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https://www.readbyqxmd.com/read/29333049/marine-derived-fungi-extracts-enhance-the-cytotoxic-activity-of-doxorubicin-in-nonsmall-cell-lung-cancer-cells-a459
#1
Bruno Castro-Carvalho, Alice A Ramos, Maria Prata-Sena, Fernanda Malhão, Márcia Moreira, Daniela Gargiulo, Tida Dethoup, Suradet Buttachon, Anake Kijjoa, Eduardo Rocha
Background: Drug resistance is a major concern in the current chemotherapeutic approaches and the combination with natural compounds may enhance the cytotoxic effects of the anticancer drugs. Therefore, this study evaluated the cytotoxicity of crude ethyl extracts of six marine-derived fungi - Neosartorya tsunodae KUFC 9213 (E1), Neosartorya laciniosa KUFC 7896 (E2), Neosartorya fischeri KUFC 6344 (E3), Aspergillus similanensis KUFA 0013 (E4), Neosartorya paulistensis KUFC 7894 (E5), and Talaromyces trachyspermum KUFC 0021 (E6) - when combined with doxorubicin (Dox), in seven human cancer cell lines...
December 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/29327756/isomeric-and-hybrid-ferrocenyl-cyrhetrenyl-aldimines-a-new-family-of-multifunctional-compounds
#2
Juan Oyarzo, Alejandra Acuña, Hugo Klahn, Rodrigo Arancibia, Carlos P Silva, Ramón Bosque, Concepción López, Mercè Font-Bardía, Carme Calvis, Ramón Messeguer
The synthesis and characterization of two novel and isomeric hybrid ferrocenyl/cyrhetrenyl aldimines [(η5-C5H5)Fe{(η5-C5H4)-CH[double bond, length as m-dash]N-(η5-C5H4)}Re(CO)3] (1) and [(η5-C5H5)Fe{(η5-C5H4)-N[double bond, length as m-dash]CH-(η5-C5H4)}Re(CO)3] (2) are reported. Their X-ray crystal structures reveal that both adopt the E form. However, molecules of 1 and 2 differ in the relative arrangement of the "Fe(η5-C5H5)" and "Re(CO)3" units (anti in 1 and syn in 2). This affects the type of intermolecular interactions, the assembly of the molecules and therefore their crystal architecture...
January 12, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/29326016/synthesis-of-novel-6-substituted-amino-9-%C3%AE-d-ribofuranosyl-purine-analogs-and-their-bioactivities-on-human-epithelial-cancer-cells
#3
Meral Tuncbilek, Aslıgul Kucukdumlu, Ebru Bilget Guven, Duygu Altiparmak, Rengul Cetin-Atalay
New nucleoside derivatives with nitrogen substitution at the C-6 position were prepared and screened initially for their in vitro anticancer bioactivity against human epithelial cancer cells (liver Huh7, colon HCT116, breast MCF7) by the NCI-sulforhodamine B assay. N6-(4-trifluoromethylphenyl)piperazine analog (27) exhibited promising cytotoxic activity. The compound 27 was more cytotoxic (IC50 = 1-4 μM) than 5-FU, fludarabine on Huh7, HCT116 and MCF7 cell lines. The most potent nucleosides (11, 13, 16, 18, 19, 21, 27, 28) were further screened for their cytotoxicity in hepatocellular cancer cell lines...
January 2, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29323210/anticancer-potentiality-of-lignan-rich-fraction-of-six-flaxseed-cultivars
#4
Shahira M Ezzat, Samia A Shouman, Abeer Elkhoely, Yasmin M Attia, Mohamed S Elsesy, Amira S El Senousy, Mouchira A Choucry, Sabah H El Gayed, Abeer A El Sayed, Essam Abdel Sattar, Nebal El Tanbouly
The objective of our study is to highlight the therapeutic effect and mechanism of action by which purified Flaxseed hydrolysate (PFH) which is a lignan rich fraction exerts its anticancer activity on a human breast cancer cell line (T47D) and in mice bearing tumor. HPLC analysis of PFH of six flaxseed cultivars had shown that PFH of the cultivar Giza 9 (PFH-G9) contains the highest concentration of SDG (81.64 mg/g). The in vitro cytotoxic potentiality of PFH's of six flaxseed cultivars was screened against a panel of human cancer cell lines...
January 11, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29322918/a-linear-programming-computational-framework-integrates-phosphor-proteomics-and-prior-knowledge-to-predict-drug-efficacy
#5
Zhiwei Ji, Bing Wang, Ke Yan, Ligang Dong, Guanmin Meng, Lei Shi
BACKGROUND: In recent years, the integration of 'omics' technologies, high performance computation, and mathematical modeling of biological processes marks that the systems biology has started to fundamentally impact the way of approaching drug discovery. The LINCS public data warehouse provides detailed information about cell responses with various genetic and environmental stressors. It can be greatly helpful in developing new drugs and therapeutics, as well as improving the situations of lacking effective drugs, drug resistance and relapse in cancer therapies, etc...
December 21, 2017: BMC Systems Biology
https://www.readbyqxmd.com/read/29322784/bioinformatic-analysis-of-changes-in-rna-polymerase-ii-transcription-stimulated-by-estradiol-in-mcf7-cells
#6
J Wu, Y Cai, G Zhao
Estradiol (E2) is the most potent estrogen and RNA polymerase II (Pol II) regulates a great mass of gene expression. This study was designed to illustrate the mechanisms of estrogen-dependent human breast cancer (BC) through Pol II. ChIP-seq data, DNase-seq data and other sequencing data of human BC MCF-7 cells were downloaded from Gene Expression Omnibus database. Each of these datasets included one control and one E2 treated sample. Sequence alignment was performed and Pol II factor binding signal was determined...
2018: Neoplasma
https://www.readbyqxmd.com/read/29321644/cox-2-induces-oncogenic-micro-rna-mir655-in-human-breast-cancer
#7
Mousumi Majumder, Leanna Dunn, Ling Liu, Asma Hasan, Krista Vincent, Muriel Brackstone, David Hess, Peeyush K Lala
We show that Cyclooxygenase-2 over-expression induces an oncogenic microRNA miR655 in human breast cancer cells by activation of EP4. MiR655 expression positively correlated with COX-2 in genetically disparate breast cancer cell lines and increased in all cell lines when grown as spheroids, implicating its link with stem-like cells (SLCs). Ectopic miR655 over-expression in MCF7 and SKBR3 cells resulted in increased proliferation, migration, invasion, spheroid formation and Epithelial to Masenchymal transition (EMT)...
January 10, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29321207/aberrantly-high-expression-of-the-cub-and-zona-pellucida-like-domain-containing-protein-1-cuzd1-in-mammary-epithelium-leads-to-breast-tumorigenesis
#8
Janelle Mapes, Lavanya Anandan, Quanxi Li, Alison Neff, Charles V Clevenger, Indrani C Bagchi, Milan K Bagchi
The peptide hormone prolactin (PRL) and certain members of the epidermal growth factor (EGF) family play central roles in mammary gland development and physiology, and their dysregulation has been implicated in mammary tumorigenesis. Our recent studies have revealed that the CUB and zona pellucida-like domain-containing protein 1 (CUZD1) is a critical factor for PRL-mediated activation of the transcription factor STAT5 in mouse mammary epithelium. CUZD1 controls production of a specific subset of the EGF family growth factors and consequent activation of their receptors...
January 10, 2018: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29320403/bacillibactin-and-bacillomycin-analogues-with-cytotoxicities-against-human-cancer-cell-lines-from-marine-bacillus-sp-pku-ma00093-and-pku-ma00092
#9
Mengjie Zhou, Fawang Liu, Xiaoyan Yang, Jing Jin, Xin Dong, Ke-Wu Zeng, Dong Liu, Yingtao Zhang, Ming Ma, Donghui Yang
Nonribosomal peptides from marine Bacillus strains have received considerable attention for their complex structures and potent bioactivities. In this study, we carried out PCR-based genome mining for potential nonribosomal peptides producers from our marine bacterial library. Twenty-one "positive" strains were screened out from 180 marine bacterial strains, and subsequent small-scale fermentation, HPLC and phylogenetic analysis afforded Bacillus sp. PKU-MA00092 and PKU-MA00093 as two candidates for large-scale fermentation and isolation...
January 10, 2018: Marine Drugs
https://www.readbyqxmd.com/read/29316537/picolyl-amides-of-betulinic-acid-as-antitumor-agents-causing-tumor-cell-apoptosis
#10
Uladzimir Bildziukevich, Lucie Rárová, David Šaman, Zdeněk Wimmer
A series of picolyl amides of betulinic acid (3a-3c and 6a-6c) was prepared and subjected to the cytotoxicity screening tests. Structure-activity relationships studies resulted in finding differences in biological activity in dependence on o-, m- and p-substitution of the pyridine ring in the target amides, when cytotoxicity data of 3a-3c and 6a-6c were obtained and compared. The amides 3b and 3a displayed cytotoxicity (given in the IC50 values) in G-361 (0.5 ± 0.1 μM and 2.4 ± 0.0 μM, respectively), MCF7 (1...
January 4, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29316360/a-novel-prodrug-of-a-%C3%AE-glutamylcyclotransferase-inhibitor-suppresses-cancer-cell-proliferation-in%C3%A2-vitro-and-inhibits-tumor-growth-in-a-xenograft-mouse-model-of-prostate-cancer
#11
Hiromi Ii, Taku Yoshiya, Susumu Nakata, Keiko Taniguchi, Koushi Hidaka, Shugo Tsuda, Masayoshi Mochizuki, Yuji Nishiuchi, Yuko Tsuda, Kosei Ito, Susumu Kageyama, Tatsuhiro Yoshiki
γ-Glutamylcyclotransferase (GGCT) depletion inhibits cancer cell proliferation. However, whether the enzymatic activity of GGCT is critical for the regulation of cancer cell growth remains unclear. In this study, a novel diester-type cell-permeable prodrug, pro-GA, was developed based on the structure of N-glutaryl-l-alanine (GA), by structure optimization using temporary fluorophore-tagged prodrug candidates. The antiproliferative activity of pro-GA was demonstrated using GGCT-overexpressing NIH-3T3 cells and human cancer cells including MCF7, HL-60, and PC3 cells...
January 9, 2018: ChemMedChem
https://www.readbyqxmd.com/read/29316252/manganese-12-acetate-suppresses-the-migration-invasion-and-epithelial-mesenchymal-transition-by-inhibiting-wnt-%C3%AE-catenin-and-pi3k-akt-signaling-pathways-in-breast-cancer-cells
#12
Hongping Ju, Yongxia Li, Xiqian Xing, Xisong Miao, Yunping Feng, Yunhui Ren, Jing Qin, Dian Liu, Zihao Chen, Zhaoyu Yang
BACKGROUND: Breast cancer is the leading cause of cancer-related death in the world, and it is of great value to reveal the molecular mechanisms of breast cancer progression and develop new therapeutic targets. METHODS: Transwell assay is used to analyze the migration and invasion of breast cancer cells. Real-time PCR and western blotting assay are applied to detect the expression levels of epithelial-mesenchymal transition markers and the key members of Wnt/β-catenin and PI3K/AKT signaling pathways...
January 8, 2018: Thoracic Cancer
https://www.readbyqxmd.com/read/29312586/glucose-impairs-tamoxifen-responsiveness-modulating-connective-tissue-growth-factor-in-breast-cancer-cells
#13
Maria Rosaria Ambrosio, Vittoria D'Esposito, Valerio Costa, Domenico Liguoro, Francesca Collina, Monica Cantile, Nella Prevete, Carmela Passaro, Giusy Mosca, Michelino De Laurentiis, Maurizio Di Bonito, Gerardo Botti, Renato Franco, Francesco Beguinot, Alfredo Ciccodicola, Pietro Formisano
Type 2 diabetes and obesity are negative prognostic factors in patients with breast cancer (BC). We found that sensitivity to tamoxifen was reduced by 2-fold by 25 mM glucose (High Glucose; HG) compared to 5.5 mM glucose (Low Glucose; LG) in MCF7 BC cells. Shifting from HG to LG ameliorated MCF7 cell responsiveness to tamoxifen. RNA-Sequencing of MCF7 BC cells revealed that cell cycle-related genes were mainly affected by glucose. Connective Tissue Growth Factor (CTGF) was identified as a glucose-induced modulator of cell sensitivity to tamoxifen...
December 12, 2017: Oncotarget
https://www.readbyqxmd.com/read/29312577/nitric-oxide-is-cytoprotective-to-breast-cancer-spheroids-vulnerable-to-estrogen-induced-apoptosis
#14
Yana Shafran, Naomi Zurgil, Orit Ravid-Hermesh, Maria Sobolev, Elena Afrimzon, Yaron Hakuk, Asher Shainberg, Mordechai Deutsch
Estrogen-induced apoptosis has become a successful treatment for postmenopausal metastatic, estrogen receptor-positive breast cancer. Nitric oxide involvement in the response to this endocrine treatment and its influence upon estrogen receptor-positive breast cancer progression is still unclear. Nitric oxide impact on the MCF7 breast cancer line, before and after estrogen-induced apoptosis, was investigated in 3D culture systems using unique live-cell imaging methodologies. Spheroids were established from MCF7 cells vulnerable to estrogen-induced apoptosis, before and after exposure to estrogen...
December 12, 2017: Oncotarget
https://www.readbyqxmd.com/read/29310316/fluorescein-diacetate-fda-and-its-analogue-as-substrates-for-pi-class-glutathione-s-transferase-gstp1-and-their-biological-application
#15
Yuuta Fujikawa, Taiki Nampo, Masaya Mori, Manami Kikkawa, Hideshi Inoue
Pi class glutathione S-transferase (GSTP1) is highly expressed in various cancerous cells and pre-neoplastic legions, where it is involved in apoptotic resistance or metabolism of several anti-tumour chemotherapeutics. Therefore, GSTP1 is a marker of malignant and pre-malignant cells and is a promising target for visualization and drug development. Here we demonstrate that fluorescein diacetate (FDA), a fluorescent probe used for vital staining, is a fluorescently activated by esterolytic activity of human GSTP1 (hGSTP1) selectively among various cytosolic GSTs...
March 1, 2018: Talanta
https://www.readbyqxmd.com/read/29304175/genome-scale-metabolic-models-as-tools-for-drug-design-and-personalized-medicine
#16
Vytautas Raškevičius, Valeryia Mikalayeva, Ieva Antanavičiūtė, Ieva Ceslevičienė, Vytenis Arvydas Skeberdis, Visvaldas Kairys, Sergio Bordel
In this work we aim to show how Genome Scale Metabolic Models (GSMMs) can be used as tools for drug design. By comparing the chemical structures of human metabolites (obtained using their KEGG indexes) and the compounds contained in the DrugBank database, we have observed that compounds showing Tanimoto scores higher than 0.9 with a metabolite, are 29.5 times more likely to bind the enzymes metabolizing the considered metabolite, than ligands chosen randomly. By using RNA-seq data to constrain a human GSMM it is possible to obtain an estimation of its distribution of metabolic fluxes and to quantify the effects of restraining the rate of chosen metabolic reactions (for example using a drug that inhibits the enzymes catalyzing the mentioned reactions)...
2018: PloS One
https://www.readbyqxmd.com/read/29300112/zoledronic-acid-overcomes-chemoresistance-by-sensitizing-cancer-stem-cells-to-apoptosis
#17
H Rouhrazi, N Turgan, G Oktem
Unlike low tumorigenic bulk tumor cells (non-CSCs), cancer stem cells (CSCs) are a subset of tumor cells that can self-renew and differentiate into different cancer subtypes. CSCs are considered responsible for tumor recurrence, distant metastasis, angiogenesis, and drug or radiation resistance. CSCs also are resistant to apoptosis. Zoledronic acid (ZA) is a third generation bisphosphonate that reduces cell proliferation and exhibits anti-tumor effects by inducing cell death in some malignancies; however, the effects of ZA on CSCs are unclear...
January 4, 2018: Biotechnic & Histochemistry: Official Publication of the Biological Stain Commission
https://www.readbyqxmd.com/read/29298541/chitosan-poly-lactic-acid-coated-piceatannol-nanoparticles-exert-an-in-vitro-apoptosis-activity-on-liver-lung-and-breast-cancer-cell-lines
#18
Jeevitha Dhanapal, Malathy Balaraman Ravindrran
The aim of the study was to synthesize nanoparticles (NPs) with chitosan (CS), and poly (lactic acid) (PLA) as a carrier for the drug piceatannol (PIC). The synthesized nanoparticles form the composite of polymeric-drug nanoparticles (CS/PLA-PIC NPs) by dropping method. The preliminary and stability studies were determined for the polymers drug-loading capacity and encapsulation efficiencies. The in vitro drug release study showed that NPs provided a continuous release of the entrapped PIC. The NPs found to be a good scavenger for DPPH, SOD and NO radicals...
January 3, 2018: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/29295867/hexose-6-phosphate-dehydrogenase-controls-cancer-cell-proliferation-and-migration-through-pleiotropic-effects-on-the-unfolded-protein-response-calcium-homeostasis-and-redox-balance
#19
Maria Tsachaki, Natasa Mladenovic, Hana Štambergová, Julia Birk, Alex Odermatt
Hexose-6-phosphate dehydrogenase (H6PD) produces reduced NADPH in the endoplasmic reticulum (ER) lumen. NADPH constitutes a cofactor for many reducing enzymes, and its inability to traverse biologic membranes makes in situ synthesis of NADPH in the ER lumen indispensable. The H6PD gene is amplified in several types of malignancies, and earlier work pointed toward a potential involvement of the enzyme in cancer cell growth. In the present study, we demonstrated a pivotal role of H6PD in proliferation and migratory potential of 3 human breast cancer cell lines...
January 2, 2018: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
https://www.readbyqxmd.com/read/29291446/design-synthesis-and-biological-evaluation-of-novel-combretastatin-a-4-thio-derivatives-as-microtubule-targeting-agents
#20
Tomasz Stefański, Renata Mikstacka, Rafał Kurczab, Zbigniew Dutkiewicz, Małgorzata Kucińska, Marek Murias, Małgorzata Zielińska-Przyjemska, Michał Cichocki, Anna Teubert, Mariusz Kaczmarek, Adam Hogendorf, Stanisław Sobiak
A series of novel combretastatin A-4 (CA-4) thio derivatives containing different molecular cores, namely α-phenylcinnamic acids (core 1), (Z)-stilbenes (core 2), 4,5-disubstituted oxazoles (core 3), and 4,5-disubstituted N-methylimidazoles (core 4), as cis-restricted analogues were designed and synthesized. They were selected with the use of a parallel virtual screening protocol including the generation of a virtual combinatorial library based on an elaborated synthesis protocol of CA-4 analogues. The selected compounds were evaluated for antiproliferative activity against a panel of six human cancer cell lines (A431, HeLa, MCF7, MDA-MB-231, A549 and SKOV) and two human non-cancer cell lines (HaCaT and CCD39Lu)...
December 12, 2017: European Journal of Medicinal Chemistry
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