-drug interactions...
August 7, 2016: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/27452932/characterization-of-ion-channels-on-subesophageal-ganglion-neurons-from-chinese-tarantula-ornithoctonus-huwena-exploring-the-myth-of-the-spider-insensitive-to-its-venom
#16
Meichun Deng, Zhaotun Hu, Tianfu Cai, Kai Liu, Wenfang Wu, Xuan Luo, Liping Jiang, Meichi Wang, Jing Yang, Yucheng Xiao, Songping Liang
Chinese tarantula Ornithoctonus huwena is one of the most venomous spiders distributing in the hilly areas of southern China. In this study, using whole-cell patch-clamp technique we investigated electrophysiological and pharmacological properties of ion channels from tarantula subesophageal ganglion neurons. It was found that the neurons express multiple kinds of ion channels at least including voltage-gated calcium channels, TTX-sensitive sodium channels and two types of potassium channels. They exhibit pharmacological properties similar to mammalian subtypes...
September 15, 2016: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/27418672/calcium-channels-and-associated-receptors-in-malignant-brain-tumor-therapy
#17
Fernanda B Morrone, Marina P Gehring, Natália F Nicoletti
Malignant brain tumors are highly lethal and aggressive. Despite recent advances in the current therapies, which include the combination of surgery and radio/chemotherapy, the average survival rate remains poor. Altered regulation of ion channels is part of the neoplastic transformation, which suggests that ion channels are involved in cancer. Distinct classes of calcium-permeable channels are abnormally expressed in cancer and are likely involved in the alterations underlying malignant growth. Specifically, cytosolic Ca(2+) activity plays an important role in the regulation of cell proliferation, and Ca(2+) signaling is altered in proliferating tumor cells...
September 2016: Molecular Pharmacology
https://www.readbyqxmd.com/read/27381826/augmentation-of-poly-adp-ribose-polymerase-dependent-neuronal-cell-death-by-acidosis
#18
Jian Zhang, Xiaoling Li, Herman Kwansa, Yun Tai Kim, Liye Yi, Gina Hong, Shaida A Andrabi, Valina L Dawson, Ted M Dawson, Raymond C Koehler, Zeng-Jin Yang
Tissue acidosis is a key component of cerebral ischemic injury, but its influence on cell death signaling pathways is not well defined. One such pathway is parthanatos, in which oxidative damage to DNA results in activation of poly(ADP-ribose) polymerase and generation of poly(ADP-ribose) polymers that trigger release of mitochondrial apoptosis-inducing factor. In primary neuronal cultures, we first investigated whether acidosis per sé is capable of augmenting parthanatos signaling initiated pharmacologically with the DNA alkylating agent, N-methyl-N'-nitro-N-nitrosoguanidine...
July 5, 2016: Journal of Cerebral Blood Flow and Metabolism
https://www.readbyqxmd.com/read/27342111/cav-channels-and-cancer-canonical-functions-indicate-benefits-of-repurposed-drugs-as-cancer-therapeutics
#19
REVIEW
Paul J Buchanan, Karen D McCloskey
The importance of ion channels in the hallmarks of many cancers is increasingly recognised. This article reviews current knowledge of the expression of members of the voltage-gated calcium channel family (CaV) in cancer at the gene and protein level and discusses their potential functional roles. The ten members of the CaV channel family are classified according to expression of their pore-forming α-subunit; moreover, co-expression of accessory α2δ, β and γ confers a spectrum of biophysical characteristics including voltage dependence of activation and inactivation, current amplitude and activation/inactivation kinetics...
October 2016: European Biophysics Journal: EBJ
https://www.readbyqxmd.com/read/27325418/the-trpa1-ion-channel-is-expressed-in-cd4-t-cells-and-restrains-t-cell-mediated-colitis-through-inhibition-of-trpv1
#20
Samuel Bertin, Yukari Aoki-Nonaka, Jihyung Lee, Petrus R de Jong, Peter Kim, Tiffany Han, Timothy Yu, Keith To, Naoki Takahashi, Brigid S Boland, John T Chang, Samuel B Ho, Scott Herdman, Maripat Corr, Alessandra Franco, Sonia Sharma, Hui Dong, Armen N Akopian, Eyal Raz
OBJECTIVE: Transient receptor potential ankyrin-1 (TRPA1) and transient receptor potential vanilloid-1 (TRPV1) are calcium (Ca(2+))-permeable ion channels mostly known as pain receptors in sensory neurons. However, growing evidence suggests their crucial involvement in the pathogenesis of IBD. We explored the possible contribution of TRPA1 and TRPV1 to T-cell-mediated colitis. DESIGN: We evaluated the role of Trpa1 gene deletion in two models of experimental colitis (ie, interleukin-10 knockout and T-cell-adoptive transfer models)...
June 20, 2016: Gut
keyword
keyword
32058
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"