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https://www.readbyqxmd.com/read/28822888/apatinib-enhances-antitumour-activity-of-egfr-tkis-in-non-small-cell-lung-cancer-with-egfr-tki-resistance
#1
Fang Li, Tengjiao Zhu, Baoshan Cao, Jiadong Wang, Li Liang
BACKGROUND: Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs)-rechallenged therapy for EGFR-mutant non-small cell lung cancer (NSCLC) patients who acquired resistance showed moderate efficacy. Considering the high interrelation between EGFR and vascular endothelial growth factor/vascular endothelial growth factor receptor (VEGF/VEGFR) pathways, we firstly evaluated EGFR-TKI combined with apatinib (a highly selective VEGFR2 inhibitor) in EGFR-TKI-resistant model and patients...
August 17, 2017: European Journal of Cancer
https://www.readbyqxmd.com/read/28822150/-antimicrobial-and-anti-tumor-activities-of-endophytes-from-lycium-barbarum-of-ningxia
#2
Jin-Xia Dai, Xiao-Ning Du
The antimicrobial activity and cytotoxicity in vitro of the fermentation broth of 10 endophytic strains isolated from Lycium barbarum were determined to screen high activity endophytic strains. Sequences analysis of ITS and 16S rDNA was used for molecular identification of the strains. The results showed that 5 endophytic fungi had no inhibitory activity against the tested pathogens. Endophytic actinomycete strain AL6 had a certain inhibitory effect on 3 kinds of pathogenic fungi, and strain AL5 only had strong inhibitory activity against Staphylococcus aureus...
June 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28821924/-89-zr-labeled-nivolumab-for-imaging-of-t-cell-infiltration-in-a-humanized-murine-model-of-lung-cancer
#3
Christopher G England, Dawei Jiang, Emily B Ehlerding, Brian T Rekoske, Paul A Ellison, Reinier Hernandez, Todd E Barnhart, Douglas G McNeel, Peng Huang, Weibo Cai
PURPOSE: Nivolumab is a human monoclonal antibody specific for programmed cell death-1 (PD-1), a negative regulator of T-cell activation and response. Acting as an immune checkpoint inhibitor, nivolumab binds to PD-1 expressed on the surface of many immune cells and prevents ligation by its natural ligands. Nivolumab is only effective in a subset of patients, and there is limited evidence supporting its use for diagnostic, monitoring, or stratification purposes. METHODS: (89)Zr-Df-nivolumab was synthesized to map the biodistribution of PD-1-expressing tumor infiltrating T-cells in vivo using a humanized murine model of lung cancer...
August 19, 2017: European Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/28819431/tat-interactive-protein-60kda-tip60-regulates-the-tumorigenesis-of-lung-cancer-in-vitro
#4
Yang Yang, Jian Sun, Ting Chen, Zengyue Tao, Xianwei Zhang, Feng Tian, Xiao Zhou, Daru Lu
Histone acetyltransferases (HATs) play vital functions in the tumorigenesis of many solid organ malignancies. We previously screened a human HATs cDNA library and identified Tat-interactive protein-60KDa (TIP60) as a candidate critical HATs in the origination of lung cancer. In this study, our data suggested that overexpression of TIP60 inhibited the cell viability of A549 and H1299 cells since day 2. Compared to the control group, the viability of these two lung cancer cells was inhibited by 25% and 19% at day 6 with the overexpression of TIP60...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/28819407/ccr7-promote-lymph-node-metastasis-via-regulating-vegf-c-d-r3-pathway-in-lung-adenocarcinoma
#5
Jie Yu, Shaolin Tao, Pingping Hu, Ruwen Wang, Chunshu Fang, Yi Xu, Di Qi, Zhuanqin Wei, Jingge Zhang, Qunyou Tan
Lymph node metastasis is still an important issue in metastatic process of lung adenocarcinoma. C-C chemokine receptor 7 (CCR7) has been proved to be closely associated with the metastasis of lung adenocarcinoma, and the mechanism is poorly understood. In order to investigate the relationship between CCR7 and lymph node metastasis in lung adenocarcinoma, and to explore the role of CCR7 in treating lung adenocarcinoma, 40 clinical specimens were collected to define the relationship between CCR7 and lymph node metastasis in lung adenocarcinoma by immunohistochemistry...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/28819390/fluorofenidone-inhibits-the-proliferation-of-lung-adenocarcinoma-cells
#6
Zheng-Hao Deng, Jie Meng, Juan Tang, Gao-Yun Hu, Li-Jian Tao
Background: Lung carcinoma is the leading cause of malignant tumor related mortality in China in recent decades, and the development of new and effective therapies for patients with advanced lung carcinoma is needed. We recently found that fluorofenidone (FD), a newly developed pyridine compound, reduced the activation of Stat3 (Signal transducer and activator of transcription 3) in fibroblasts. Stat3 plays a crucial role in the development of lung cancer and may represent a new therapeutic target. In this study, we examined the effect of FD on human lung adenocarcinoma cells in vivo and in vitro...
2017: Journal of Cancer
https://www.readbyqxmd.com/read/28819223/levobuipivacaine-induced-dissemination-of-a549-lung-cancer-cells
#7
Shun-Ming Chan, Bo-Feng Lin, Chih-Shung Wong, Wen-Ting Chuang, Yu-Ting Chou, Zhi-Fu Wu
While anaesthetics are frequently used on cancer patients during surgical procedures, their consequence on cancer progression remains to be elucidated. In this study, we sought to investigate the influence of local anesthetics on lung cancer cell dissemination in vitro and in vivo. A549 human non-small lung cancer cells were treated with various local anaesthetics including ropivacaine, lidocaine, levobupivacaine and bupivacaine. Cell barrier property was assessed using an electric cell-substrate impedance sensing (ECIS) system...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28819152/dissecting-the-genomic-activity-of-a-transcriptional-regulator-by-the-integrative-analysis-of-omics-data
#8
Giulio Ferrero, Valentina Miano, Marco Beccuti, Gianfranco Balbo, Michele De Bortoli, Francesca Cordero
In the study of genomic regulation, strategies to integrate the data produced by Next Generation Sequencing (NGS)-based technologies in a meaningful ensemble are eagerly awaited and must continuously evolve. Here, we describe an integrative strategy for the analysis of data generated by chromatin immunoprecipitation followed by NGS which combines algorithms for data overlap, normalization and epigenetic state analysis. The performance of our strategy is illustrated by presenting the analysis of data relative to the transcriptional regulator Estrogen Receptor alpha (ERα) in MCF-7 breast cancer cells and of Glucocorticoid Receptor (GR) in A549 lung cancer cells...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28818740/assessment-of-genotoxicity-of-four-volatile-pollutants-from-cigarette-smoke-based-on-the-in-vitro-%C3%AE-h2ax-assay-using-high-content-screening
#9
Sen Zhang, Huan Chen, An Wang, Yong Liu, Hongwei Hou, Qingyuan Hu
To evaluate the genotoxic effects of formaldehyde, acetaldehyde, acrolein and benzene on A549 cells, the in vitro γH2AX assay was used in combination with high content screening (HCS) technology. All aldehydes showed a significant genotoxicity in a dose/time-dependent effect on the induction of γH2AX. Benzene failed to show a significant genotoxicity based on the γH2AX assay. However, hydroquinone (one of metabolites of benzene) showed a significant genotoxicity in vitro. Based on the dose-response of γH2AX and Hill model, the ability to induce DNA double-strand break can be evaluated as acrolein>formaldehyde>acetaldehyde>benzene...
July 18, 2017: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/28818492/-dexmedetomidine-preconditioning-protects-against-lipopolysaccharides-induced-injury-in-the-human-alveolar-epithelial-cells
#10
Lei Zhang, Xian-Jin Zhou, Li-Ying Zhan, Xiao-Jing Wu, Wen-Lan Li, Bo Zhao, Qing-Tao Meng, Zhong-Yuan Xia
BACKGROUND AND OBJECTIVES: Dexmedetomidine (DEX) has demonstrated the preconditioning effect and shown protective effects against organize injury. In this study, using A549 (human alveolar epithelial cell) cell lines, we investigated whether DEX preconditioning protected against acute lung injury (ALI) in vitro. METHODS: A549 were randomly divided into four groups (n=5): control group, DEX group, lipopolysaccharides (LPS) group, and D-LPS (DEX+LPS) group. Phosphate buffer saline (PBS) or DEX were administered...
August 14, 2017: Revista Brasileira de Anestesiologia
https://www.readbyqxmd.com/read/28818113/respiratory-syncytial-virus-rsv-entry-is-inhibited-by-serine-protease-inhibitor-aebsf-when-present-during-an-early-stage-of-infection
#11
Winke Van der Gucht, Annelies Leemans, Marjorie De Schryver, Annick Heykers, Guy Caljon, Louis Maes, Paul Cos, Peter L Delputte
BACKGROUND: Host proteases have been shown to play important roles in many viral activities such as entry, uncoating, viral protein production and disease induction. Therefore, these cellular proteases are putative targets for the development of antivirals that inhibit their activity. Host proteases have been described to play essential roles in Ebola, HCV, HIV and influenza, such that specific protease inhibitors are able to reduce infection. RSV utilizes a host protease in its replication cycle but its potential as antiviral target is unknown...
August 17, 2017: Virology Journal
https://www.readbyqxmd.com/read/28816439/1-3-dipolar-cycloaddition-reactions-for-the-synthesis-of-novel-oxindole-derivatives-and-their-cytotoxic-properties
#12
Prakash Rambhau Mali, Prashishkumar Kisan Shirsat, Navnath Bapurao Khomane, V Lakshama Nayak, Jagadeesh Babu Nanubolu, Harshadas Mitaram Meshram
The multicomponent reaction between isatin, amino acid, but-2-ynedioates and phenacyl bromide has been developed using microwave irradiation under catalyst and base free conditions in aqueous medium. This synthetic protocol is useful for the synthesis of various functionalized spirooxindole derivatives. This MCR exhibits a broad substrate scope with excellent yields and shorter reaction time. Additionally the synthesized spirooxindole derivatives were evaluated for their anticancer activity against three human cancer cell lines; MCF-7 (breast), A549 (lung) and Hela cervical...
August 17, 2017: ACS Combinatorial Science
https://www.readbyqxmd.com/read/28816372/in-vitro-antitubercular-activity-of-3-deoxysappanchalcone-isolated-from-the-heartwood-of-caesalpinia-sappan-linn
#13
Hoonhee Seo, Sukyung Kim, Hafij Al Mahmud, Md Imtiazul Islam, Kung-Woo Nam, Byung-Eui Lee, Hanna Lee, Myoung-Lae Cho, Heung-Mook Shin, Ho-Yeon Song
Responsible for nearly 1.5 million deaths every year, the infectious disease tuberculosis remains one of the most serious challenges to global health. The emergence of multidrug-resistant tuberculosis and, more recently, extensively drug-resistant tuberculosis poses a significant threat in our effort to control this epidemic. New drugs are urgently needed to combat the growing threat of antimicrobial resistance. To achieve this goal, we screened approximately 500 species of medicinal plant methanol extracts and their solvent partitioned fractions for potential inhibitors of Mycobacterium tuberculosis growth...
August 17, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28816009/protective-effect-of-atazanavir-sulfate-against-pulmonary-fibrosis-in-vivo-and-in-vitro
#14
Shina Song, Yunxia Ji, Guanghua Zhang, Xue Zhang, Bin Li, Defang Li, Wanglin Jiang
Atazanavir sulfate, an antiretroviral protease inhibitor, has been used to treat HIV/AIDS, but its ability to serve as an anti-pulmonary fibrosis (PF) agent remains unknown. In this study, the effects of atazanavir sulfate on various aspects of PF were examined and CoCl2 was used to induce the hypoxia-mimicking condition in vitro, including epithelial-mesenchymal transition (EMT) in A549 cells, endothelial-mesenchymal transition (EndMT) in human pulmonary microvascular endothelial cells (HPMECs), proliferation in human lung fibroblasts (HLF-1) and potential protective effects in human type I alveolar epithelial cells (AT I)...
August 16, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/28815927/metallofullerenol-inhibits-cellular-iron-uptake-by-inducing-transferrin-tetramerization
#15
Jinxia Li, Xueqing Xing, Baoyun Sun, Yuliang Zhao, Zhonghua Wu
Herein, A549 tumor cell proliferation was confirmed to be positively dependent on the concentration of Fe3+ or transferrin (Tf). Gd@C₈₂(OH)₂₂ or C₆₀(OH)₂₂ effectively inhibited the iron uptake and the subsequent proliferation of A549 cells. The conformation changes of Tf mixed with FeCl₃, GdCl₃, C₆₀(OH)₂₂ or Gd@C₈₂(OH)₂₂ were obtained by SAXS. The results demonstrate that Tf homodimers can be decomposed into monomers in the presence of FeCl₃, GdCl3 or C₆₀(OH)₂₂, but aggregated into tetramers in the presence of Gd@C₈₂(OH)₂₂...
August 16, 2017: Chemistry, An Asian Journal
https://www.readbyqxmd.com/read/28814929/in-vitro-cytotoxic-and-anticancer-effects-of-zamzam-water-in-human-lung-cancer-a594-cell-line
#16
Ulfat M Omar, Huda A Al Doghaither, Sawsan A Rahimulddin, Shiekhah M Al Zahrani, Ayat B Al-Ghafari
BACKGROUND: Zamzam water is naturally alkaline and rich in a variety of minerals which may represent a powerful tool for cancer therapy. In this research, the cytotoxic effects of Zamzam water were investigated in human lung cancer (A549) cell line and compared with human skin fibroblasts (HSF). METHODS: Two different preparations of Zamzam water were used: Z1, with pH adjusted to 7.2 and Z2, with no pH adjustment. The effects of both treatments on the morphology of the A549 and HSF cell lines were investigated...
May 2017: Malaysian Journal of Medical Sciences: MJMS
https://www.readbyqxmd.com/read/28813624/tp53-mutational-status-and-ros-effect-the-expression-of-the-survivin-associated-radio-adaptive-response
#17
Jeffrey S Murley, Richard C Miller, Ralph R Weichselbaum, David J Grdina
A survivin-associated radio-adaptive response, characterized by increased radiation resistance or sensitization, was induced by exposure to 5 mGy of ionizing radiation and was correlated to the TP53 mutational status of exposed cells. Ten human cancer lines were investigated: colorectal carcinomas HCT116 and RKO [TP53 wild-type (WT)] and their respective TP53 null isogenic lines; breast adenocarcinomas MCF7 (TP53 WT) and MDA-MB-231 (TP53 Mut); lung carcinomas A549 (TP53 WT) and NCI-H1975 (TP53 Mut); and pancreatic carcinomas Hs766T (TP53 WT) and Panc-1 (TP53 Mut)...
August 16, 2017: Radiation Research
https://www.readbyqxmd.com/read/28813465/long-term-persistent-infection-of-hpv-16-e6-up-regulate-sp1-and-htert-by-inhibiting-lkb1-in-lung-cancer-cells
#18
Jing-Hua Yang, Xiao-Yan Li, Xin Wang, Wei-Jian Hou, Xue-Shan Qiu, En-Hua Wang, Guang-Ping Wu
HPV 16 E6 upregulates hTERT expression in lung cancer cells. However, the underlying molecular mechanism is unclear. In this paper, E6, LKB1, SP1, and hTERT mRNA expression levels were detected in brushing cells of patients with lung cancer (n = 106) and with benign lung disease (n = 68) by qRT-PCR. The mRNA expression levels of E6, SP1, and hTERT were significantly increased in the malignant group compared with the benign group (P < 0.01). Conversely, the mRNA expression level of LKB1 was significantly decreased in the malignant group (P < 0...
2017: PloS One
https://www.readbyqxmd.com/read/28813147/synthesis-and-evaluation-of-asymmetric-acyclic-nucleoside-bisphosphonates-as-inhibitors-of-plasmodium-falciparum-and-human-hypoxanthine-guanine-xanthine-phosphoribosyltransferase
#19
Petr Špaček, Dianne T Keough, Marina Chavchich, Martin Dracinsky, Zlatko Janeba, Lieve Naesens, Michael D Edstein, Luke W Guddat, Dana Hocková
Acyclic nucleoside bisphosphonates (ANbPs) have previously been shown to be good inhibitors of human hypoxanthine-guanine phosphoribosyltransferase (HGPRT) and Plasmodium falciparum (Pf) hypoxanthine-guanine-xanthine phosphoribosyltransferase (PfHGXPRT). Based on this scaffold, a new series of ANbPs was synthesized. One of these new ANbPs, [3-(guanine-9-yl)-2-((2-phosphonoethoxy)methyl)propoxy]methylphosphonic acid, exhibited Ki values of 6 and 70 nM for human HGPRT and Pf HGXPRT, respectively. These low Ki values were achieved by inserting an extra carbon atom in the linker connecting the N9 atom of guanine to one of the phosphonate groups...
August 16, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28813052/mixed-ligand-iridium-iii-complexes-as-photodynamic-anticancer-agents
#20
Yue Zheng, Liang He, Dong-Yang Zhang, Cai-Ping Tan, Liang-Nian Ji, Zong-Wan Mao
Many phosphorescent iridium complexes are potent candidates as photodynamic therapeutic agents. In this work, a series of mixed-ligand phosphorescent iridium complexes (Ir1: [Ir(L1)(bpy)Cl](PF6)2; Ir2: [Ir(L1)(ppy)Cl](PF6); Ir3: [Ir(L2)(bpy)Cl](PF6)2; Ir4: [Ir(L2)(ppy)Cl](PF6). L1 = 2,6-bis(2-benzimidazolyl)pyridine; bpy = 2,2'-bipyridine; L2 = 2,6-bis(1-methyl-benzimidazol-2-yl)pyridine; ppy = 2-phenylpyridine) have been synthesized and characterized. These complexes display high luminescence quantum yields and long phosphorescence lifetimes...
August 16, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
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