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https://www.readbyqxmd.com/read/27934321/copper-ii-complexes-of-phenanthroline-and-histidine-containing-ligands-synthesis-characterization-and-evaluation-of-their-dna-cleavage-and-cytotoxic-activity
#1
Sílvia M G Leite, Luís M P Lima, Sofia Gama, Filipa Mendes, Maylis Orio, Isabel Bento, António Paulo, Rita Delgado, Olga Iranzo
Copper(II) complexes have been intensely investigated in a variety of diseases and pathological conditions due to their therapeutic potential. The development of these complexes requires a good knowledge of metal coordination chemistry and ligand design to control species distribution in solution and tailor the copper(II) centers in the right environment for the desired biological activity. Herein we present the synthesis and characterization of two ligands HL1 and H2L2 containing a phenanthroline unit (phen) attached to the amino group of histidine (His)...
November 21, 2016: Inorganic Chemistry
https://www.readbyqxmd.com/read/27928955/discovery-of-new-aminosubstituted-pyrrolopyrimidines-with-antiproliferative-activity-against-breast-cancer-cells-and-investigation-of-their-effect-towards-the-pi3k%C3%AE-enzyme
#2
Konstantinos Daniilides, Nikolaos Lougiakis, Thomas Evangelidis, Ioannis K Kostakis, Nicole Pouli, Panagiotis Marakos, Emmanuel Mikros, Alexios-Leandros Skaltsounis, Stéphane Bach, Blandine Baratte, Sandrine Ruchaud, Valia Karamani, Alexandra Papafotika, Savvas Christoforidis, Orestis Argyros, Eva Kouvari, Constantin Tamvakopoulos
A series of novel 2,4-diaminosubstituted pyrrolo[3,2-d]pyrimidines was synthesized together with their corresponding 7-phenyl or 7-isopropyl counterparts. Among the target derivatives, the 7-substituted analogues exhibited interesting cytotoxic activity against a panel of PI3Kα related human breast cancer cell lines, namely MCF7, T47D, MDA-MB-231 and HCC1954. Selected compounds were tested for potential PI3Kα inhibitory activity as well as for their cytotoxic effect in prostate cancer cell lines (DU145 and PC3)...
December 7, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27927249/the-af-1-deficient-estrogen-receptor-er%C3%AE-46-isoform-is-frequently-expressed-in-human-breast-tumors
#3
Elodie Chantalat, Frédéric Boudou, Henrik Laurell, Gaëlle Palierne, René Houtman, Diana Melchers, Philippe Rochaix, Thomas Filleron, Alexandre Stella, Odile Burlet-Schiltz, Anne Brouchet, Gilles Flouriot, Raphaël Métivier, Jean-François Arnal, Coralie Fontaine, Françoise Lenfant
BACKGROUND: To date, all studies conducted on breast cancer diagnosis have focused on the expression of the full-length 66-kDa estrogen receptor alpha (ERα66). However, much less attention has been paid to a shorter 46-kDa isoform (ERα46), devoid of the N-terminal region containing the transactivation function AF-1. Here, we investigated the expression levels of ERα46 in breast tumors in relation to tumor grade and size, and examined the mechanism of its generation and its specificities of coregulatory binding and its functional activities...
December 7, 2016: Breast Cancer Research: BCR
https://www.readbyqxmd.com/read/27922047/new-arylated-benzo-h-quinolines-induce-anti-cancer-activity-by-oxidative-stress-mediated-dna-damage
#4
Dharmendra K Yadav, Reeta Rai, Naresh Kumar, Surjeet Singh, Sanjeev Misra, Praveen Sharma, Priyanka Shaw, Horacio Pérez-Sánchez, Ricardo L Mancera, Eun Ha Choi, Mi-Hyun Kim, Ramendra Pratap
The anti-cancer activity of the benzo[h]quinolines was evaluated on cultured human skin cancer (G361), lung cancer (H460), breast cancer (MCF7) and colon cancer (HCT116) cell lines. The inhibitory effect of these compounds on the cell growth was determined by the MTT assay. The compounds 3e, 3f, 3h and 3j showed potential cytotoxicity against these human cancer cell lines. Effect of active compounds on DNA oxidation and expression of apoptosis related gene was studied. We also developed a quantitative method to measure the activity of cyclin-dependent kinases-2 (CDK2) by western blotting in the presence of active compound...
December 6, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27921518/increased-radio-toxicity-in-two-cancerous-cell-lines-irradiated-by-low-and-high-energy-photons-in-the-presence-of-thio-glucose-bound-gold-nanoparticles
#5
Shokouhozaman Soleymanifard, Atefeh Rostami, Seyed Amir Aledavood, Maryam Moghadam Matin, Ameneh Sazgarnia
PURPOSE: Gold nanoparticles modified by thio-glucose have been believed to increase the toxicity of radiotherapy in human malignant cells. We report the effect of thio-glucose-bound gold nanoparticles (Glu-G nanoparticles), 16 nm in size, on two human lung (QU-DB) and breast (MCF7) cancer cell lines combined with kilo and megavoltage X-rays. MATERIALS AND METHODS: The shape and surface characteristics, the size distribution and light absorption spectrum of the prepared nanoparticles were measured by transmission electron microscopy, dynamic light scattering, and Ultraviolet-Visible spectrophotometry, respectively...
December 6, 2016: International Journal of Radiation Biology
https://www.readbyqxmd.com/read/27914571/evaluating-the-anticancer-activity-and-nanoparticulate-nature-of-homeopathic-preparations-of-terminalia-chebula
#6
Kirtee Wani, Nilesh Shah, Asmita Prabhune, Arun Jadhav, Prabhakar Ranjekar, Ruchika Kaul-Ghanekar
BACKGROUND: Breast cancer is the most common cancer diagnosed among women and is the second leading cause of cancer death. Homeopathic medicines are part of the alternative medicines that are given as a supportive therapy in breast cancer. The objective of this study was to investigate the anticancer activity of commercially available homeopathic preparations of Terminalia chebula (TC) and evaluate their nanoparticulate nature. METHODS: Mother tincture (MT) and other homeopathic preparations (3X, 6C and 30C) of TC were tested for their effect on the viability of breast cancer (MDAMB231 and MCF7) and non-cancerous (HEK 293) cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay...
November 2016: Homeopathy: the Journal of the Faculty of Homeopathy
https://www.readbyqxmd.com/read/27912880/combination-of-baicalein-and-10-hydroxy-camptothecin-exerts-remarkable-synergetic-anti-cancer-effects
#7
Qin Tang, Fangling Ji, Wenhui Sun, Jingyun Wang, Jianli Guo, Lianying Guo, Yachen Li, Yongming Bao
BACKGROUND: 10-Hydroxy camptothecin (HCPT), a naturally occurring alkaloid, is a clinical drug for cancer chemotherapy. Baicalein (BA) is a flavonoid extracted from the root of Scutellaria baicalensis. The synergistic anti-cancer effect of BA and HCPT has not been reported. PURPOSE: To explore whether and how BA enhances the anti-cancer effect of HCPT in BGC823 cells. METHODS: Cell viability was measured by MTT assay. Apoptosis and cell cycle were analyzed through flow cytometry and western blotting analysis...
December 15, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/27903409/synthesis-of-novel-substituted-pyrimidine-derivatives-bearing-a-sulfamide-group-and-their-in-vitro-cancer-growth-inhibition-activity
#8
Carole-Anne Lefebvre, Elsa Forcellini, Sophie Boutin, Marie-France Côté, René C-Gaudreault, Patrick Mathieu, Patrick Lagüe, Jean-François Paquin
The synthesis of two series of novel substituted pyrimidine derivatives bearing a sulfamide group have been described and their in vitro cancer growth inhibition activities have been evaluated against three human tumour cell lines (HT-29, M21, and MCF7). In general, growth inhibition activity has been enhanced by the introduction of a bulky substituent on the aromatic ring with the best compound having GI50<6μM for all the human tumour cell lines. The MCF7 selective compounds were evaluated on four additional human invasive breast ductal carcinoma cell lines (MDA-MB-231, MDA-MB-468, SKBR3, and T47D) and were selective against T47D cell line in all cases except one, suggesting a potential antiestrogen activity...
November 19, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27901111/optogenetic-clustering-of-cnk1-reveals-mechanistic-insights-in-raf-and-akt-signalling-controlling-cell-fate-decisions
#9
Adrian Fischer, Bettina Warscheid, Wilfried Weber, Gerald Radziwill
Scaffold proteins such as the multidomain protein CNK1 orchestrate the signalling network by integrating and controlling the underlying pathways. Using an optogenetic approach to stimulate CNK1 uncoupled from upstream effectors, we identified selective clusters of CNK1 that either stimulate RAF-MEK-ERK or AKT signalling depending on the light intensity applied. OptoCNK1 implemented in MCF7 cells induces differentiation at low light intensity stimulating ERK activity whereas stimulation of AKT signalling by higher light intensity promotes cell proliferation...
November 30, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27900058/effect-of-surgical-wound-fluids-after-intraoperative-electron-radiotherapy-on-the-cancer-stem-cell-phenotype-in-a-panel-of-human-breast-cancer-cell-lines
#10
Karolina Zaleska, Wiktoria Maria Suchorska, Anna Przybyła, Dawid Murawa
The wound healing process after surgery alters the area surrounding the original tumor and around the scar, and the modified microenvironment is more favorable for tumor recurrence. Intraoperative radiotherapy (IORT) is one of the more novel strategies in breast cancer (BC) treatment. Irradiation during surgery has effects on the tumor microenvironment, abrogating the proliferative cascade induced by surgical wound healing. The aim of the present study was to determine the effect of surgical wound fluids from IOERT treatment (RT-WF) compared with wound fluids from conservative-breast surgery only (WF) on the cancer stem cell phenotype in a panel of BC cell lines...
November 2016: Oncology Letters
https://www.readbyqxmd.com/read/27899033/novel-antibacterial-polymeric-nanocomposite-for-smart-co-delivery-of-anticancer-drugs
#11
Elham Zakerzadeh, Effat Alizadeh, Hossein Samadi Kafil, Azad Mohammad Hassanzadeh, Roya Salehi, Mehrdad Mahkam
Here a novel antibacterial nanocomposite was developed for combination cancer therapy. The synthesized nanocarrier was characterized by FTIR, (1)H NMR, thermogravimetric analysis (TGA), and FESEM-EDX. Its antibacterial activity was assessed by determining minimum inhibitory concentration (MIC) values. Doxorubicin (DOX) and methotrexate (MTX) conjugation with nanocarrier sustained the release of both drugs with apparent pH-triggered manner. Co-administration of DOX with MTX leads to an efficient anticancer performance to MCF7 cell lines verified by qRT-PCR and MTT assay tests...
November 29, 2016: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/27895744/identification-of-targets-of-mirna-221-and-mirna-222-in-fulvestrant-resistant-breast-cancer
#12
Pengfei Liu, Manna Sun, Wenhua Jiang, Jinkun Zhao, Chunyong Liang, Huilai Zhang
The present study aimed to identify the differentially expressed genes (DEGs) regulated by microRNA (miRNA)-221 and miRNA-222 that are associated with the resistance of breast cancer to fulvestrant. The GSE19777 transcription profile was downloaded from the Gene Expression Omnibus database, and includes data from three samples of antisense miRNA-221-transfected fulvestrant-resistant MCF7-FR breast cancer cells, three samples of antisense miRNA-222-transfected fulvestrant-resistant MCF7-FR cells and three samples of control inhibitor (green fluorescent protein)-treated fulvestrant-resistant MCF7-FR cells...
November 2016: Oncology Letters
https://www.readbyqxmd.com/read/27895513/tumor-suppressor-ing4-inhibits-estrogen-receptor-activity-in-breast-cancer-cells
#13
Madeline M Keenen, Suwon Kim
Resistance to antiestrogen therapy remains a significant problem in breast cancer. Low expression of inhibitor of growth 4 (ING4) in primary tumors has been correlated with increased rates of recurrence in estrogen receptor-positive (ER+) breast cancer patients, suggesting a role for ING4 in ER signaling. This study provides evidence that ING4 inhibits ER activity. ING4 overexpression increased the sensitivity of T47D and MCF7 ER+ breast cancer cells to hormone deprivation. ING4 attenuated maximal estrogen-dependent cell growth without affecting the dose-response of estrogen...
2016: Breast Cancer: Targets and Therapy
https://www.readbyqxmd.com/read/27892708/antitumoral-effects-of-d-fraction-from-grifola-frondosa-maitake-mushroom-in-breast-cancer
#14
Eliana Noelia Alonso, María Julia Ferronato, Norberto Ariel Gandini, María Eugenia Fermento, Diego Javier Obiol, Alejandro López Romero, Julián Arévalo, María Emilia Villegas, María Marta Facchinetti, Alejandro Carlos Curino
D-Fraction is protein-bound β-1,6 and β-1,3 glucans (proteoglucan) extracted from the edible and medicinal mushroom Grifola frondosa (Maitake). The antitumoral effect of D-Fraction has long been exclusively attributed to their immunostimulatory capacity. However, in recent years increasing evidence showed that D-Fraction directly affects the viability of canine and human tumor cells, independent of the immune system. Previously, we have reported that D-Fraction modulates the expression of genes associated with cell proliferation, cell death, migration, invasion, and metastasis in MCF7 human breast cancer cells...
November 28, 2016: Nutrition and Cancer
https://www.readbyqxmd.com/read/27889857/accurate-control-of-17%C3%AE-estradiol-long-term-release-increases-reliability-and-reproducibility-of-preclinical-animal-studies
#15
Céline Gérard, Anne Gallez, Charline Dubois, Pierre Drion, Philippe Delahaut, Etienne Quertemont, Agnès Noël, Christel Pequeux
Estrogens are the subject of intensive researches aiming to elucidate their mechanism of action on the various tissues they target and especially on mammary gland and breast cancer. The use of ready-to-use slow releasing devices to administer steroids, especially estrogens, to small experimental animals remains the method of choice in terms of animal well-being and of safety for both the researcher and the animal. In this study, we evaluated and compared, in vitro and in vivo, the release kinetic of estradiol (E2) over sixty days from two different slow-releasing systems: the matrix pellet (MP) and the reservoir implant (RI)...
November 26, 2016: Journal of Mammary Gland Biology and Neoplasia
https://www.readbyqxmd.com/read/27889762/evaluation-of-isolation-methods-for-circulating-tumor-cells-ctcs
#16
Galatea Kallergi, Eleni Politaki, Saad Alkahtani, Christos Stournaras, Vassilis Georgoulias
BACKGROUND: Detection of CTCs is a poor prognostic factor for many cancer types; however, their very low frequency represents an obstacle for their detection. The objective of the current study was to compare the performance of commonly used methods for CTCs isolation. METHODS: The evaluated methods using spiking experiments of MCF7, SKBR3 and MDA MB-231 breast cancer cell lines were (i) ficoll density gradient separation (DGS), (ii) red blood cell lysis (Erythrolysis) isolation, (iii) positive immunomagnetic selection (EpCAM Dynal beads), (iv) two different negative immunomagnetic separation systems (Dynal vs Miltenyi CD45 beads) as well as (v) the Cell Search platform and (vi) the ISET system...
November 25, 2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27887573/in-vitro-function-of-upstream-visfatin-polymorphisms-that-are-associated-with-adverse-cardiometabolic-parameters-in-obese-children
#17
Delicia Shu Qin Ooi, Siong Gim Ong, Chew Kiat Heng, Kah Yin Loke, Yung Seng Lee
BACKGROUND: Visfatin is an adipokine associated with glucose and lipid metabolism. We previously reported two visfatin upstream single nucleotide polymorphisms (SNPs), c.-3187G > A (rs11977021) and c.-1537C > T (rs61330082), which were in perfect linkage disequilibrium, in a Singaporean cohort of severely obese children and are associated with visfatin level and adverse cardiometabolic parameters. We aim to functionally characterize the effect of c.-3187G > A and c...
November 25, 2016: BMC Genomics
https://www.readbyqxmd.com/read/27883910/influence-of-reduced-glutathione-on-end-joining-of-dna-double-strand-breaks-cytogenetical-and-molecular-approach
#18
Nitin Ghoshal, Sheetal Sharma, Atanu Banerjee, Sillarine Kurkalang, Sathees C Raghavan, Anupam Chatterjee
Radiation induced DNA double-strand breaks (DSB) are the major initial lesions whose misrejoining may lead to exchange aberrations. However, the role of glutathione (GSH), a major cellular thiol, in regulating cell's sensitivity to DNA damaging agents is not well understood. Influence of endogenous GSH on the efficiency of X-rays and bleomycin (Blem) induced DNA DSBs end-joining has been tested here cytogenetically, in human lymphocytes and Hct116 cells. In another approach, oligomeric DNA (75bp) containing 5'-compatible and non-compatible overhangs mimicking the endogenous DSB were for rejoining in presence of cell-free extracts from cells having different endogenous GSH levels...
November 9, 2016: Mutation Research
https://www.readbyqxmd.com/read/27876144/in-tip-nanoreactors-for-cancer-cells-proteome-profiling
#19
Ling Yan, Liang Qiao, Ji Ji, Yixin Li, Xuefei Yin, Ling Lin, Xiaohui Liu, Jun Yao, Yi Wang, Bin Liu, Kun Qian, Baohong Liu, Pengyuan Yang
Mass spectrometry (MS)-based proteome profiling is essential for molecular diagnostics in modern biomedical study. To date, sample preparation including protein extraction and proteolysis is still very challenging and lack of efficiency. Recently tips-based sample preparation protocols exhibit strong potentials to achieve the goal of "a proteome in an hour". However, in-tip proteolysis is still rarely reported and far from ideal for dealing with complex bio-samples. In this work, nanoreactors encapsulated micropipette tips were demonstrated as high performance devices for fast (∼minutes) and multiplexing proteolysis to assist the profiling of cancer cells proteome...
January 1, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/27872854/identification-of-novel-inhibitors-against-coactivator-associated-arginine-methyltransferase-1-based-on-virtual-screening-and-biological-assays
#20
Fei Ye, Weiyao Zhang, Wenchao Lu, Yiqian Xie, Hao Jiang, Jia Jin, Cheng Luo
Overexpression of coactivator associated arginine methyltransferase 1 (CARM1), a protein arginine N-methyltransferase (PRMT) family enzyme, is associated with various diseases including cancers. Consequently, the development of small-molecule inhibitors targeting PRMTs has significant value for both research and therapeutic purposes. In this study, together with structure-based virtual screening with biochemical assays, two compounds DC_C11 and DC_C66 were identified as novel inhibitors of CARM1. Cellular studies revealed that the two inhibitors are cell membrane permeable and effectively blocked proliferation of cancer cells including HELA, K562, and MCF7...
2016: BioMed Research International
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