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https://www.readbyqxmd.com/read/28528251/biological-activity-and-safety-profile-of-the-essential-oil-from-fruits-of-heracleum-mantegazzianum-sommier-levier-apiaceae
#1
Krystyna Skalicka-Woźniak, Agnieszka Grzegorczyk, Łukasz Świątek, Magdalena Walasek, Jarosław Widelski, Barbara Rajtar, Małgorzata Polz-Dacewicz, Anna Malm, Hosam O Elansary
A composition of essential oils obtained from Heracleum mantegazzianum (Apiaceae) was examined using a GC-MS method. n-Octyl acetate (19.92%), n-hexyl-2-methylbutanoate (10.84%), n-octanol (10.13%), n-octyl butanoate (8.88%), n-octyl-2-methylbutanoate (8.01%), n-hexyl acetate (7.11%), n-octyl isobutanoate (5.5%) and n-hexyl isobutanoate (5.43%) were the main compounds. The high-performance counter-current chromatography was applied for purification of aliphatic alcohols and esters. A mixture of n-hexane, acetonitrile and tetr-butyl methyl ether (1:1:0...
May 17, 2017: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/28527829/graphene-oxide-nanosheets-and-d-%C3%AE-tocopheryl-polyethylene-glycol-1000-succinate-tpgs-doping-improves-biocompatibility-and-ultrafiltration-in-polyethersulfone-hollow-fiber-membranes
#2
Akshay Modi, Surendra Kumar Verma, Jayesh Bellare
Novel graphene oxide (G)-and d-α-Tocopheryl polyethylene glycol 1000 succinate (T)-doped polyethersulfone (P) hollow fiber membranes (GTP HFMs) were efficiently prepared. GTP HFMs were found to be a desirable biocompatible substrate for attachment and proliferation of human embryonic kidney-293 (HEK-293) cells. Significantly high porosity (94.58±1.1%), low contact angle (61.1±2.5°), low hemolysis (0.58% in batch mode and 0.64% in continuous mode), low terminal complement complex activation (SC5b-9 marker level ∼6...
May 12, 2017: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/28527222/functional-characterization-of-c-terminal-ryanodine-receptor-1-variants-associated-with-central-core-disease-or-malignant-hyperthermia
#3
Remai Parker, Anja H Schiemann, Elaine Langton, Terasa Bulger, Neil Pollock, Andrew Bjorksten, Robyn Gillies, David Hutchinson, Richard Roxburgh, Kathryn M Stowell
BACKGROUND: Central core disease and malignant hyperthermia are human disorders of skeletal muscle resulting from aberrant Ca2+ handling. Most malignant hyperthermia and central core disease cases are associated with amino acid changes in the type 1 ryanodine receptor (RyR1), the skeletal muscle Ca2+-release channel. Malignant hyperthermia exhibits a gain-of-function phenotype, and central core disease results from loss of channel function. For a variant to be classified as pathogenic, functional studies must demonstrate a correlation with the pathophysiology of malignant hyperthermia or central core disease...
May 15, 2017: Journal of Neuromuscular Diseases
https://www.readbyqxmd.com/read/28526626/longevity-and-healthy-ageing-genes-foxo3a-and-sirt3-serum-protein-marker-and-new-road-map-to-burst-oxidative-stress-by-withania-somnifera
#4
Rashmita Pradhan, Rahul Kumar, Shashank Shekhar, Nitish Rai, Akash Ambashtha, Joyita Banerjee, Mona Pathak, S N Dwivedi, Sharmistha Dey, Aparajit B Dey
BACKGROUND: Ageing process is characterized by a decline in function; different age related diseases and excessive age associated mortality. There has always been a quest for easily accessible biomarkers to monitor and identify the development of age-associated stress for providing new anti-ageing strategies. Forkhead box protein O3A (FOXO3A) and Sirtuin3 (SIRT3) are such potential markers which plays important role in a wide variety of cellular mechanisms and has been proposed to be an ideal candidate to study longevity and are potential candidate for healthy ageing by oxidative burst...
May 16, 2017: Experimental Gerontology
https://www.readbyqxmd.com/read/28526263/n-stearoyl-l-tyrosine-inhibits-the-cell-senescence-and-apoptosis-induced-by-h2o2-in-hek293-tau-cells-via-the-cb2-receptor
#5
Yue Hu, Kai-Yi Zhou, Ze-Jian Wang, Yang Lu, Ming Yin
Although considerable energy and money have been spent trying to inhibit Aβ production and its related metabolic enzyme activities, there are still no drug treatments available to cure even slow for Alzheimer's disease. Therefore, tau protein has been focused recently as the new target for the treatment of Alzheimer's disease. The transfected human embryonic kidney 293 (HEK 293) cells with or without Tau 411 plasmid were used to evaluate the effect of tau protein on cell viability. H2O2 was added to simulate microenvironment of oxidative stress (OS) during aging...
May 16, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28525902/mir-148a-impairs-ras-erk-signaling-in-b-lymphocytes-by-targeting-sos-proteins
#6
Julia Alles, Nicole Ludwig, Stefanie Rheinheimer, Petra Leidinger, Friedrich A Grässer, Andreas Keller, Eckart Meese
Although microRNAs have been recognized as central cellular regulators, there is an evident lack of knowledge about their targets. Here, we analyzed potential target genes for miR-148a functioning in Ras signaling in B cells, including SOS1 and SOS2. A dual-luciferase reporter assay showed significantly decreased luciferase activity upon ectopic overexpression of miR-148a in HEK-293T cells that were co-transfected with the 3'UTR of either SOS1 or SOS2. Each of the 3'UTRs of SOS1 and SOS2 contained two binding sites for miR-148a both of which were necessary for the decreased luciferase activity...
May 7, 2017: Oncotarget
https://www.readbyqxmd.com/read/28523102/design-and-synthesis-of-mercaptoacetamides-as-potent-selective-and-brain-permeable-histone-deacetylase-6-inhibitors
#7
Wei Lv, Guangming Zhang, Cyril Barinka, James H Eubanks, Alan P Kozikowski
A series of nonhydroxamate HDAC6 inhibitors were prepared in our effort to develop potent and selective compounds for possible use in central nervous system (CNS) disorders, thus obviating the genotoxicity often associated with the hydroxamates. Halogens are incorporated in the cap groups of the designed mercaptoacetamides in order to increase brain accessibility. The indole analogue 7e and quinoline analogue 13a displayed potent HDAC6 inhibitory activity (IC50, 11 and 2.8 nM) and excellent selectivity against HDAC1...
May 11, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28516479/g%C3%AE-s-signalling-of-the-cb1-receptor-and-the-influence-of-receptor-number
#8
David B Finlay, Erin E Cawston, Natasha L Grimsey, Morag R Hunter, Anisha Korde, V Kiran Vemuri, Alexandros Makriyannis, Michelle Glass
BACKGROUND AND PURPOSE: CB1 cannabinoid receptor signalling is canonically mediated through inhibitory Gαi proteins, but signalling through other G proteins occurs under some circumstances; Gαs being the most characterised secondary pathway. Determinants of this signalling switch identified to date include Gαi blockade, CB1 /D2 dopamine receptor co-stimulation, CB1 agonist class, and cell background. The aim of this study was to examine the effects of receptor number and ligand dependence on CB1 signalling...
May 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28512022/synthesis-antimycobacterial-activity-and-docking-study-of-2-aroyl-1-benzopyrano-4-3-c-pyrazol-4-1h-one-derivatives-and-related-hydrazide-hydrazones
#9
Violina T Angelova, Violeta Valcheva, Tania Pencheva, Yulian Voynikov, Nikolay Vassilev, Rositsa Mihaylova, Georgi Momekov, Boris Shivachev
A new convenient method for preparation of 2-aroyl-[1]benzopyrano[4,3-c]pyrazol-4(1H)-one derivatives 5b-g and coumarin containing hydrazide-hydrazone analogues 4a-e was presented. The antimycobacterial activity against reference strain Mycobacterium tuberculosis H37Rv and cytotoxicity against the human embryonic kidney cell line HEK-293 were tested in vitro. All compounds demonstrated significant minimum inhibitory concentrations (MIC) ranging 0.28-1.69μM, which were comparable to those of isoniazid. The cytotoxicity (IC50>200µM) to the "normal cell" model HEK-293T exhibited by 2-aroyl-[1]benzopyrano[4,3-c]pyrazol-4(1H)-one derivatives 5b-e, was noticeably milder compared to that of their hydrazone analogues 4a-e (IC50 33-403µM)...
May 5, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28511693/antagonistic-action-on-nmda-glun2b-mediated-currents-of-two-peptides-that-were-conantokin-g-structure-based-designed
#10
Edwin A Reyes-Guzman, Nohora Vega-Castro, Edgar A Reyes-Montaño, Esperanza Recio-Pinto
BACKGROUND: The GluN2B subunit of the N-methyl-D-aspartate receptor (NMDAr) modulates many physiological processes including learning, memory, and pain. Excessive increase in NMDAr/GluN2B activity has been associated with various disorders such neuropathic pain and neuronal death following hypoxia. Thus there is an interest in identifying NMDAr antagonists that interact specifically with the GluN2B subunit. Recently based on structural analysis between the GluN2B subunit and conantokin-G, a toxin that interacts selectively with the GluN2B subunit, we designed various peptides that are predicted to act as NMDAr antagonists by interacting with the GluN2B subunit...
May 16, 2017: BMC Neuroscience
https://www.readbyqxmd.com/read/28510366/hmga2-plays-an-important-role-in-cr-vi-induced-autophagy
#11
Fan Yang, Lian Zhao, Dan Mei, Liping Jiang, Chengyan Geng, Qiujuan Li, Xiaofeng Yao, Yong Liu, Ying Kong, Jun Cao
Cr (VI) is mutagenic and carcinogenic, but the mechanism is unclear. In this study, the involvement of high mobility group A2 (HMGA2) in Cr (VI)-induced autophagy was investigated. Cr (VI) treatment induced formation of autophagosomes, increased expression of LC3II, Atg12-Atg5, Atg4, Atg10, HMGA1 and HMGA2 proteins, and decreased the expression of p62 in A549 cells. Silencing of HMGA2 gene by siRNA blocked Cr (VI)-induced formation of autophagosomes, expression of LC3II, Atg12-Atg5, Atg10 and reduction of p62...
May 16, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28506725/the-first-invertebrate-nfil3-transcription-factor-with-role-in-immune-defense-identified-from-the-hong-kong-oyster-crassostrea-hongkongensis
#12
Jun Li, Yang Zhang, Yuehuan Zhang, Fan Mao, Zhiming Xiang, Shu Xiao, Haitao Ma, Ziniu Yu
NFIL3 (nuclear factor interleukin 3-regulated) is a basic leucine zipper type transcription factor that mediates a variety of immune responses in vertebrates. However, the sequence information and function of NFIL3 homologs in invertebrates, especially mollusks, remains unknown. In the present study, the first NFIL3 homolog was identified in a marine mollusk, Crassostrea hongkongensis (designated as ChNFIL3), followed by its functional characterization. The full-length cDNA of ChNFIL3 is 2221 bp and consists of an open reading frame (ORF) of 1536 bp that encodes a polypeptide of 551 amino acids...
May 12, 2017: Developmental and Comparative Immunology
https://www.readbyqxmd.com/read/28505480/triphenyltin-iv-benzoates-with-diazenyl-imino-scaffold-exhibiting-remarkable-apoptosis-mediated-by-reactive-oxygen-species
#13
Tushar S Basu Baul, Dhrubajyoti Dutta, Andrew Duthie, Ritika Prasad, Nishant Kumar Rana, Biplob Koch, Edward R T Tiekink
The cytotoxic potency of a series of triphenyltin(IV) compounds of general composition [Ph3Sn(L(n))] (1-6) has been probed in vitro employing MDA-MB-231 (human breast cancer) and HeLa (human cervical cancer) cell lines, where L(n)=L(1-3); isomeric 2/3/4-{(E)-2-[4-(dimethylamino)phenyl]diazenyl}benzoates and L(4-6) are their corresponding isoelectronic imino analogues 2/3/4-[(E)-{[4-(dimethylamino)phenyl]methylidene}amino]benzoates. Compounds 1-6 have been characterized by elemental analysis and their spectroscopic properties were studied using IR and NMR ((1)H, (13)C, (119)Sn) techniques...
April 29, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/28504248/the-flavonoid-tl-2-8-induces-cell-death-and-immature-mitophagy-in-breast-cancer-cells-via-abrogating-the-function-of-the-aha1-hsp90-complex
#14
Hui-Juan Liu, Xiao-Xiao Jiang, Yi-Zhen Guo, Fang-Hui Sun, Xin-Hui Kou, Yong Bao, Zhu-Qing Zhang, Zhao-Hu Lin, Ting-Bo Ding, Lan Jiang, Xin-Sheng Lei, Yong-Hua Yang
The flavonoid quercetin exhibits significant anticancer activities with few side effects. In the current study, we characterized TL-2-8, a quercetin derivative, as a novel anticancer agent in vitro and in vivo. Cell proliferation and viability were assessed using Cell Counting Kit-8 and CellTiter-Blue assay, respectively. Cell death was examined using PI staining or a TUNEL assay. Mitophagy was determined by measuring autophagic flux and by confocal imaging. Protein expression was examined by Western blotting...
May 1, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28503428/soluble-expression-of-recomb-inant-cmyc-klf4-oct4-and-sox2-proteins-in-bacteria-and-transduction-into-living-cells
#15
Guo-Dan Liu, Shi-Feng Zhou, Xu-Chen Ding, Chun-Lai Fang, Shu-Yong Mi, Xiang-Chun Gao, Qing Han
AIM: To develop a new method to produce recombinant reprogramming proteins, cMyc, Klf4, Oct4, and Sox2, in soluble format with low cost for the generation of induced pluripotent stem cells (iPSCs). METHODS: A short polypeptide sequence derived from the HIV trans-activator of transcription protein (TAT) and the nucleus localization signal (NLS) polypeptide were fused to the N terminus of the reprogramming proteins and they were constructed into pCold-SUMO vector which can extremely improve the solubility of recombinant proteins...
2017: International Journal of Ophthalmology
https://www.readbyqxmd.com/read/28502792/drug-binding-poses-relate-structure-with-efficacy-in-the-%C3%AE-opioid-receptor
#16
Katy J Sutcliffe, Graeme Henderson, Eamonn Kelly, Richard B Sessions
The μ-opioid receptor (MOPr) is a clinically important G protein-coupled receptor (GPCR) which couples to Gi/o proteins and arrestins. At present the receptor conformational changes that occur following agonist binding and activation are poorly understood. This study has employed molecular dynamics simulations to investigate the binding mode and receptor conformational changes induced by structurally similar opioid ligands of widely differing intrinsic agonist efficacy, norbuprenorphine, buprenorphine and diprenorphine...
May 11, 2017: Journal of Molecular Biology
https://www.readbyqxmd.com/read/28501618/assessing-activity-of-hepatitis-a-virus-3c-protease-using-a-cyclized-luciferase-based-biosensor
#17
Junwei Zhou, Dang Wang, Yongqiang Xi, Xinyu Zhu, Yuting Yang, Mengting Lv, Chuanzhen Luo, Jiyao Chen, Xu Ye, Liurong Fang, Shaobo Xiao
Hepatitis A is an acute infection caused by Hepatitis A virus (HAV), which is widely distributed throughout the world. The HAV 3C cysteine protease (3C(pro)), an important nonstructural protein, is responsible for most cleavage within the viral polyprotein and is critical for the processes of viral replication. Our group has previously demonstrated that HAV 3C(pro) cleaves human NF-κB essential modulator (NEMO), a kinase required in interferon signaling. Based on this finding, we generated four luciferase-based biosensors containing the NEMO sequence (PVLKAQ↓ADIYKA) that is cleaved by HAV 3C(pro) and/or the Nostoc punctiforme DnaE intein, to monitor the activity of HAV 3C(pro) in human embryonic kidney cells (HEK-293T)...
May 10, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28500977/endocytosis-and-intracellular-traffic-of-cholesterol-pdmaema-liposome-complexes-in-human-epithelial-like-cells
#18
F Szymanowski, A A Hugo, P Alves, P N Simões, A Gómez-Zavaglia, Pablo F Pérez
Liposomes are generally used as delivery systems, as they are capable of encapsulating a wide variety of molecules (i.e. plasmids, recombinant proteins, therapeutic drugs). However, liposomal drug delivery have to fulfill different requirements, such as the effective internalization by the target cells and avoidance of the degradative activity of the intracellular compartments. The use of polymer lipid complexes (PLCs), by including different polymers in the liposome formulation, could improve internalization and intracellular release of drugs...
May 1, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28500862/enhanced-tau-aggregation-in-the-presence-of-amyloid-%C3%AE
#19
Rachel E Bennett, Sarah L DeVos, Simon Dujardin, Bianca Corjuc, Rucha Gor, Jose Gonzalez, Allyson D Roe, Matthew P Frosch, Rose Pitstick, George A Carlson, Bradley T Hyman
Amyloid plaques and neurofibrillary tangles co-occur in Alzheimer disease, but with different topological and temporal patterns. Whether these two lesions are independent or pathobiologically related is uncertain. For example, amyloid deposition in the neocortex precedes the spread of tau neurofibrillary tangles from the limbic areas to the cortex. We examined the aggregation properties of tau isolated from human cases with early tau pathology (Braak II) with and without plaques. Using a well-established HEK cell biosensor assay, we show that tau from cases with plaques has an enhanced ability to induce tau aggregates compared to tau from cases without plaques...
May 10, 2017: American Journal of Pathology
https://www.readbyqxmd.com/read/28500657/modulation-of-herg-channels-by-5-1h-indazol-5-yl-oxy-methyl-n-4-trifluoromethoxy-phenyl-pyrimidin-2-amine-itp-2-a-novel-small-molecule-activator
#20
Harinath Sale, Samrat Roy, Jayakumar Warrier, Srinivasan Thangathirupathy, Yoganand Vadari, Shruthi K Gopal, Prasad Krishnamurthy, Manjunath Ramarao
BACKGROUND AND PURPOSE: hERG channel activators have potential utility in the treatment of acquired and congenital long QT syndrome. In this article, we describe a new hERG activator, 5-(((1H-indazol-5-yl)oxy)methyl)-N-(4-(trifluoromethoxy)phenyl)pyrimidin-2-amine (ITP-2), with a chemical structure distinct from the previously reported compounds. EXPERIMENTAL APPROACH: We investigated the effect of ITP-2 on hERG1a and hERG1a/1b channels expressed heterologously in HEK-293 cells using conventional electrophysiological methods...
May 12, 2017: British Journal of Pharmacology
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