keyword
MENU ▼
Read by QxMD icon Read
search

HEK

keyword
https://www.readbyqxmd.com/read/29156592/activation-of-trek-1-but-not-trek-2-channel-by-mood-stabilizers
#1
Eun-Jin Kim, Dong Kun Lee, Seong-Geun Hong, Jaehee Han, Dawon Kang
Earlier studies have demonstrated that the tandem pore domain weak inward rectifying K⁺ channel (TWIK)-related K⁺ (TREK)-1 channel is inhibited by antidepressants and is associated with major depression. However, little is known about the effect of mood stabilizers that are commonly used for treatment of bipolar disorder on TREK channels, members of the two-pore domain K⁺ (K2P) channel family. This study sought to investigate the effect of mood stabilizers on TREK-1 and TREK-2 channels. HEK-293A cells were transfected with human TREK-1 or TREK-2 DNA...
November 19, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29156097/4-aminopyridine-a-pan-kv-channel-inhibitor-that-enhances-kv7-4-currents-and-inhibits-noradrenaline-mediated-contraction-of-rat-mesenteric-small-arteries
#2
Makhala M Khammy, Sukhan Kim, Bo H Bentzen, Soojung Lee, Inyeoung Choi, Christian Aalkjaer, Thomas A Jepps
BACKGROUND AND PURPOSE: Kv7.4 and Kv7.5 channels are regulators of vascular tone. 4-aminopyridine (4-AP) is considered a broad inhibitor of voltage-gated potassium (KV ) channels, with little inhibitory effect on Kv7 family members at millimolar concentrations. However, the effect of 4-AP on Kv7 channels has not been systematically studied. The aim of this study was to investigate the pharmacological activity of 4-AP on Kv7.4 and Kv7.5 channels and characterise the effect of 4-AP on rat resistance arteries...
November 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29154833/photo-based-pdt-ptt-dual-model-killing-and-imaging-of-cancer-cells-using-phycocyanin-polypyrrole-nanoparticles
#3
Subramaniyan Bharathiraja, Panchanathan Manivasagan, Madhappan Santha Moorthy, Nhat Quang Bui, Bian Jang, Thi Tuong Vy Phan, Won-Kyo Jung, Young-Mok Kim, Kang Dae Lee, Junghwan Oh
Photodynamic therapy (PDT) and photothermal therapy (PTT) using nanoparticles have gained significant attention for its therapeutic effect for cancer treatment. In the present study, we fabricated polypyrrole nanoparticles by employing bovine serum albumin-phycocyanin complex and the formulated particles were stable in various physiological solutions like water, phosphate buffered saline and culture media. The formulated nanoparticles did not cause any noticeable toxicity to MDA-MB-231 and HEK-293 cells. The obtained nanoparticles effectively killed MDA-MB-231 cells in a dual way upon laser illumination, one is through phycocyanin propagated reactive oxygen species (PDT) upon laser illumination and in another way it eradicated the treated cells by converting optical energy into heat energy (PTT)...
November 14, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29146595/the-cartilage-specific-lectin-c-type-lectin-domain-family-3-member-a-clec3a-enhances-tissue-plasminogen-activator-mediated-plasminogen-activation
#4
Daniela Lau, Dzemal Elezagic, Gabriele Hermes, Matthias Mörgelin, Alexander P Wohl, Manuel Koch, Ursula Hartmann, Stefan Höllriegl, Raimund Wagener, Mats Paulsson, Thomas Streichert, Andreas R Klatt
C-type lectin domain family 3 member A (CLEC3A) is a poorly characterized protein belonging to the superfamily of C-type lectins. Its closest homologue tetranectin binds to the kringle 4 domain of plasminogen and enhances its association with tissue plasminogen activator (tPA) thereby enhancing plasmin production, but whether CLEC3A contributes to plasminogen activation is unknown. Here, we recombinantly expressed murine and human full-length CLEC3As as well as truncated forms of CLEC3A in HEK-293 EBNA cells...
November 16, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29144788/panchakola-reduces-oxidative-stress-in-mcf-7-breast-cancer-and-hek293-cells
#5
Tooba Naz Shamsi, Romana Parveen, Sadaf Fatima
A large number of studies have proven the efficacy of ayurveda in the field of health and wellness. Panchakola, an ayurvedic formulation, is a general health tonic primarily used to cure fever, inflammation, pain, indigestion, and so on. We investigated effects of panchakola on oxidative stress in MCF-7 breast cancer and human embryonic kidney 293 (HEK293) cells. This work was performed to assess the antineoplastic and free radical-scavenging potential of aqueous extract of panchakola, a polyherbal formulation, in normal and breast cancer cell lines (i...
November 16, 2017: Journal of Dietary Supplements
https://www.readbyqxmd.com/read/29143966/drug-interaction-at-herg-channel-in-vitro-assessment-of-the-electrophysiological-consequences-of-drug-combinations-and-comparison-against-theoretical-models
#6
Barbara Wiśniowska, Bartosz Lisowski, Magdalena Kulig, Sebastian Polak
Drugs carry a proarrhythmic risk, which gets even greater when they are used in combination. In vitro assessment of the proarrhythmic potential of drugs is limited to one compound and thus neglects the potential of drug-drug interactions, including those involving active metabolites. Here we present the results of an in vitro study of potential drug-drug interactions at the level of the hERG channel for the combination of up to three compounds: loratadine, desloratadine and ketoconazole. Experiments were performed at room temperature on an automated patch-clamp device CytoPatch 2, with the use of heterogeneously, stably transfected HEK cells...
November 16, 2017: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/29142410/methanolic-extract-of-costus-pictus-d-don-induces-cytotoxicity-in-liver-hepatocellular-carcinoma-cells-mediated-by-histone-deacetylase-inhibition
#7
P V Neethu, K Suthindhiran, M A Jayasri
Background: Leaves of Costus pictus D. Don, (insulin plant) are used as dietary supplement for the treatment of diabetes. Objective: The antidiabetic activity of this plant is well documented, but its activity on different cell types and mechanism remains unknown. Thus, the present study evaluates the cytotoxicity of C. pictus methanolic extract (CPME) against various cancer and normal cells. Materials and Methods: Dried leaves of C. pictus were extracted using methanol and were subjected to histone deacetylase (HDAC) inhibition and toxicity studies...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29140689/tissue-inhibitor-of-metalloprotease-2-timp-2-bioprocess-development-physicochemical-biochemical-and-biological-characterization-of-highly-expressed-recombinant-protein
#8
Ananda Chowdhury, Robert G Brinson, Beiyang Wei, William G Stetler-Stevenson
Tissue Inhibitor of Metalloprotease -2 (TIMP-2) is a secreted 21 kDa multifunctional protein first described as an endogenous inhibitor of matrix metalloproteinases (MMPs) that prevents breakdown of the extracellular matrix often observed in chronic diseases. TIMP-2 diminishes growth factor-mediated cell proliferation in vitro, as well as neoangiogenesis and tumor growth in vivo independent of its MMP-inhibitory activity, . These physiological properties make TIMP-2 an excellent candidate for further pre-clinical development as a biologic therapy of cancer...
November 15, 2017: Biochemistry
https://www.readbyqxmd.com/read/29139616/raft-polymerization-for-the-synthesis-of-tertiary-amine-based-diblock-copolymer-nucleic-acid-delivery-vehicles
#9
Annie K McClellan, Taisen Hao, Tracy A Brooks, Adam E Smith
The synthesis and characterization of a family of nine pH-responsive, diblock copolymers designed to effectively deliver nucleic acids are reported. The stabilizing A block is comprised of an oligo(ethylene glycol) methyl ether methacrylate to impart water solubility. The cationic blocks of varying degrees of polymerization (DPs) are derived from three pH responsive, tertiary amine-containing methacrylates capable of complexing negatively charged nucleic acids. The cytotoxicity studies utilizing human embryonic kidney cells (HEK-293) and Michigan Cancer Foundation-7 (MCF-7) breast cancer cells indicate no decrease of cell viability with the diblock copolymers, with the exception of the two highest DPs of the cationic blocks with ethyl-substitutes tertiary amine...
November 15, 2017: Macromolecular Bioscience
https://www.readbyqxmd.com/read/29133173/effects-of-norquetiapine-the-active-metabolite-of-quetiapine-on-cloned-herg-potassium-channels
#10
Hong Joon Lee, Jin-Sung Choi, Bok Hee Choi, Sang June Hahn
Quetiapine is an atypical antipsychotic drug that is widely used for the treatment of schizophrenia. It is mainly metabolized by a cytochrome P450 system in the liver. Norquetiapine is a major active metabolite in humans with a pharmacological profile that differs distinctly from that of quetiapine. We used the whole-cell patch-clamp technique to investigate the effects of norquetiapine on hERG channels that are stably expressed in HEK cells. Quetiapine and norquetiapine inhibited the hERG tail currents at -50mV in a concentration-dependent manner with IC50 values of 8...
November 11, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/29132810/medium-retaining-petri-dish-insert-to-grow-and-image-cultured-cells
#11
Lech Kiedrowski, Alan Feinerman
BACKGROUND: Microscope chambers that accept glass coverslips with cultured cells are often used to monitor intracellular Ca(2+) concentration ([Ca(2+)]i) during cell superfusion. Unfortunately, the experimental maneuvers associated with the coverslip installation in these chambers (medium removal and re-application) trigger unintended [Ca(2+)]i elevations. NEW METHOD: To prevent these [Ca(2+)]i elevations, a Petri dish insert has been constructed. The insert features a superfusion-optimized well to grow cell cultures...
November 10, 2017: Journal of Neuroscience Methods
https://www.readbyqxmd.com/read/29129572/biocompatible-fluorinated-poly-%C3%AE-amino-ester-s-for-safe-and-efficient-gene-therapy
#12
Jia-Hui Gong, Yi Wang, Lei Xing, Peng-Fei Cui, Jian-Bin Qiao, Yu-Jing He, Hu-Lin Jiang
Cationic polymers have been widely used as one of the most promising non-viral vehicles for gene delivery due to their potential safety and ease of large-scale production. Here, we report the design and synthesis of a series of novel biodegradable fluorinated poly(β-amino ester)s (FPBAEs) by simple Michael-addition reaction as safe and efficient gene carrier. The results of transfection efficacy assay demonstrated the optimal FPBAE could mediated much higher GFP expression than the commercial transfection agents, polyethyleneimine (PEI, Mw = 25K) and Lipo 2000, as well as the non-fluorinated poly(β-amino ester)s (PBAE) on both HeLa and HEK-293T cell lines (higher than 70 and 90%, respectively), which was largely attributed to fluorination...
November 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29129206/differential-cytotoxicity-and-intracellular-calcium-signalling-following-activation-of-the-calcium-permeable-ion-channels-trpv1-and-trpa1
#13
Thomas Stueber, Mirjam J Eberhardt, Yaki Caspi, Shaya Lev, Alexander Binshtok, Andreas Leffler
Several members of the transient receptor channel (TRP) family can mediate a calcium-dependent cytotoxicity. In sensory neurons, vanilloids like capsaicin induce neurotoxicity by activating TRPV1. The closely related ion channel TRPA1 is also activated by irritants, but it is unclear if and how TRPA1 mediates cell death. In the present study we explored cytotoxicity and intracellular calcium signalling resulting from activation of TRPV1 and TRPA1, either heterologously expressed in HEK 293 cells or in native mouse dorsal root ganglion (DRG) neurons...
December 2017: Cell Calcium
https://www.readbyqxmd.com/read/29126939/synthesis-and-evaluation-of-anti-fungal-activities-of-sodium-alginate-amphotericin-b-conjugates
#14
Vasanthan Ravichandran, A Jayakrishnan
Sodium alginate (SA) was oxidized using periodate and amphotericin B (AmB) was conjugated via imine and amine linkages to the oxidized alginate. Oxidization drastically reduced the molecular weight (MW) of the alginate. The conjugates were highly water-soluble to the extent of 1000mg/mL making them useful for therapeutic applications. SA-AmB conjugates derived from 20 and 50% oxidized alginate were non-toxic to HEK 293T and RAW 264.7 cell line at 100μg/mL and was also non-hemolytic to human blood at 100μg/mL...
November 7, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29126749/corrigendum-to-efficacy-of-e2-glycoprotein-fused-to-porcine-cd154-as-a-novel-chimeric-subunit-vaccine-to-prevent-classical-swine-fever-virus-vertical-transmission-in-pregnant-sows
#15
Sara Muñoz-González, Yusmel Sordo, Marta Pérez-Simó, Marisela Suarez, Albert Canturri, Maria Pilar Rodriguez, María Teresa Frías-Lepoureau, Mariano Domingo, Mario Pablo Estrada, Llilianne Ganges
Here we evaluated the effect of double vaccination with a novel subunit marker vaccine candidate based in the CSFV E2 glycoprotein fused to the porcine CD154 to prevent CSFV vertical transmission. A lentivirus-based gene delivery system was used to obtain a stable recombinant HEK 293 cell line for the expression of E2 fused to porcine CD154 molecule. Six pregnant sows were distributed in two groups and at 64days of gestation animals numbered 1-4 (group 1) were vaccinated via intramuscular inoculation with 50μg of E2-CD154 subunit vaccine...
November 7, 2017: Veterinary Microbiology
https://www.readbyqxmd.com/read/29126725/conformationally-rigid-derivatives-of-way-267-464-synthesis-and-pharmacology-at-the-human-oxytocin-and-vasopressin-1a-receptors
#16
William T Jorgensen, Damien W Gulliver, Timothy A Katte, Eryn L Werry, Tristan A Reekie, Mark Connor, Michael Kassiou
WAY-267,464 (1) and twelve conformationally rigid analogues (3a-f-4a-f) were synthesised, characterised and evaluated in cellular assays with the aim of systematically exploring interactions with the oxytocin receptor (OTR). Each analogue was evaluated in radioligand binding displacement assays at both human OTR and arginine vasopressin 1a receptors (V1aR). Physiological characterisation was determined by whole cell IP1 accumulation assays on stably transfected human embryonic kidney (HEK) cells. Incorporation of the rigid, optionally substituted benzene ring abolished OTR activity and diminished V1aR pharmacology when compared to 1...
October 23, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29109685/binding-and-signaling-studies-disclose-a-potential-allosteric-site-for-cannabidiol-in-cannabinoid-cb2-receptors
#17
Eva Martínez-Pinilla, Katia Varani, Irene Reyes-Resina, Edgar Angelats, Fabrizio Vincenzi, Carlos Ferreiro-Vera, Julen Oyarzabal, Enric I Canela, José L Lanciego, Xavier Nadal, Gemma Navarro, Pier Andrea Borea, Rafael Franco
The mechanism of action of cannabidiol (CBD), the main non-psychotropic component of Cannabis sativa L., is not completely understood. First assumed that the compound was acting via cannabinoid CB2 receptors (CB2Rs) it is now suggested that it interacts with non-cannabinoid G-protein-coupled receptors (GPCRs); however, CBD does not bind with high affinity to the orthosteric site of any GPCR. To search for alternative explanations, we tested CBD as a potential allosteric ligand of CB2R. Radioligand and non-radioactive homogeneous binding, intracellular cAMP determination and ERK1/2 phosphorylation assays were undertaken in heterologous systems expressing the human version of CB2R...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29109527/the-rna-binding-protein-la-ss-b-promotes-rig-i-mediated-type-i-and-type-iii-ifn-responses-following-sendai-viral-infection
#18
Rebecca Mahony, Lindsay Broadbent, Jacen S Maier-Moore, Ultan F Power, Caroline A Jefferies
La/SS-B (or La) is a 48 kDa RNA-binding protein and an autoantigen in autoimmune disorders such as systemic lupus erythematosus (SLE) and Sjögren's syndrome (SS). La involvement in regulating the type I interferon (IFN) response is controversial - acting through both positive and negative regulatory mechanisms; inhibiting the IFN response and enhancing viral growth, or directly inhibiting viral replication. We therefore sought to clarify how La regulates IFN production in response to viral infection. ShRNA knockdown of La in HEK 293 T cells increased Sendai virus infection efficiency, decreased IFN-β, IFN-λ1, and interferon-stimulated chemokine gene expression...
November 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29107984/treatment-with-proteasome-inhibitor-bortezomib-decreases-organic-anion-transporting-polypeptide-oatp-1b3-mediated-transport-in-a-substrate-dependent-manner
#19
Khondoker Alam, Taleah Farasyn, Alexandra Crowe, Kai Ding, Wei Yue
OATP1B1 and OATP1B3 mediate hepatic uptake of many drugs (e.g., statins) and can mediate transporter-mediated drug-drug-interactions (DDIs). Bortezomib is the first-in-class proteasome inhibitor drug approved by the U. S. Food and Drug Administration for the treatment of multiple myeloma. The potential of bortezomib to cause OATP-mediated DDIs has not been assessed. The current study investigated the involvement of the ubiquitin-proteasome system (UPS) in OATP1B1 and OATP1B3 degradation and determined the effects of proteasome inhibitors on OATP1B1- and OATP1B3-mediated transport...
2017: PloS One
https://www.readbyqxmd.com/read/29107899/role-of-micrornas-in-senescence-and-its-contribution-to-peripheral-neuropathy-in-the-arsenic-exposed-population-of-west-bengal-india
#20
Debmita Chatterjee, Apurba Bandyopadhyay, Nilendu Sarma, Santanu Basu, Tarit Roychowdhury, Sib Sankar Roy, Ashok K Giri
Arsenic induced senescence (AIS) has been identified in the population of West Bengal, India very recently. Also there is a high incidence of arsenic induced peripheral neuropathy (PN) throughout India. However, the epigenetic regulation of AIS and its contribution in arsenic induced PN remains unexplored. We recruited seventy two arsenic exposed and forty unexposed individuals from West Bengal to evaluate the role of senescence associated miRNAs (SA-miRs) in AIS and their involvement if any, in PN. The downstream molecules of the miRNA associated with the disease outcome, was also checked by immuoblotting...
November 3, 2017: Environmental Pollution
keyword
keyword
79428
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"