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https://www.readbyqxmd.com/read/28340413/design-synthesis-and-biological-evaluation-of-novel-coumarin-based-benzamides-as-potent-histone-deacetylase-inhibitors-and-anticancer-agents
#1
Tooba Abdizadeh, Mohammad Reza Kalani, Khalil Abnous, Zahra Tayarani-Najaran, Bibi Zahra Khashyarmanesh, Rahman Abdizadeh, Razieh Ghodsi, Farzin Hadizadeh
Histone deacetylases (HDACs) are attractive therapeutic targets for the treatment of cancer and other diseases. It has four classes (I-IV), among them especially class I isozyme are involved in promoting tumor cells proliferation, angiogenesis, differentiation, invasion and metastasis and also viable targets for cancer therapeutics. A novel series of coumarin-based benzamides was designed and synthesized as HDAC inhibitors. The cytotoxic activity of the synthesized compounds (8a-u) was evaluated against six human cancer cell lines including HCT116, A2780, MCF7, PC3, HL60 and A549 and a single normal cell line (Huvec)...
March 18, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28339031/p53-inducible-long-non-coding-rna-picart1-mediates-cancer-cell-proliferation-and-migration
#2
Yu Cao, Minglin Lin, Yiwen Bu, Hongyan Ling, Yingchun He, Chenfei Huang, Yi Shen, Bob Song, Deliang Cao
Long non-coding RNAs (lncRNAs) function in the development and progression of cancer, but only a small portion of lncRNAs have been characterized to date. A novel lncRNA transcript, 2.53 kb in length, was identified by transcriptome sequencing analysis, and was named p53-inducible cancer-associated RNA transcript 1 (PICART1). PICART1 was found to be upregulated by p53 through a p53-binding site at -1808 to -1783 bp. In breast and colorectal cancer cells and tissues, PICART1 expression was found to be decreased...
March 20, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28337997/the-mir-24-3p-p130cas-a-novel-axis-regulating-the-migration-and-invasion-of-cancer-cells
#3
Hoin Kang, Jun Gi Rho, Chongtae Kim, Hyosun Tak, Heejin Lee, Eunbyul Ji, Sojin Ahn, A-Ri Shin, Hyun-Il Cho, Yun Hyun Huh, Woo Keun Song, Wook Kim, Eun Kyung Lee
MicroRNAs (miRNAs) are small non-coding RNAs that negatively regulate gene expression by suppressing translation or facilitating mRNA decay. Differential expression of miRNAs is involved in the pathogenesis of several diseases including cancer. Here, we investigated the role of-miR-24-3p as a downregulated miRNA in metastatic cancer. miR-24-3p was decreased in metastatic cancer and lower expression of miR-24-3p was related to poor survival of cancer patients. Consistently, ectopic expression of miR-24-3p suppressed the cell migration, invasion, and proliferation of MCF7, Hep3B, B16F10, SK-Hep1, and PC-3 cells by directly targeting p130Cas...
March 24, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28336967/the-gene-expression-profiles-in-response-to-102-traditional-chinese-medicine-tcm-components-a-general-template-for-research-on-tcms
#4
Chao Lv, Xueting Wu, Xia Wang, Juan Su, Huawu Zeng, Jing Zhao, Shan Lin, Runhui Liu, Honglin Li, Xuan Li, Weidong Zhang
Traditional Chinese medicines (TCMs) have important therapeutic value in long-term clinical practice. However, because TCMs contain diverse ingredients and have complex effects on the human body, the molecular mechanisms of TCMs are poorly understood. In this work, we determined the gene expression profiles of cells in response to TCM components to investigate TCM activities at the molecular and cellular levels. MCF7 cells were separately treated with 102 different molecules from TCMs, and their gene expression profiles were compared with the Connectivity Map (CMAP)...
March 23, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28335434/induction-of-g2m-arrest-by-flavokawain-a-a-kava-chalcone-increases-the-responsiveness-of-her2-overexpressing-breast-cancer-cells-to-herceptin
#5
Danielle D Jandial, Lauren S Krill, Lixia Chen, Chunli Wu, Yu Ke, Jun Xie, Bang H Hoang, Xiaolin Zi
HER2/neu positive breast tumors predict a high mortality and comprise 25%-30% of breast cancer. We have shown that Flavokawain A (FKA) preferentially reduces the viabilities of HER2-overexpressing breast cancer cell lines (i.e., SKBR3 and MCF7/HER2) versus those with less HER2 expression (i.e., MCF7 and MDA-MB-468). FKA at cytotoxic concentrations to breast cancer cell lines also has a minimal effect on the growth of non-malignant breast epithelial MCF10A cells. FKA induces G2M arrest in cell cycle progression of HER2-overexpressing breast cancer cell lines through inhibition of Cdc2 and Cdc25C phosphorylation and downregulation of expression of Myt1 and Wee1 leading to increased Cdc2 kinase activities...
March 14, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28334432/uch-l1-containing-exosomes-mediate-chemotherapeutic-resistance-transfer-in-breast-cancer
#6
Kuan Ning, Teng Wang, Xu Sun, Pengfei Zhang, Yun Chen, Jian Jin, Dong Hua
BACKGROUND: Chemotherapy resistance has become a serious challenge in the treatment of breast cancer. Previous studies showed cells can transfer proteins, including those responsible for drug resistance to adjacent cells via exosomes. METHODS: The switches of drug resistance via exosomes transfer were assessed by CellTiter-Blue Viability assay, flow cytometry, and immunostaining analysis. Relative protein levels of Ubiquitin carboxyl terminal hydrolase-L1 (UCH-L1), P-glycoprotein (P-gp), extracellular-signal regulated protein kinase1/2 (ERK1/2), and phospho-extracellular-signal regulated protein kinase1/2 (p-ERK1/2) were measured by Western blot...
March 23, 2017: Journal of Surgical Oncology
https://www.readbyqxmd.com/read/28333977/transition-into-inflammatory-cancer-associated-adipocytes-in-breast-cancer-microenvironment-requires-microrna-regulatory-mechanism
#7
Jiwoo Lee, Bok Sil Hong, Han Suk Ryu, Han-Byoel Lee, Minju Lee, In Ae Park, Jisun Kim, Wonshik Han, Dong-Young Noh, Hyeong-Gon Moon
The role of adipocytes in cancer microenvironment has gained focus during the recent years. However, the characteristics of the cancer-associated adipocytes (CAA) in human breast cancer tissues and the underlying regulatory mechanism are not clearly understood. We reviewed pathology specimens of breast cancer patients to understand the morphologic characteristics of CAA, and profiled the mRNA and miRNA expression of CAA by using indirect co-culture system in vitro. The CAAs in human breast cancers showed heterogeneous topographic relationship with breast cancer cells within the breast microenvironment...
2017: PloS One
https://www.readbyqxmd.com/read/28333152/radiation-inducible-mir-770-5p-sensitizes-tumors-to-radiation-through-direct-targeting-of-pdz-binding-kinase
#8
Hyung Chul Lee, Nam-Gu Her, Donghee Kang, Seung Hee Jung, Jinwook Shin, Minyoung Lee, In Hwa Bae, Young-Nyun Kim, Heon Joo Park, Young-Gyu Ko, Jae-Seon Lee
Radiotherapy represents the most effective non-surgical modality in cancer treatment. MicroRNAs (miRNAs) are small non-coding RNAs that regulate gene expression, and are involved in many biological processes and diseases. To identify miRNAs that influence the radiation response, we performed miRNA array analysis using MCF7 cells at 2, 8, and 24 h post irradiation. We demonstrated that miR-770-5p is a novel radiation-inducible miRNA. When miR-770-5p was overexpressed, relative cell number was reduced due to increased apoptosis in MCF7 and A549 cells...
March 23, 2017: Cell Death & Disease
https://www.readbyqxmd.com/read/28330480/real-time-label-free-monitoring-of-cell-viability-based-on-cell-adhesion-measurements-with-an-atomic-force-microscope
#9
Fang Yang, René Riedel, Pablo Del Pino, Beatriz Pelaz, Alaa Hassan Said, Mahmoud Soliman, Shashank R Pinnapireddy, Neus Feliu, Wolfgang J Parak, Udo Bakowsky, Norbert Hampp
BACKGROUND: The adhesion of cells to an oscillating cantilever sensitively influences the oscillation amplitude at a given frequency. Even early stages of cytotoxicity cause a change in the viscosity of the cell membrane and morphology, both affecting their adhesion to the cantilever. We present a generally applicable method for real-time, label free monitoring and fast-screening technique to assess early stages of cytotoxicity recorded in terms of loss of cell adhesion. RESULTS: We present data taken from gold nanoparticles of different sizes and surface coatings as well as some reference substances like ethanol, cadmium chloride, and staurosporine...
March 22, 2017: Journal of Nanobiotechnology
https://www.readbyqxmd.com/read/28329677/phd2-targeting-overcomes-breast-cancer-cell-death-upon-glucose-starvation-in-a-pp2a-b55%C3%AE-mediated-manner
#10
Giusy Di Conza, Sarah Trusso Cafarello, Xingnan Zheng, Qing Zhang, Massimiliano Mazzone
B55α is a regulatory subunit of the PP2A phosphatase. We have recently found that B55α-associated PP2A promotes partial deactivation of the HIF-prolyl-hydroxylase enzyme PHD2. Here, we show that, in turn, PHD2 triggers degradation of B55α by hydroxylating it at proline 319. In the context of glucose starvation, PHD2 reduces B55α protein levels, which correlates with MDA-MB231 and MCF7 breast cancer cell death. Under these conditions, PHD2 silencing rescues B55α degradation, overcoming apoptosis, whereas in SKBR3 breast cancer cells showing resistance to glucose starvation, B55α knockdown restores cell death and prevents neoplastic growth in vitro...
March 21, 2017: Cell Reports
https://www.readbyqxmd.com/read/28325302/aptamer-drug-conjugates-of-active-metabolites-of-nucleoside-analogs-and-cytotoxic-agents-inhibit-pancreatic-tumor-cell-growth
#11
Sorah Yoon, Kai-Wen Huang, Vikash Reebye, Duncan Spalding, Teresa M Przytycka, Yijie Wang, Piotr Swiderski, Lin Li, Brian Armstrong, Isabella Reccia, Dimitris Zacharoulis, Konstantinos Dimas, Tomokazu Kusano, John Shively, Nagy Habib, John J Rossi
Aptamer-drug conjugates (ApDCs) have the potential to improve the therapeutic index of traditional chemotherapeutic agents due to their ability to deliver cytotoxic drugs specifically to cancer cells while sparing normal cells. This study reports on the conjugation of cytotoxic drugs to an aptamer previously described by our group, the pancreatic cancer RNA aptamer P19. To this end, P19 was incorporated with gemcitabine and 5-fluorouracil (5-FU), or conjugated to monomethyl auristatin E (MMAE) and derivative of maytansine 1 (DM1)...
March 17, 2017: Molecular Therapy. Nucleic Acids
https://www.readbyqxmd.com/read/28323051/anticancer-and-anti-angiogenic-activities-of-extract-from-actinidia-eriantha-benth-root
#12
Jian-Guo Wu, Li Ma, Shui-Hua Lin, Yan-Bin Wu, Jun Yi, Bin-Jun Yang, Jin-Zhong Wu, Ka-Hing Wong
ETHNOPHARMACOLOGICAL RELEVANCE: The roots of Actinidia eriantha Benth (AER) are commonly used traditional folk medicine for the treatment of gastric carcinoma, nasopharyngeal carcinoma, and breast carcinoma. Besides, the anti-proliferative and immunomodulatory effects of AER polysaccharides on tumor-bearing mice have been reported previously. AIM OF THE STUDY: This work was carried out to investigate the anticancer and anti-angiogenic activities of AER. MATERIALS AND METHODS: The growth inhibitory effects of ethanol extracts from the leaves (EEL), stems (EES) and roots (EER) of A...
March 17, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28322779/semisynthetic-oleanane-triterpenoids-inhibit-migration-and-invasion-of-human-breast-cancer-cells-through-downregulated-expression-of-the-itgb1-ptk2-pxn-pathway
#13
Natalia Lisiak, Anna Paszel-Jaworska, Ewa Toton, Błażej Rubiś, Martyna Pakuła, Barbara Bednarczyk-Cwynar, Lucjusz Zaprutko, Maria Rybczyńska
This paper reports a study on the role of two synthetic derivatives of oleanolic acid (OA), HIMOXOL and Br-HIMOLID, in the regulation of cell migration and invasion and the underlying molecular mechanisms of breast cancer cells. The effect of the compounds on four breast cancer cell lines (MCF7, MDA-MB-231, MDA-MB-468, and T-47D) and also on noncancerous breast cells, MCF-12A, was reported. The compounds had no effect on the migration of MCF-12A cells. However, both the derivatives revealed a higher cytotoxicity than the maternal compound OA, and in sub-cytotoxic concentrations, they decreased the migration of MCF7, MDA-MB-231, and MDA-MB-468 breast cancer cells and also the invasion of MCF7 and MDA-MB-231 cells; although, the derivatives had no effect on the migration and invasion of T-47D cells...
March 17, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28322778/down-regulation-of-cyclin-dependent-kinase-4-and-mapk-through-estrogen-receptor-mediated-cell-cycle-arrest-in-human-breast-cancer-induced-by-gold-nanoparticle-tagged-toxin-protein-nkct1
#14
Tanmoy Bhowmik, Antony Gomes
AIM: The aim of this study was to determine whether gold nanoparticles conjugated cytotoxic protein NKCT1 (GNP-NKCT1) acted through the estrogen receptor mediated pathway in MCF-7 cells and to establish the MAPK and PI3k/Akt signal transduction pathway. METHODS: Apoptosis was done by flow cytometry. BrdU incorporation and nuclear proliferating antigen was measured by flow cytometry. Wound healing assay along with matrigel chamber invasion and migration was done...
March 18, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28321273/characterization-of-a-new-monoclonal-anti-glypican-3-antibody-specific-to-the-hepatocellular-carcinoma-cell-line-hepg2
#15
Preeyanat Vongchan, Robert J Linhardt
AIM: To characterize the antigen on HepG2 cell that is specifically recognized by a new monoclonal antibody raised against human liver heparan sulfate proteoglycan (HSPG), clone 1E4-1D9. METHODS: The antigen recognized by mAb 1E4-1D9 was immunoprecipitated and its amino acid sequence was analyzed LC/MS. The transmembrane domain, number of cysteine residues, and glycosylation sites were predicted from these entire sequences. Data from amino acid analysis was aligned with glypican-3 (https://www...
March 8, 2017: World Journal of Hepatology
https://www.readbyqxmd.com/read/28319020/in%C3%A2-vitro-preparation-and-assessment-of-radical-reducing-peptide-from-octopus-aegina-using-digestive-proteases
#16
Sekar Sudhakar, Rasool Abdul Nazeer
Antioxidant peptides protect biological macromolecules against radical damages. The use of these peptides was evaluated using free radicals scavenging assays [2,2-diphenyl-1 picrylhydrazyl (DPPH) and hydroxyl] with the help of UV-visible and electron spin resonance (ESR) spectroscopy methods. The Octopus aegina mantle protein were tested upon hydrolysis using gastrointestinal enzymes up to 12 h, where pepsin hydrolysate exhibited superior properties (DPPH: 44.39±0.67% and hydroxyl: 38.84±1.07%) compared with trypsin and α-chymotrypsin...
March 16, 2017: Journal of Bioscience and Bioengineering
https://www.readbyqxmd.com/read/28318944/cytotoxic-dammarane-type-triterpenoids-from-the-leaves-of-viburnum-sambucinum
#17
Thanh Tra Nguyen, Bich Ngan Truong, Huong Doan Thi Mai, Marc Litaudon, Van Hung Nguyen, Thao Do Thi, Van Minh Chau, Van Cuong Pham
Four new dammarane-type triterpenoids (1-4) and twelve known compounds (5-16) were isolated from the leaves of Viburnum sambucinum Reinw. ex Blume. Their structures were determined by spectral data analysis, including MS and 2D NMR. Cytotoxic activity evaluation in vitro against four cancer cell lines (KB, LU-1, HepG2 and MCF7) suggested that the octanor-dammarane derivatives were the main cytotoxic components of the leaves of V. sambucinum.
March 7, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28301933/ferritin-decorated-plga-paclitaxel-loaded-nanoparticles-endowed-with-an-enhanced-toxicity-toward-mcf-7-breast-tumor-cells
#18
Ludmila N Turino, Maria R Ruggiero, Rachele Stefanìa, Juan C Cutrin, Silvio Aime, Simonetta Geninatti Crich
Polylactic and glycolic acid nanoparticles (PLGA-NPs), coated with L-ferritin, are exploited for the simultaneous delivery of paclitaxel and an amphiphilic Gd based MRI contrast agent into breast cancer cells (MCF7). L-ferritin has been covalently conjugated to the external surface of PLGA-NPs exploiting NHS activated carboxylic groups. The results confirmed that nanoparticles decorated with L-ferritin have many advantages with respect to both albumin-decorated and nondecorated particles. Ferritin moieties endow PLGA-NPs with targeting capability, exploiting SCARA5 receptors overexpressed by these tumor cells, that results in an increased paclitaxel cytotoxicity...
March 24, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28296597/acetylation-targets-hsd17b4-for-degradation-via-the-cma-pathway-in-response-to-estrone
#19
Ye Zhang, Ying-Ying Xu, Chuan-Bo Yao, Jin-Tao Li, Xiang-Ning Zhao, Hong-Bin Yang, Min Zhang, Miao Yin, Jing Chen, Qun-Ying Lei
Dysregulation of hormone metabolism is implicated in human breast cancer. 17β-hydroxysteroid dehydrogenase type 4 (HSD17B4) catalyzes the conversion of estradiol (E2) to estrone (E1), and is associated with the pathogenesis and development of various cancers. Here we show that E1 upregulates HSD17B4 acetylation at lysine 669 (K669) and thereby promotes HSD17B4 degradation via chaperone-mediated autophagy (CMA), while a single mutation at K669 reverses the degradation and confers migratory and invasive properties to MCF7 cells upon E1 treatment...
March 4, 2017: Autophagy
https://www.readbyqxmd.com/read/28296189/tlr4-promotes-breast-cancer-metastasis-via-akt-gsk3%C3%AE-%C3%AE-catenin-pathway-upon-lps-stimulation
#20
Jun Li, Jing Yin, Wenzhi Shen, Ruifang Gao, Yanhua Liu, Yanan Chen, Xiru Li, Chenghu Liu, Rong Xiang, Na Luo
Bacteria/virus-induced chronic inflammation is involved in both tumor initiation and tumor progression. Toll-like receptor 4 (TLR4) has been implicated in the development of several types of cancer. In this study, we explored the impact of TLR4 activation by lipopolysaccharide (LPS) on breast cancer metastasis and associated signaling molecules. We first examined TLR4 expression levels in breast tissue using a human breast tissue microarray and breast cell lines. We then studied the role of TLR4 activation by LPS stimulation in breast cancer metastasis using both in vitro and in vivo models...
March 14, 2017: Anatomical Record: Advances in Integrative Anatomy and Evolutionary Biology
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