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https://www.readbyqxmd.com/read/29792857/tgf-%C3%AE-plays-a-vital-role-in-triple-negative-breast-cancer-tnbc-drug-resistance-through-regulating-stemness-emt-and-apoptosis
#1
Xiaodan Xu, Lu Zhang, Xiaogang He, Ping Zhang, Caihong Sun, Xiaojun Xu, Yaojuan Lu, Feifei Li
Triple negative breast cancer (TNBC) is the most malignant subtype of breast cancer in which the cell surface lacks usual targets for drug to exhibit its effects. Epirubicin (Epi) is widely used for TNBC, but a substantial number of patients develop Epi resistance that is usually associated with poor prognosis. Transforming growth factor (TGF-β) is a multifunctional cytokine. In recent study, it appears that TGF-β influences the cancer stem cell population, thus, the drug resistance of cancer may also be affected...
May 21, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29792166/the-pdgfr%C3%AE-erk1-2-pathway-regulates-cdcp1-expression-in-triple-negative-breast-cancer
#2
Luca Forte, Federica Turdo, Cristina Ghirelli, Piera Aiello, Patrizia Casalini, Marilena Valeria Iorio, Elvira D'Ippolito, Patrizia Gasparini, Roberto Agresti, Beatrice Belmonte, Gabriella Sozzi, Lucia Sfondrini, Elda Tagliabue, Manuela Campiglio, Francesca Bianchi
BACKGROUND: CDCP1, a transmembrane protein with tumor pro-metastatic activity, was recently identified as a prognostic marker in TNBC, the most aggressive breast cancer subtype still lacking an effective molecular targeted therapy. The mechanisms driving CDCP1 over-expression are not fully understood, although several stimuli derived from tumor microenvironment, such as factors present in Wound Healing Fluids (WHFs), reportedly increase CDCP1 levels. METHODS: The expression of CDCP1, PDGFRβ and ERK1/2cell was tested by Western blot after stimulation of MDA-MB-231 cells with PDGF-BB and, similarly, in presence or not of ERK1/2 inhibitor in a panel of TNBC cell lines...
May 23, 2018: BMC Cancer
https://www.readbyqxmd.com/read/29791797/modulating-macrophage-polarization-through-ccr2-inhibition-and-multivalent-engagement
#3
Michael B Deci, Scott W Ferguson, Sydney L Scatigno, Juliane Nguyen
Excessive or prolonged recruitment of inflammatory monocytes to damaged tissue can significantly worsen patient outcomes. Monocytes migrate to sites of tissue inflammation in response to high local concentrations of CCL2, a chemokine that binds to and signals through the CCR2 receptor. While the role of CCR2 in cellular migration is well studied, it is unclear how CCR2 inhibition affects macrophage polarization and if multivalency can increase downstream signaling effects. Using affinity selection with a phage library, we identified a novel scFv (58C) that binds specifically and with high affinity to the N-terminal domain of CCR2 (KD = 59...
May 23, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29790797/curcumin-loaded-redox-responsive-mesoporous-silica-nanoparticles-for-targeted-breast-cancer-therapy
#4
Nana Li, Zhi Wang, Yongtai Zhang, Kai Zhang, Jianxu Xie, Ying Liu, Wansi Li, Nianping Feng
HYPOTHESIS: The antitumor applications of curcumin (CUR) are limited because of its low water solubility, poor stability, and low bioavailability. We developed novel nanocarrier systems for tumour targeting and controlled CUR release and evaluated their therapeutic efficacy. EXPERIMENTS: The surface of mesoporous silica nanoparticles (MSN) was modified with hyaluronan (HA) or polyethyleneimine-folic acid (PEI-FA) via disulfide bonds. The capacity of the resultant nanocarriers (MSN-HA and MSN-PEI-FA, respectively) for CUR delivery was evaluated in a breast cancer cell line and a mouse xenograft model...
May 23, 2018: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/29790302/bioactive-constituents-of-juniperus-turbinata-gussone-from-la-maddalena-archipelago
#5
A Venditti, F Maggi, L Quassinti, M Bramucci, G Lupidi, L Ornano, M Ballero, C Sanna, M Bruno, S Rosselli, A Bianco
In this paper is reported a comprehensive phytochemical study of Juniperus turbinata (Cupressaceae) collected from La Maddalena Archipelago (Sardinia, Italy). Both the essential oil and the ethanolic extract were analyzed. The essential oil appears to belong to a new chemotype compared to other Mediterranean juniper accessions, as it was favored by geographic isolation of the isles. It showed a low content of monoterpene hydrocarbons and α-terpineol, ent-manoyl oxide 1,10-di-epi-cubenol as the major constituents...
May 22, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29789259/synthesis-characterization-and-cytotoxicity-studies-of-1-2-3-triazoles-and-1-2-4-triazolo-1-5-a-pyrimidines-in-human-breast-cancer-cells
#6
Maryam Gilandoust, Kachigere B Harsha, Chakrabhavi Dhananjaya Mohan, Ainiah Rushdiana Raquib, Shobith Rangappa, Vijay Pandey, Peter E Lobie, Basappa, Kanchugarakoppal S Rangappa
Vascular endothelial growth factor (VEGF) and its receptor (VEGFR) is essential for physiological functions of tissues and neovasculature. VEGFR signaling is associated with the progression of pathological angiogenesis in various types of malignancies, making it an attractive therapeutic target in cancer treatment. In the present work, we report the synthesis of 1,4-disubstituted 1,2,3-triazoles and 1,2,4-triazolo[1, 5-a]pyrimidine derivatives via copper (I)-catalyzed azide-alkyne cycloaddition (CuAAC) reaction and screened for their anticancer activity against MCF7 cells...
May 9, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29789258/design-synthesis-and-biological-evaluation-of-artemisinin-derivatives-containing-fluorine-atoms-as-anticancer-agents
#7
Shu Li, Gongming Li, Xiaohong Yang, Qian Meng, Shuo Yuan, Yun He, Dequn Sun
Ten novel artemisinin derivatives containing fluorine atoms were synthesized and their structures were confirmed by 1 H NMR, 13 C NMR and HRMS technologies in this study. The in vitro cytotoxicity against U87MG, SH-SY5Y, MCF-7, MDA-MB-231, A549 and A375 cancer cell lines was evaluated by MTT assay. Compound 9j was the most potent anti-proliferative agent against the human breast cancer MCF-7 cells (IC50  = 2.1 μM). The mechanism of action of compound 9j was further investigated by analysis of cell apoptosis and cell cycle...
May 17, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29787758/tissue-factor-mediates-microvesicles-shedding-from-mda-mb-231-breast-cancer-cells
#8
Araci M da R Rondon, Vitor H de Almeida, Tainá Gomes, Bruno R F Verçoza, Renato S Carvalho, Sandra König, Juliany C F Rodrigues, Claudia Dos S Mermelstein, Henri H Versteeg, Robson Q Monteiro
Extracellular vesicles, such as microvesicles (MVs), were identified as important players in tumor progression and acquisition of an aggressive phenotype. Tissue factor (TF) is a transmembrane protein that initiates the blood coagulation cascade. In tumor cells, TF has been associated with aggressiveness and cancer progression. Previous studies demonstrate that TF is incorporated into MVs secreted by tumor cells; however, it is unknown whether TF is actively involved in the release of MVs. Here, we investigated the influence of TF expression on the release of MVs...
May 19, 2018: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/29786782/preclinical-impact-of-high-dose-intermittent-antiangiogenic-tyrosine-kinase-inhibitor-pazopanib-in-intrinsically-resistant-tumor-models
#9
Elaine Reguera-Nuñez, Shan Man, Ping Xu, Robert S Kerbel
Antiangiogenic tyrosine kinase inhibitors (TKIs) target vascular endothelial growth factor receptors and other receptor tyrosine kinases. As a result of toxicity, the clinical failures or the modest benefits associated with antiangiogenic TKI therapy may be related in some cases to suboptimal drug dosing and scheduling, thereby facilitating resistance. Most antiangiogenic TKIs, including pazopanib, are administered on a continuous daily basis. Here, instead, we evaluated the impact of increasing the dose and administering the drug intermittently...
May 21, 2018: Angiogenesis
https://www.readbyqxmd.com/read/29786642/determining-the-radiation-enhancement-effects-of-gold-nanoparticles-in-cells-in-a-combined-treatment-with-cisplatin-and-radiation-at-therapeutic-megavoltage-energies
#10
Celina Yang, Kyle Bromma, Wonmo Sung, Jan Schuemann, Devika Chithrani
Combined use of chemotherapy and radiation therapy is commonly used in cancer treatment, but the toxic effects on normal tissue are a major limitation. This study assesses the potential to improve radiation therapy when combining gold nanoparticle (GNP) mediated radiation sensitization with chemoradiation compared to chemoradiation alone. Incorporation of GNPs with 2 Gy, 6 MV (megavoltage) radiation resulted in a 19 ± 6% decrease in survival of MDA-MB-231 cells. Monte-Carlo simulations were performed to assess dosimetric differences in the presence of GNPs in radiation...
May 22, 2018: Cancers
https://www.readbyqxmd.com/read/29786602/microfluidic-system-for-modelling-3d-tumour-invasion-into-surrounding-stroma-and-drug-screening
#11
Zhichang Du, Shengli Mi, Xiaoman Yi, Yuanyuan Xu, Wei Sun
Tumour invasion into the surrounding stroma is a critical step in metastasis, and it is necessary to clarify the role of microenvironmental factors in tumour invasion. We present a microfluidic system that simulated and controlled multi-factors of the tumour microenvironment for three-dimensional (3D) assessment of tumour invasion into the stroma. The simultaneous, precise and continuous arrangement of two 3D matrices was visualised to observe the migration of cancer cell populations or single cells by transfecting cells with a fluorescent protein...
May 22, 2018: Biofabrication
https://www.readbyqxmd.com/read/29784502/corrigendum-to-cnot2-promotes-proliferation-and-angiogenesis-via-vegf-signaling-in-mda-mb-231-breast-cancer-cells-cancer-lett-412-2018-jan-1-88-98
#12
E J Sohn, D B Jung, H Lee, I Han, J Lee, H Lee, S H Kim
No abstract text is available yet for this article.
May 19, 2018: Cancer Letters
https://www.readbyqxmd.com/read/29783719/in-vitro-estrogenic-and-breast-cancer-inhibitory-activities-of-chemical-constituents-isolated-from-rheum-undulatum-l
#13
Dahae Lee, SeonJu Park, Sungyoul Choi, Seung Hyun Kim, Ki Sung Kang
We investigated the estrogenic and breast cancer inhibitory activities of chemical constituents isolated from Rhei undulati Rhizoma (roots of Rheum undulatum L.), which is used as a laxative, an anti-inflammatory, and an anti-blood stagnation agent. Estrogen-like activity was studied using the well characterized E-screen assay in estrogen receptor (ER)-positive MCF-7 cells. The mechanism underlying the breast cancer inhibitory activity of the compounds was studied using human ER-negative MDA-MB-231 and ER-positive MCF-7 cells...
May 18, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29783017/the-hydro-ethanolic-extract-of-acacia-seyal-mimosaceae-stem-barks-induced-death-in-an-er-negative-breast-cancer-cell-line-by-the-intrinsic-pathway-of-apoptosis-and-inhibited-cell-migration
#14
Stephane Zingue, Thomas Michel, Julia Cisilotto, Alain Brice Tueche, Derek Tantoh Ndinteh, Leônidas João Mello, Dieudonné Njamen, Tânia Beatriz Creczynski-Pasa
BACKGROUND: Despite the significant developments occurring in the treatment of cancer, it still remains the second deadly disease, responsible for 8.2 million deaths every year. Various natural substances have been studied for active molecules of tumor suppression in the past and the tropical flora, by its diversity, continues to provide new antitumor drugs. Acacia seyal is a plant used in Cameroonian traditional system to treat cancer. It exhibited cytotoxic effects towards human breast adenocarcinoma cells...
May 18, 2018: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29779937/estrogen-receptor-positive-breast-tumors-resist-chemotherapy-by-the-overexpression-of-p53-in-cancer-stem-cells
#15
Fatma Ashour, Mohammed H Awwad, Hayam E L Sharawy, Mohamed Kamal
BACKGROUND AND OBJECTIVES: Breast cancer (BC) is classified according to estrogen receptor (ER) status into ER+ and ER- tumors. ER+ tumors have a worse response to chemotherapy compared to ER- tumors. BCL-2, TP53, BAX and NF-ΚB are involved in drug resistance in the ER+ tumors. Recently it was shown that Cancer Stem Cells (CSCs) play an important role in drug resistance. In this study we tested the hypothesis that CSCs of the ER+ tumors resist drug through the overexpression of BCL-2, TP53, BAX and NF-ΚB...
May 17, 2018: Journal of the Egyptian National Cancer Institute
https://www.readbyqxmd.com/read/29778718/nimbolide-epigenetically-regulates-autophagy-and-apoptosis-in-breast-cancer
#16
Venkatesh Pooladanda, Soumya Bandi, Sandhya Rani Mondi, Krishna Mohan Gottumukkala, Chandraiah Godugu
Autophagy is a critical regulator of cellular homeostasis and its dysregulation often results in various disease manifestations, including cancer. Nimbolide, an active chemical constituent of neem (Azadirachta indica) exhibits potent anticancer effects. Although, nimbolide mediated apoptosis activation in breast cancer cells is well known. Nevertheless, its role in autophagy induction mechanism and epigenetic alteration is not explored previously. Our current study intended to bridge the gaps in the existing research by exploring the potential of nimbolide in inducing autophagy, which could counter regulate the transformations in breast cancer...
May 17, 2018: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/29778572/four-new-cinnamoyl-phloroglucinols-from-the-leaves-of-xanthostemon-chrysanthus
#17
Fen Liu, Wei-Jin Lu, Ni-Ping Li, Jiao-Wen Liu, Ju He, Wen-Cai Ye, Lei Wang
Four new cinnamoyl-phloroglucinols (1-4) were isolated from the leaves of Xanthostemon chrysanthus. Compounds 1 and 2 represent the first example of natural phloroglucinols with an oxazole unit. Their structures were elucidated on the basis of NMR spectroscopic data and single crystal X-ray diffraction. Compound 3 showed moderate cytotoxic activity against MDA-MB-231 and SGC-7901 cells with IC50 values of 25.26 ± 0.35 μM and 31.2 ± 0.94 μM, respectively.
May 17, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29777275/overexpression-of-abcb4-contributes-to-acquired-doxorubicin-resistance-in-breast-cancer-cells-in-vitro
#18
Jia-Feng Huang, Chun-Jie Wen, Guo-Zhi Zhao, Yi Dai, Ying Li, Lan-Xiang Wu, Hong-Hao Zhou
PURPOSE: Doxorubicin is one of the most active agents in the first-line therapy for metastatic breast cancer, but its utility is partially limited by the frequent emergence of doxorubicin resistance. In this study, we aimed to investigate the role of ATP-binding cassette sub-family B, member 4 (ABCB4) in acquired doxorubicin resistance in breast cancer cells, as well as its potential mechanism. METHODS: In doxorubicin-sensitive and -resistant breast cancer cell lines MCF-7 and MDA-MB-231, the expression levels of ABCB4 were detected using real-time quantitative PCR and Western blot analysis, the DNA methylation and histone acetylation status of ABCB4 gene were investigated by bisulfite-sequencing PCR (BSP) and chromatin immunoprecipitation (ChIP) assays, and the doxorubicin sensitivity and intracellular doxorubicin accumulation were observed using cell cytotoxicity assay and flow cytometry...
May 18, 2018: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/29777274/the-natural-agent-4-vinylphenol-targets-metastasis-and-stemness-features-in-breast-cancer-stem-like-cells
#19
Hoi-Wing Leung, Chun-Hay Ko, Grace Gar-Lee Yue, Ingrid Herr, Clara Bik-San Lau
BACKGROUND AND PURPOSE: Cancer stem-like cells (CSC) are regarded as the source of tumour origins, metastasis and drug resistance, and limits current treatment regimens. Previously, we reported the first study of the anti-angiogenic and anti-tumour activities of 4-vinylphenol. To further examine the therapeutic role of 4-vinylphenol, the inhibitory effects of 4-vinylphenol on cancer stemness, drug resistance and metastasis in breast cancer were investigated in the present study. STUDY DESIGN AND METHODS: We enriched parental MDA-MB-231 cells with CSCs in serum-free medium to give spheroids...
May 18, 2018: Cancer Chemotherapy and Pharmacology
https://www.readbyqxmd.com/read/29776832/an-sar-study-of-hydroxy-trifluoromethylpyrazolines-as-inhibitors-of-orai1-mediated-store-operated-ca-2-entry-in-mda-mb-231-breast-cancer-cells-using-a-convenient-fluorescence-imaging-plate-reader-assay
#20
Ralph J Stevenson, Iman Azimi, Jack U Flanagan, Marco Inserra, Irina Vetter, Gregory R Monteith, William A Denny
The proteins Orai1 and STIM1 control store-operated Ca2+ entry (SOCE) into cells. SOCE is important for migration, invasion and metastasis of MDA-MB-231 human triple negative breast cancer (TNBC) cells and has been proposed as a target for cancer drug discovery. Two hit compounds from a medium throughput screen, displayed encouraging inhibition of SOCE in MDA-MB-231 cells, as measured by a Fluorescence Imaging Plate Reader (FLIPR) Ca2+ assay. Following NMR spectroscopic analysis of these hits and reassignment of their structures as 5-hydroxy-5-trifluoromethylpyrazolines, a series of analogues was prepared via thermal condensation reactions between substituted acylhydrazones and trifluoromethyl 1,3-dicarbonyl arenes...
May 9, 2018: Bioorganic & Medicinal Chemistry
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