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https://www.readbyqxmd.com/read/28222316/discovery-and-characterization-of-novel-cyp1b1-inhibitors-based-on-heterocyclic-chalcones-overcoming-cisplatin-resistance-in-cyp1b1-overexpressing-lines
#1
Neill J Horley, Kenneth J M Beresford, Tarun Chawla, Glen J P McCann, Ketan C Ruparelia, Linda Gatchie, Vinay R Sonawane, Ibidapo S Williams, Hoon L Tan, Prashant Joshi, Sonali S Bharate, Vikas Kumar, Sandip B Bharate, Bhabatosh Chaudhuri
The structure of alpha-napthoflavone (ANF), a potent inhibitor of CYP1A1 and CYP1B1, mimics the structure of chalcones. Two potent CYP1B1 inhibitors 7k (DMU2105) and 6j (DMU2139) have been identified from two series of synthetic pyridylchalcones. They inhibit human CYP1B1 enzyme bound to yeast-derived microsomes (Sacchrosomes™) with IC50 values of 10 and 9 nM, respectively, and show a very high level of selectivity towards CYP1B1 with respect to the IC50 values obtained with CYP1A1, CYP1A2, CYP3A4, CYP2D6, CYP2C9 and CYP2C19 Sacchrosomes™...
February 9, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28219718/a-novel-regulatory-role-of-rgs4-in-stat5b-activation-neurite-outgrowth-and-neuronal-differentiation
#2
Paschalina Pallaki, Eirini-Maria Georganta, Ioannis Serafimidis, Maria-Pagona Papakonstantinou, Vassilis Papanikolaou, Sofia Koutloglou, Elsa Papadimitriou, Adamantia Agalou, Aggeliki Tserga, Alexandra Simeonof, Dimitra Thomaidou, Maria Gaitanou, Zafiroula Georgoussi
The Regulator of G protein Signalling 4 (RGS4) is a multitask protein that interacts with and negatively modulates opioid receptor signalling. Previously, we showed that the δ-opioid receptor (δ-OR) forms a multiprotein signalling complex consisting of Gi/Go proteins and the Signal Transducer and Activator of Transcription 5B (STAT5B) that leads to neuronal differentiation and neurite outgrowth upon δ-ΟR activation. Here, we investigated whether RGS4 could participate in signalling pathways to regulate neurotropic events...
February 17, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28218286/vinculin-variant-m94i-identified-in-sudden-unexplained-nocturnal-death-syndrome-decreases-cardiac-sodium-current
#3
Jianding Cheng, John W Kyle, Brandi Wiedmeyer, Di Lang, Ravi Vaidyanathan, Jonathan C Makielski
Sudden unexplained nocturnal death syndrome (SUNDS) remains an autopsy negative disorder with unclear etiology. Vinculin (VCL) was linked to sudden arrhythmia death in VCL knockout mice prior to the appearance of cardiomyopathy. We hypothesized VCL mutations underlie risk for SUNDS. A rare heterozygous variant VCL-M94I was found in a SUNDS victim who suffered sudden nocturnal tachypnea and lacked pathogenic variants in known arrhythmia-causing genes. VCL was identified to interact with SCN5A in vitro/vivo. The VCL-M94I was co-expressed with the cardiac sodium channel in HEK293 cells and also overexpressed in induced pluripotent stem cells derived cardiomyocytes (iPSCs-CM)...
February 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28216001/loperamide-inhibits-sodium-channels-to-alleviate-inflammatory-hyperalgesia
#4
Ying Wu, Beiyan Zou, Lingli Liang, Min Li, Yuan-Xiang Tao, Haibo Yu, Xiaoliang Wang, Min Li
Previous studies demonstrated that Loperamide, originally known as an anti-diarrheal drug, is a promising analgesic agent primarily targeting mu-opioid receptors. However some evidences suggested that non-opioid mechanisms may be contributing to its analgesic effect. In the present study, Loperamide was identified as a Nav1.7 blocker in a pilot screen. In HEK293 cells expressing Nav1.7 sodium channels, Loperamide blocked the resting state of Nav1.7 channels (IC50 = 1.86 ± 0.11 μM) dose-dependently and reversibly...
February 16, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28215700/effect-of-therapeutic-concentration-of-lithium-on-live-hek293-cells-increase-of-na-k-atpase-change-of-overall-protein-composition-and-alteration-of-surface-layer-of-plasma-membrane
#5
Miroslava Vosahlikova, Hana Ujcikova, Oleksandr Chernyavskiy, Jana Brejchova, Lenka Roubalova, Martin Alda, Petr Svoboda
BACKGROUND: The effect of long-term exposure of live cells to lithium cations (Li) was studied in HEK293 cells cultivated in the presence of 1mM LiCl for 7 or 21days. The alteration of Na(+)/K(+)-ATPase level, protein composition and biophysical state of plasma membrane was determined with the aim to characterize the physiological state of Li-treated cells. METHODS: Na(+)/K(+)-ATPase level was determined by [(3)H]ouabain binding and immunoblot assays. Overall protein composition was determined by 2D electrophoresis followed by proteomic analysis by MALDI-TOF MS/MS and LFQ...
February 12, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28214891/up-regulated-atf4-expression-increases-cell-sensitivity-to-apoptosis-in-response-to-radiation
#6
Ying Zong, Shijie Feng, Jinwei Cheng, Chenlin Yu, Guocai Lu
BACKGROUND/AIMS: Activating transcription factor 4 (ATF4) is a member of the activating transcription factor family which regulates the expression of genes involved in amino acid metabolism, redox homeostasis and ER stress responses. ATF4 is also over-expressed in human solid tumors, although its effect on responsiveness to radiation is largely unexplored. METHODS: Real-time PCR was used to detect ATF4 mRNA levels in cells treated with different doses of 60Coγ radiation...
February 13, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28214294/ptk6-localized-at-the-plasma-membrane-promotes-cell-proliferation-and-migration-through-phosphorylation-of-eps8
#7
Won-Sik Shin, Hyun Jae Shim, Young Hun Lee, Minju Pyo, Jun Sang Park, So Yun Ahn, Seung-Taek Lee
Protein tyrosine kinase 6 (PTK6; also known as Brk) is closely related to the Src family kinases, but lacks a membrane-targeting myristoylation signal. Sublocalization of PTK6 at the plasma membrane enhances its oncogenic potential. To understand the mechanism(s) underlying the oncogenic property of plasma-membrane-associated PTK6, proteins phosphorylated by membrane-targeted myristoylated PTK6 (Myr-PTK6) were enriched and analyzed using a proteomics approach. Eps8 which was identified by this method is phosphorylated by Myr-PTK6 in HEK293 cells...
February 18, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28213468/microencapsulation-of-lefty-secreting-engineered-cells-for-pulmonary-fibrosis-therapy-in-mice
#8
Hongge Ma, Shupei Qiao, Zeli Wang, Shuai Geng, Yufang Zhao, Xiaolu Hou, Weiming Tian, Xiongbiao Chen, Lifen Yao
Idiopathic pulmonary fibrosis (IPF) is a progressive disease that causes unremitting deposition of extracellular matrix proteins, thus resulting in distortion of the pulmonary architecture and impaired gas exchange. Associated with high morbidity and mortality, IPF is generally refractory to current pharmacological therapies. Lefty A, a potent inhibitor of transforming growth factor (TGF)-β signaling, has been shown to have promising antifibrotic ability in vitro for the treatment of renal fibrosis and other potential organ fibroses...
February 17, 2017: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/28213290/zd0947-a-sulphonylurea-receptor-modulator-detects-functional-sulphonylurea-receptor-subunits-in-murine-vascular-smooth-muscle-atp-sensitive-k-channels
#9
Tadashi Yamamoto, Kohei Takahara, Keiichiro Uchida, Noriyoshi Teramoto
In order to identify functional sulphonylurea receptor (SUR.x) subunits of native ATP-sensitive K(+) channels (KATP channels) in mouse portal vein, the effects of ZD0947, a SUR.x modulator, were investigated on spontaneous portal vein contractions, macroscopic membrane currents and unitary currents recorded (using patch-clamp techniques) in freshly dispersed mouse portal vein myocytes. Spontaneous contractions in mouse portal vein were reversibly reduced by ZD0947 in a concentration-dependent manner (Ki = 293nM)...
February 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28210905/hypermagnesemia-disturbances-in-rats-no-related-pentadecapeptide-bpc-157-abrogates-l-name-and-l-arginine-worsen
#10
Maria Medvidovic-Grubisic, Vasilije Stambolija, Danijela Kolenc, Jadranka Katancic, Tamara Murselovic, Ivna Plestina-Borjan, Sanja Strbe, Domagoj Drmic, Ivan Barisic, Aleksandra Sindic, Sven Seiwerth, Predrag Sikiric
AIM: Stable gastric pentadecapeptide BPC 157, administered before a high-dose magnesium injection in rats, might be a useful peptide therapy against magnesium toxicity and the magnesium-induced effect on cell depolarization. Moreover, this might be an NO-system-related effect. Previously, BPC 157 counteracts paralysis, arrhythmias and hyperkalaemia, extreme muscle weakness; parasympathetic and neuromuscular blockade; injured muscle healing and interacts with the NOS-blocker and NOS-substrate effects...
February 16, 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/28198152/discovery-of-cdc25a-lead-inhibitors-with-novel-chemotype-by-virtual-screening-application-of-pharmacophore-modeling-based-on-training-set-with-unique-limited-components
#11
Yushu Ge, Qianqian Han, Wenxiu Duan, Jiaqi Zhang, Kai Chen, Jiajia Wan, Yi Liu, Dan Liu
Cdc25 phosphatase has been studied as an attractive target for cancer therapy. Multiple pharmacophore models with unique core features of classic quinone inhibitors and novel inhibitors were used to discover novel lead inhibitor. 21 compounds with qualified physical properties were screened out from Maybridge hitfinderTM database containing 14400 compounds by pharmacophore models. 4 compounds inhibit the Cdc25A activity more than 50% at concentration of 100 μM. Among them, compound KM10389 (N-(2-((furan-2-ylmethyl)thio)ethyl)-2-((4-hydroxy-6-propylpyrimidin-2-yl)thio)acetamide) shows high enzyme inhibition activity with IC₅₀ of 7...
February 14, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28193731/selective-transport-of-neurotransmitters-and-modulators-by-distinct-volume-regulated-lrrc8-anion-channels
#12
Darius Lutter, Florian Ullrich, Jennifer C Lueck, Stefan Kempa, Thomas J Jentsch
In response to swelling, mammalian cells release chloride and organic osmolytes through VRAC volume-regulated anion channels. VRACs are heteromers of LRRC8A and other LRRC8 isoforms (B-E) which are co-expressed in HEK293 and most other cells. The spectrum of VRAC substrates and its dependence on particular LRRC8 isoforms remains largely unknown. We show that besides the osmolytes taurine and myo-inositol, LRRC8 channels transport the neurotransmitters glutamate, aspartate and GABA and the co-activator D-serine...
February 13, 2017: Journal of Cell Science
https://www.readbyqxmd.com/read/28193314/celecoxib-mediated-activation-of-endoplasmic-reticulum-stress-induces-de-novo-ceramide-biosynthesis-and-apoptosis-in-hepatoma-hepg2-cells
#13
Hyo Jin Maeng, Jae-Hwi Song, Goon-Tae Kim, Yoo-Jeong Song, Kangpa Lee, Jae-Young Kim, Tae-Sik Park
Ceramides are the major sphingolipid metabolites involved in cell survival and apoptosis. When HepG2 hepatoma cells were treated with celecoxib, the expression of the genes in de novo sphingolipid biosynthesis and sphingomyelinase pathway was upregulated and cellular ceramide was elevated. In addition, celecoxib induced endoplasmic reticulum (ER) stress in a time-dependent manner. SPTLC2, a subunit of serine palmitoyltransferase, was overexpressed by adenovirus. Adenoviral overexression of SPTLC2 (AdSPTLC2) decreased cell viability of HEK293 and HepG2 cells...
February 10, 2017: BMB Reports
https://www.readbyqxmd.com/read/28192748/exposure-to-pm2-5-induces-aberrant-activation-of-nf-%C3%AE%C2%BAb-in-human-airway-epithelial-cells-by-downregulating-mir-331-expression
#14
Lei Song, Dan Li, Xiaoping Li, Lianjun Ma, Xiaoxue Bai, Zhongmei Wen, Xiufang Zhang, Dong Chen, Liping Peng
Exposure to particulate matter (PM) with an aerodynamic diameter≤2.5μm (PM2.5) induces reactive oxygen species (ROS) and pro-inflammatory cytokine production, leading to airway epithelial injury. However, the mechanisms underlying the toxicity of PM2.5 have not been clarified. Here, we show that exposure to PM2.5 induces sustained activation of the nuclear factor kappa B (NF-κB) signaling in human airway epithelial Beas-2B (B2B) cells. In addition, PM2.5 exposure significantly decreased miR-331 expression in B2B cells, which was abrogated by inhibition of ROS or phosphoinositide 3-kinase (PI3K)/Akt pathway...
February 6, 2017: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/28192150/effect-of-artemisinin-on-neuropathic-pain-mediated-by-p2x4-receptor-in-dorsal-root-ganglia
#15
Mofeng Ying, Hui Liu, Tengling Zhang, Chenxu Jiang, Yingxin Gong, Bing Wu, Lifang Zou, Zhihua Yi, Shenqiang Rao, Guilin Li, Chunping Zhang, Tianyu Jia, Shanhong Zhao, Huilong Yua, Liran Shi, Lin Li, Shangdong Liang, Shuangmei Liu
Neuropathic pain is a type of chronic pain caused by nervous system damage and dysfunction. The pathogenesis of chronic pain is complicated, and there are no effective therapies for neuropathic pain. Studies show that the P2X4 receptor expressed in the satellite glial cells (SGCs) of dorsal root ganglia (DRG) is related to neuropathic pain. Artemisinin is a monomeric component extracted from traditional Chinese medicine and has a variety of important pharmacological effects and potential applications. This study observed the effect of artemisinin on neuropathic pain and delineated its possible mechanism...
February 9, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/28192090/optogenetic-control-of-ca-2-and-voltage-dependent-large-conductance-bk-potassium-channels
#16
Thomas Mager, Phillip G Wood, Ernst Bamberg
Ca(2+) concentration jumps for the activation of Ca(2+) dependent ion channels or transporters can be obtained either by fast solution exchange or the use of caged Ca(2+). Here we report on an alternate optogenetic method for activation of Ca(2+) and voltage dependent large conductance (BK) potassium channels. This was achieved through the use of the light-gated Ca(2+) permeable Channelrhodopsin 2 variant, CatCh, with enhanced Ca(2+) permeability, which produces locally [Ca(2+)] in the μM range on the inner side of the membrane, without significant [Ca(2+)] increase in the cytosol...
February 10, 2017: Journal of Molecular Biology
https://www.readbyqxmd.com/read/28190756/organic-anion-transporting-polypeptide-oatp-2b1-contributes-to-the-cellular-uptake-of-theaflavin
#17
Ayuko Kondo, Katsuya Narumi, Jiro Ogura, Ai Sasaki, Keisuke Yabe, Taku Kobayashi, Ayako Furugen, Masaki Kobayashi, Ken Iseki
Organic anion-transporting polypeptide (OATP) 2B1 has been reported in the apical membranes of the human small intestinal epithelium, where it contributes to the intestinal absorption of pharmacologically active drugs. To investigate the potential for OATP2B1-mediated drug-food interactions, the effects of several polyphenolic compounds on OATP2B1-mediated estrone-3-sulfate (E3S) transport were studied by using OATP2B1-expressing HEK293 cells. Our results showed that some compounds, especially theaflavin, were strong inhibitors of OATP2B1-mediated E3S uptake...
November 22, 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28190470/berberine-inhibits-the-proliferation-and-migration-of-breast-cancer-zr-75-30-cells-by-targeting-ephrin-b2
#18
Weina Ma, Man Zhu, Dongdong Zhang, Liu Yang, Tianfeng Yang, Xin Li, Yanmin Zhang
BACKGROUND: Berberine, a plant-derived compound isolated from Coptis chinensis used in traditional Chinese medicine, has been shown to possess anti-cancer properties. However, no study has shown that berberine could target ephrin-B2, which plays a critical role in cell proliferation and migration. PURPOSE: The aim of this study is to investigate the effect of berberine on cancer cell growth and migration, through the regulation of ephrin-B2 and downstream signaling molecules...
February 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28188930/microrna-135a-regulates-sodium-calcium-exchanger-gene-expression-and-cardiac-electrical-activity
#19
Eric Duong, Jiening Xiao, Xiao Yan Qi, Stanley Nattel
BACKGROUND: Complete atrioventricular block (CAVB) causes arrhythmogenic remodeling and increases the risk of Torsades de Pointes (TdP) arrhythmias. MicroRNAs (miRNAs) are key regulators of gene-expression that contribute to cardiac remodeling. OBJECTIVE: To assess miRNA changes after complete atrioventricular block (CAVB) and identify novel candidates potentially involved in arrhythmogenic cardiac remodeling. METHODS: CAVB was induced in mice via His bundle ablation...
February 7, 2017: Heart Rhythm: the Official Journal of the Heart Rhythm Society
https://www.readbyqxmd.com/read/28188415/apoptosis-inducing-ability-of-silver-i-cyanide-phosphines-useful-for-anti-cancer-studies
#20
Zelinda Human-Engelbrecht, Reinout Meijboom, Marianne J Cronjé
Metal-based drugs have shown early promise as anticancer agents suggesting the potential application of silver(I) complexes as apoptosis-inducing agents. The ability of a silver(I) cyanide containing phosphine complex to induce cell death was evaluated in both a malignant (SNO esophageal cancer) and non-malignant (HDF-a skin and HEK293 kidney) cell lines. A dose-dependent decrease in cell viability was observed in the SNO cells. Light microscopy revealed morphological features indicative of apoptotic cell death...
February 10, 2017: Cytotechnology
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