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https://www.readbyqxmd.com/read/27914362/an-overview-of-the-binding-models-of-fgfr-tyrosine-kinases-in-complex-with-small-molecule-inhibitors
#1
REVIEW
Weiyan Cheng, Mixiang Wang, Xin Tian, Xiaojian Zhang
The fibroblast growth factor receptor (FGFR) family receptor tyrosine kinase (RTK) includes four structurally related members, termed as FGFR1, FGFR2, FGFR3, and FGFR4. Given its intimate role in the progression of several solid tumors, excessive FGFR signaling provides an opportunity for anticancer therapy. Along with extensive pharmacological studies validating the therapeutic potential of targeting the FGFRs for cancer treatment, co-crystal structures of FGFRs/inhibitors are continuously coming up to study the mechanism of actions and explore new inhibitors...
November 25, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27914336/thermoresponsive-supramolecular-micellar-drug-delivery-system-based-on-star-linear-pseudo-block-polymer-consisting-of-%C3%AE-cyclodextrin-poly-n-isopropylacrylamide-and-adamantyl-poly-ethylene-glycol
#2
Xia Song, Jing-Ling Zhu, Yuting Wen, Feng Zhao, Zhong-Xing Zhang, Jun Li
Chemotherapy is facing several limitations such as low water solubility of anticancer drugs and multidrug resistance (MDR) in cancer cells. To overcome these limitations, a thermoresponsive micellar drug delivery system formed by a non-covalently connected supramolecular block polymer was developed. The system is based on the host-guest interaction between a well-defined β-cyclodextrin (β-CD) based poly(N-isopropylacrylamide) star host polymer and an adamantyl-containing poly(ethylene glycol) (Ad-PEG) guest polymer...
November 16, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/27914241/engot-ov-6-trinova-2-randomised-double-blind-phase-3-study-of-pegylated-liposomal-doxorubicin-plus-trebananib-or-placebo-in-women-with-recurrent-partially-platinum-sensitive-or-resistant-ovarian-cancer
#3
Christian Marth, Ignace Vergote, Giovanni Scambia, Willi Oberaigner, Andrew Clamp, Regina Berger, Christian Kurzeder, Nicoletta Colombo, Peter Vuylsteke, Domenica Lorusso, Marcia Hall, Vincent Renard, Sandro Pignata, Rebecca Kristeleit, Sevilay Altintas, Gordon Rustin, Robert M Wenham, Mansoor Raza Mirza, Peter C Fong, Amit Oza, Bradley J Monk, Haijun Ma, Florian D Vogl, Bruce A Bach
AIMS: Trebananib, a peptide-Fc fusion protein, inhibits angiogenesis by inhibiting binding of angiopoietin-1/2 to the receptor tyrosine kinase Tie2. This randomised, double-blind, placebo-controlled phase 3 study evaluated whether trebananib plus pegylated liposomal doxorubicin (PLD) improved progression-free survival (PFS) in patients with recurrent epithelial ovarian cancer. METHODS: Women with recurrent ovarian cancer (platinum-free interval ≤12 months) were randomised to intravenous PLD 50 mg/m(2) once every 4 weeks plus weekly intravenous trebananib 15 mg/kg or placebo...
November 30, 2016: European Journal of Cancer
https://www.readbyqxmd.com/read/27914215/lysine-specific-demethylase-1-lsd1-inhibitor-s2101-induces-autophagy-via-the-akt-mtor-pathway-in-skov3-ovarian-cancer-cells
#4
Shujun Feng, Ye Jin, Mengjiao Cui, Jianhua Zheng
BACKGROUND S2101 is one of the most potent LSD1 inhibitors, which can inhibit ovarian cancer cells viability. This study aimed to detect the mechanism behind the anticancer properties of S2101 in SKOV3 ovarian cells. MATERIAL AND METHODS Cell viability was tested by Cell Counting Kit-8 (CCK-8) assay. Cellular apoptosis and autophagy were evaluated by flow cytometric analysis using Annexin-V/PI staining methods and Green fluorescent protein (GFP)-fused-LC3 (GFP-LC3), respectively. Western blotting was performed for analyzing the Bax, Bcl-2, mTOR, p- mTOR, p62, LC3-I, LC3-II, AKT, and p-AKT protein expression...
December 3, 2016: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/27913286/cytotoxic-activity-of-soy-phytoestrogen-coumestrol-against-human-breast-cancer-mcf-7%C3%A2-cells-insights-into-the-molecular-mechanism
#5
Atif Zafar, Swarnendra Singh, Imrana Naseem
Coumestrol is a phytoestrogen present in soybean products and recognized as potential cancer therapeutic agent against breast cancer. However, the clear molecular mechanism of anticancer-activity of coumestrol in breast carcinoma has not been reported. It is well established that copper levels are elevated in different malignancies. Therefore, the objective of this study was to investigate the copper-dependent cytotoxic action of coumestrol in human breast cancer MCF-7 cells. Results showed that coumestrol inhibited proliferation and induced apoptosis in MCF-7 cells, which was prevented by copper chelator neocuproine and ROS scavengers...
November 29, 2016: Food and Chemical Toxicology
https://www.readbyqxmd.com/read/27912948/therapeutic-efficacy-of-traditional-chinese-medicine-kuan-sin-yin-in-patients-undergoing-chemotherapy-for-advanced-colon-cancer-a-controlled-trial
#6
Tsai-Ju Chien, Chia-Yu Liu, Ruey-Hwa Lu, Chin-Wei Kuo, Yang-Chao Lin, Chung-Hua Hsu
BACKGROUND: Traditional Chinese Medicine (TCM) has been used increasingly as complementary medicine in cancer care. Kuan-Sin-Yin (KSY) is a TCM decoction containing seven herbs known to cause immunomodulation or anticancer activity, and which are associated with the TCM concept of Qi and energy supply. Kuan-Sin-Yin has cytostatic effects on cancer cells in animal models. OBJECTIVE: The aim of this study is to evaluate the level of improvement in meridian energy and heart-rate variability (HRV) and to assess whether these observations are compatible with TCM theory...
December 2016: Complementary Therapies in Medicine
https://www.readbyqxmd.com/read/27910791/effects-of-ethyl-acetate-extracts-from-the-polycephalomyces-nipponicus-isolate-cod-mk1201-ascomycetes-against-human-pathogenic-bacteria-and-a-breast-cancer-cell-line
#7
Kusavadee Sangdee, Prapairat Seephonkai, Benjaporn Buranrat, Nilawan Surapong, Aphidech Sangdee
This study aimed to identify a suitable organic solvent for extracting bioactive compounds from Polycephalomyces nipponicus and to evaluate the antibacterial and anticancer activities of the extracts obtained. Only extracts obtained with ethyl acetate exhibited antibacterial activity, so ethyl acetate was chosen for large-scale extraction. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) against Gram-positive and Gram-negative human pathogenic bacteria of the 3 ethyl acetate-derived extracts-ethyl acetate extract from P...
2016: International Journal of Medicinal Mushrooms
https://www.readbyqxmd.com/read/27910781/inhibition-of-dimethylbenz-a-anthracene-dmba-croton-oil-induced-mouse-skin-tumorigenesis-by-gmelina-arborea-with-potential-anti-inflammatory-activity
#8
Lincy Lawrence, Seema Menon, Divya Menon K, Vipin P Sivaram, Jose Padikkala
In traditional Indian medicine, the plant Gmelina arborea Linn. (GA) is described to have the ability to relieve edema. The present study evaluates the anticancer property of GA stem bark against 7,12-dimethylbenz(a) anthracene (DMBA)-croton oil-induced skin tumorigenesis along with the evaluation of anti-inflammatory activity. The observed inhibition of inflammation in carrageenan-induced (41.8%) and formalin-induced (34.07%) models may be due to inhibition of prostaglandins (PGs). Skin papilloma was induced by a single topical application of DMBA (470 nmol/200 µL acetone), followed by repeated application of croton oil (1% in 200 µL acetone)...
2016: Journal of Environmental Pathology, Toxicology and Oncology
https://www.readbyqxmd.com/read/27909934/current-achievements-and-future-perspectives-of-metronomic-chemotherapy
#9
REVIEW
Adriana Romiti, Rosa Falcone, Michela Roberto, Paolo Marchetti
In recent years, many anticancer drugs have been tested at metronomic dosages for a variety of tumours. Mechanisms of action attributed to metronomic chemotherapy (MCT) include antiangiogenesis, immunomodulation, direct inhibition of tumour growth, effect on tumour initiating cells and the modulation of clonal evolution. An active clinical research, aimed at testing MCT in several cancers, has been conducted over the past 15 years. However, because the majority of available results come from earlier phase II studies, mainly performed in the area of breast cancer (BC), it is clear that there are areas still to be investigated...
December 1, 2016: Investigational New Drugs
https://www.readbyqxmd.com/read/27909719/the-expression-and-function-of-epithelial-membrane-protein-1-in-laryngeal-carcinoma
#10
Hong Li, Xiaowen Zhang, Xuejun Jiang, Xu Ji
In this study, we compared the expression of epithelial membrane protein 1 (EMP1) on the steady-state mRNA level (by quantitative real-time PCR) and on the protein level (by western immunoblot and immunohistochemistry) in 51 pairs of laryngeal carcinoma tissues and matched cancer-free peritumor tissues, and we analyzed the correlation between EMP1 expression and different clinicopathological factors. Furthermore, we ectopically expressed EMP1 in human laryngeal carcinoma Hep-2 cells and examined the effects on cell viability, apoptosis, colonogenicity, and motility, by MTT assay, flow cytometry, colony formation assay and Transwell migration assay, respectively...
November 28, 2016: International Journal of Oncology
https://www.readbyqxmd.com/read/27909709/synthesis-of-a-fluorescent-photoaffinity-probe-of-osw-1-by-site-selective-acylation-of-an-inactive-congener-and-biological-evaluation
#11
K Sakurai, M Hiraizumi, N Isogai, R Komatsu, T Shibata, Y Ohta
A novel fluorescent photoaffinity probe of OSW-1 was prepared in two steps from a naturally occurring inactive congener by a sequential site-selective acylation strategy using Me2SnCl2. It displayed highly potent anticancer activity and a similar intracellular localization property to that of a fluorescently-tagged OSW-1, thereby demonstrating its potential utility in live cell studies.
December 2, 2016: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/27908776/3-geranyl-mono-substituted-chalcone-xanthoangelovl-induces-apoptosis-in-human-leukemia-k562%C3%A2-cells-via-activation-of-mitochondrial-pathway
#12
Yuou Teng, Lixin Wang, Huan Liu, Yuan Yuan, Qian Zhang, Meng Wu, Luyao Wang, Haomeng Wang, Zhen Liu, Peng Yu
3'-Geranyl-mono-substituted chalcone Xanthoangelol (1b), a chalcone derivative, was previously reported to show selective cytotoxicity against human chronic myelogenous leukemia K562 cells with a half-maximal inhibitory concentration (IC50) of 3.98 μM. In the present study, we investigated the molecular mechanism underlying the cytotoxicity of 1b in K562 cells. Treatment with compound 1b caused K562 cells to adopt a typical apoptotic morphology. Flow cytometric analysis also confirmed the presence of an apoptotic cell population following treatment of Annexin-V-FITC and propidium iodide (PI) double-labeled K562 cells with 1b...
November 28, 2016: Chemico-biological Interactions
https://www.readbyqxmd.com/read/27908730/mtor-activation-is-critical-for-betulin-treatment-in-renal-cell-carcinoma-cells
#13
Wenlong Cheng, Shiqi Ji, Haijian Zhang, Zhixing Han, Qingjun Liu, Jianwen Wang, Hao Ping
Betulin, a natural product isolated from the bark of the birch trees, exhibits multiple anticancer effects. Activation of mTOR signaling pathway has been found in numerous cancers, including renal cell carcinoma (RCC). Here, we attempted to study whether mTOR signaling was essential for betulin to treat RCC. Based on cell survival and colony formation assays, we found that mTOR hyperactive RCC cell line 786-O cells were more sensitive to betulin treatment compared with mTOR-inactive Caki-2 cells. Knockdown of TSC2 in Caki-2 cells had similar results to 786-O cells, and mTOR silencing in 786-O cells rescued the inhibitory effect of betulin, indicating that betulin inhibited RCC cell proliferation in an mTOR-dependent manner...
November 28, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27906201/the-cost-of-molecular-guided-therapy-in-oncology-a-prospective-cost-study-alongside-the-moscato-trial
#14
Arnaud Pagès, Stéphanie Foulon, Zhaomin Zou, Ludovic Lacroix, François Lemare, Thierry de Baère, Christophe Massard, Jean-Charles Soria, Julia Bonastre
AIM: There is increasing use of molecular technologies to guide cancer treatments, but few cost data are available. Our objective was to assess the costs of molecular-guided therapy for patients with advanced solid tumors alongside the Molecular Screening for Cancer Treatment and Optimization (MOSCATO) trial. MATERIALS AND METHODS: The study population consisted of 529 patients. The molecular diagnosis included seven steps from tumor biopsy to the multidisciplinary molecular tumor board...
December 1, 2016: Genetics in Medicine: Official Journal of the American College of Medical Genetics
https://www.readbyqxmd.com/read/27906147/biogenic-synthesis-of-silver-nanoparticles-from-cassia-fistula-linn-in-vitro-assessment-of-their-antioxidant-antimicrobial-and-cytotoxic-activities
#15
Yugal Kishore Mohanta, Sujogya Kumar Panda, Kunal Biswas, Abiral Tamang, Jaya Bandyopadhyay, Debashis De, Dambarudhar Mohanta, Akshaya Kumar Bastia
The present study reports on biogenic-synthesised silver nanoparticles (AgNPs) derived by treating Ag ions with an extract of Cassia fistula leaf, a popular Indian medicinal plant found in natural habitation. The progress of biogenic synthesis was monitored time to time using a ultraviolet-visible spectroscopy. The effect of phytochemicals present in C. fistula including flavonoids, tannins, phenolic compounds and alkaloids on the homogeneous growth of AgNPs was investigated by Fourier-transform infrared spectroscopy...
December 2016: IET Nanobiotechnology
https://www.readbyqxmd.com/read/27905872/knockdown-of-ggct-inhibits-cell-proliferation-and-induces-late-apoptosis-in-human-gastric-cancer
#16
Wenjie Zhang, Lei Chen, Honggang Xiang, Chunhua Hu, Weibin Shi, Ping Dong, Wenjie Lv
BACKGROUND: Gamma glutamylcyclotransferase (GGCT) has been proved to be involved in various cancers, but the biological function of GGCT in gastric cancer is still largely unknown. METHODS: The expression level of GGCT was evaluated by informatics analyses based on the Oncomine database. GGCT gene was then effectively knocked down via lentivirus mediated short hairpin RNA (shRNA) system. Then a series of functional assays, including MTT, colony formation and flow cytometry analysis were conducted on gastric cancer cells following GGCT knockdown...
December 1, 2016: BMC Biochemistry
https://www.readbyqxmd.com/read/27905583/intracellular-water-an-overlooked-drug-target-cisplatin-impact-in-cancer-cells-probed-by-neutrons
#17
M P M Marques, A L M Batista de Carvalho, V Garcia Sakai, L Hatter, L A E Batista de Carvalho
The first neutron scattering study on human nucleated cells is reported, addressing the subject of solvent-slaving to a drug by probing intracellular water upon drug exposure. Inelastic and quasi-elastic neutron scattering spectroscopy with isotope labelling was applied for monitoring interfacial water response to the anticancer drug cisplatin, in the low prognosis human metastatic breast cancer cells MDA-MB-231. Optical vibrational data were also obtained for lyophilised cells. Concentration-dependent dynamical changes evidencing a progressive mobility reduction were unveiled between untreated and cisplatin-exposed samples, concurrent with variations in the native organisation of water molecules within the intracellular medium as a consequence of drug action...
December 1, 2016: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/27904848/silencing-the-livin-gene-enhances-the-cytotoxic-effects-of-anticancer-drugs-on-colon-cancer-cells
#18
Bo Young Oh, Kwang Ho Kim, Soon Sup Chung, Ryung-Ah Lee
PURPOSE: Livin is associated with drug response in several cancers. The aim of this study was to investigate the effect of silencing the livin gene expression on anticancer drug response in colorectal cancer. METHODS: siRNA was transfected at different concentrations (0, 10, and 30nM) into HCT116 cells, then cells were treated with either 5-fluorouracil (FU)/leucovorin (LV) or oxaliplatin (L-OHP)/5-FU/LV. Cellular viability and apoptosis were evaluated following silencing of livin gene expression combined with treatment with anticancer drugs...
December 2016: Annals of Surgical Treatment and Research
https://www.readbyqxmd.com/read/27904580/quercetin-and-ovarian-cancer-an-evaluation-based-on-a-systematic-review
#19
REVIEW
Arefe Parvaresh, Roghaye Razavi, Nahid Rafie, Reza Ghiasvand, Makan Pourmasoumi, Maryam Miraghajani
Some studies have suggested chemopreventive and therapeutic effects of quercetin (Q) on carcinogenesis. The aim of this review was to evaluate the association between Q and ovarian cancer risk among human researches and induced sensitivity to some types of chemotherapeutic drugs and antiproliferative effects of this flavonoid in the animals and cell lines studies. Data for this systematic review were achieved through searches of the MEDLINE (PubMed), Google Scholar, Science Direct, Scopus, Cochrane, SID, and Magiran databases for studies published up to May 2015...
2016: Journal of Research in Medical Sciences: the Official Journal of Isfahan University of Medical Sciences
https://www.readbyqxmd.com/read/27903226/protective-effects-of-caffeic-acid-and-the-alzheimer-s-brain-an-update
#20
Solomon Habtemariam
Caffeic acid (CA) and related phenylpropanoic acids are ubiquitous natural products of the shikimic acid pathway origin. Due to the presence of diorthohydroxyl aromatic (catecholic) moiety, CA is not only one of the most potent antioxidant phenyl propanoids but also display numerous other pharmacological effects ranging from antiinflammatory to anticancer effects. Recent studies also demonstrated that CA both in its free form or conjugated with other groups such as quinic acid and sugars display profound effects in the brain including protection from toxicity induced by a variety of agents and/or experimental models of Alzheimer's disease (AD)...
November 29, 2016: Mini Reviews in Medicinal Chemistry
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