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https://www.readbyqxmd.com/read/28534969/the-cdc2-cdk1-inhibitor-purvalanol-a-enhances-the-cytotoxic-effects-of-taxol-through-op18-stathmin-in-non-small-cell-lung-cancer-cells-in%C3%A2-vitro
#1
Xian Chen, Ying Liao, Dan Long, Ting Yu, Fang Shen, Xuechi Lin
Purvalanol A is a highly selective inhibitor of Cdc2 [also known as cyclin-dependent kinase 1 (CDK1)]. Taxol is an anti-tumor chemotherapeutic drug which is widely used clinically. In this study, the CDK1 inhibitor, purvalanol A was applied to explore the relevance of Cdc2 signaling and taxol sensitivity through analyses, such as cellular proliferation and apoptosis assays, ELISA, western blot analysis and immunoprecipitation. We demonstrated that purvalanol A effectively enhanced the taxol-induced apoptosis of NCI-H1299 cells, as well as its inhibitory effects on cellular proliferation and colony formation...
May 15, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28512026/one-pot-synthesis-and-biological-evaluation-of-n-aminosulfonyl-4-podophyllotoxin-carbamates-as-potential-anticancer-agents
#2
Xiao-Hui Xu, Xiao-Wen Guan, Shi-Liang Feng, You-Zhen Ma, Shi-Wu Chen, Ling Hui
A series of N-(aminosulfonyl)-4-podophyllotoxin carbamates were synthesized via the Burgess-type intermediate, and their antiproliferative activities were evaluated. Most of them possessed more potent cytotoxic effects against four human tumor cell lines (HeLa, A-549, HCT-8 and HepG2) and less toxic to normal human fetal lung fibroblast WI-38 cells than etoposide. In particular, N-(morpholinosulfonyl)-4-podophyllotoxin carbamate (9) exhibited the most potent activity towards these four tumor cells with IC50 values in the range of 0...
April 27, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28484902/the-molecular-mechanisms-of-protective-role-of-se-on-the-g2-m-phase-arrest-of-jejunum-caused-by-afb1
#3
Jing Fang, Heng Yin, Zhixiang Zheng, Panpan Zhu, Xi Peng, Zhicai Zuo, Hengmin Cui, Yi Zhou, Ping Ouyang, Yi Geng, Junliang Deng
Aflatoxin B1 (AFB1) is the most toxic among the mycotoxins and causes detrimental health effects on human and animals. Selenium (Se) plays an important role in chemopreventive, antioxidant, anticarcinogen, and detoxification and involved in cell cycle regulation. The aim of this study was to explore the molecular mechanisms of selenium involved in inhibition of G2/M cell cycle arrest of broiler's jejunum. A total of 240 one-day-old healthy Cobb broilers were randomly divided into four groups and fed with basal diet (control group), 0...
May 9, 2017: Biological Trace Element Research
https://www.readbyqxmd.com/read/28475750/astaxanthin-increases-radiosensitivity-in-esophageal-squamous-cell-carcinoma-through-inducing-apoptosis-and-g2-m-arrest
#4
X Qian, C Tan, B Yang, F Wang, Y Ge, Z Guan, J Cai
Nowadays esophageal squamous cell carcinoma (ESCC) is primarily treated by a comprehensive approach combining surgical resection and neoadjuvant chemo- or radiotherapy. However, ESCC is resistant to radiation therapy, resulting in its invasion, infiltration, and metastasis. It usually has rapidly progressed and has a poor outcome clinically. The purpose of this study is to determine the potential radiosensitizing effect of astaxanthin (ATX) and explore the underlying mechanisms in ESCC cells in vitro. ESCC cell lines were exposure to irradiation, in the presence or absence of ATX treatment...
June 1, 2017: Diseases of the Esophagus: Official Journal of the International Society for Diseases of the Esophagus
https://www.readbyqxmd.com/read/28456516/identification-of-novel-1-indolyl-acetate-5-nitroimidazole-derivatives-of-combretastatin-a-4-as-potential-tubulin-polymerization-inhibitors
#5
Yong-Fang Yao, Zhong-Chang Wang, Song-Yu Wu, Qing-Fang Li, Chen-Yu, Xin-Yi Liang, Peng-Cheng Lv, Yong-Tao Duan, Hai-Liang Zhu
Microtubules are essential for the mitotic division of cells and have become an attractive target for anti-tumour drugs due to the increased incidence of cancer and significant mitosis rate of tumour cells. In this study, a total of six indole 1-position modified 1-indolyl acetate-5-nitroimidazole derivatives were designed, synthesized, and evaluated for their ability to inhibit tubulin polymerization caused by binding to the colchicine-binding site of tubulin. Among them, compound 3 displayed the best ability to inhibit tubulin polymerization; it also exhibited better anti-proliferative activities than colchicine against a panel of human cancer cells (with IC50 values ranging from 15 to 40 nM), especially HeLa cells (with IC50 values of 15 nM), based on the cellular cytotoxicity assay results...
April 26, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28450285/low-dose-cadmium-exposure-induces-peribronchiolar-fibrosis-through-site-specific-phosphorylation-of-vimentin
#6
Fu Jun Li, Ranu Surolia, Huashi Li, Zheng Wang, Gang Liu, Rui-Ming Liu, Sergey B Mirov, Mohammad Athar, Victor J Thannickal, Veena B Antony
Exposure to cadmium (Cd) has been associated with development of chronic obstructive lung disease (COPD). The mechanisms and signaling pathways whereby Cd causes pathological peribronchiolar fibrosis, airway remodeling and subsequent airflow obstruction remain unclear. We aimed to evaluate whether low dose Cd exposure induces vimentin phosphorylation and YAP1 activation leading to peribronchiolar fibrosis and subsequent airway remodeling. Our data demonstrate that Cd induces myofibroblast differentiation and extracellular matrix (ECM) deposition around small (<2 mm in diameter) airways...
April 27, 2017: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/28442503/molecular-pathways-targeting-the-protein-kinase-wee1-in-cancer
#7
Jill J J Geenen, Jan H M Schellens
Wee1 is a protein kinase that regulates the G2 checkpoint and prevents entry into mitosis in response to DNA damage. Cyclin-dependent kinases (CDKs) are a family of 14 serine/threonine protein kinases, which coordinate the progression through the cell cycle. The Cdc2/cyclin B complex controls the progression from G2 into mitosis. There are two mechanisms by which the G2 checkpoint is initiated in response to DNA damage: phosphorylation of Cdc25c by CHK1 and of Wee1 kinase, which phosphorylates Cdc2. Blockade at the G2 checkpoint is especially important for p53 mutant cells because these tumors mainly rely on DNA repair at the G2 checkpoint...
April 25, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28440465/5-furan-2-yl-4-3-4-5-trimethoxyphenyl-3h-1-2-dithiol-3-one-oxime-6f-a-new-synthetic-compound-causes-human-%C3%AF-brosarcoma-ht-1080-cell-apoptosis-by-disrupting-tubulin-polymerisation-and-inducing-g2-m-arrest
#8
Daiying Zuo, Lili Pang, Jiwei Shen, Qi Guan, Zhaoshi Bai, Huijuan Zhang, Yao Li, Guodong Lu, Weige Zhang, Yingliang Wu
In the current study, we synthesized a series of new compounds targeting tubulin and tested their anti-proliferative activities. Among these new synthetic com-pounds, 5-(furan-2-yl)-4-(3,4,5-trimethoxyphenyl)-3H-1,2-dithiol-3-one oxime (6f) exhibited significant anti-proliferative activity against different human cancer cell lines including human gastric adenocarcinoma SGC-7901, human non-small cell lung cancer A549, and human fibrosarcoma HT-1080. As a result, 6f was selected to further test the sensitivity to different cancer cell lines including human cervical cancer cell line HeLa, human breast cancer cell line MCF-7, non-small cell lung cancer cell line A549, human liver carcinoma cell line HepG-2, human oral squamous cell carcinoma cell lines KB, SGC-7901 and HT-1080...
April 18, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28421187/subset-specific-expression-of-toll-like-receptors-by-bovine-afferent-lymph-dendritic-cells
#9
Dirk Werling, Jayne C Hope, Nazneen Siddiqui, Stephanie Widdison, Chris Russell, Paul Sopp, Tracey J Coffey
Within the ruminant system, several possibilities exist to generate dendritic cells migrating out from the tissue into the regional draining lymph nodes as afferent lymph dendritic cells (ALDCs). Here, we analyzed toll-like receptor (TLR) 1-10 mRNA expression by using quantitative real-time PCR in highly purified subsets of bovine ALDC. As TLR expression may be influenced by pathogens or vaccines and their adjuvant, it is necessary to understand what TLRs are expressed in a steady-state system to elucidate specific differences and to potentially optimize targeted vaccines...
2017: Frontiers in Veterinary Science
https://www.readbyqxmd.com/read/28416318/basic-fibroblast-growth-factor-regulates-gene-and-protein-expression-related-to-proliferation-differentiation-and-matrix-production-of-human-dental-pulp-cells
#10
Ya-Ching Chang, Mei-Chi Chang, Yi-Jane Chen, Ji-Uei Liou, Hsiao-Hua Chang, Wei-Ling Huang, Wan-Chuen Liao, Chiu-Po Chan, Po-Yuan Jeng, Jiiang-Huei Jeng
INTRODUCTION: Basic fibroblast growth factor (bFGF) plays differential effects on the proliferation, differentiation, and extracellular matrix turnover in various tissues. However, limited information is known about the effect of bFGF on dental pulp cells. The purposes of this study were to investigate whether bFGF influences the cell differentiation and extracellular matrix turnover of human dental pulp cells (HDPCs) and the related gene and protein expression as well as the role of the mitogen-activated protein kinase (MEK)/extracellular-signal regulated kinase (ERK) signaling pathway...
April 14, 2017: Journal of Endodontics
https://www.readbyqxmd.com/read/28412508/methyl-5-1h-indol-3-yl-selanyl-1h-benzoimidazol-2-ylcarbamate-m-24-a-novel-tubulin-inhibitor-causes-g2-m-arrest-and-cell-apoptosis-by-disrupting-tubulin-polymerization-in-human-cervical-and-breast-cancer-cells
#11
Daiying Zuo, Xuewei Jiang, Mengting Han, Jiwei Shen, Binyue Lang, Qi Guan, Zhaoshi Bai, Chunming Han, Zengqiang Li, Weige Zhang, Yingliang Wu
Methyl 5-[(1H-indol-3-yl)selanyl]-1H-benzoimidazol-2-ylcarbamate (M-24) is a newly synthesized analogue of nocodazole by our group and has been found to be active for some cancer cells. However, its sensitivity to different cell lines and the underlying anticancer mechanism are still unclear. In this study, we proved that M-24 had strong time- and dose-dependent anti-proliferative effects on human cervical cancer HeLa cells and human breast carcinoma MCF-7 cells. We demonstrated that the growth inhibitory effects of M-24 in both cell lines were associated with microtubule depolymerization...
April 13, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28402920/mirna-200c-enhances-radiosensitivity-of-esophageal-cancer-by-cell-cycle-arrest-and-targeting-p21
#12
Ruzhen Zheng, Yuehua Liu, Xiaoling Zhang, Pengjun Zhao, Qinghua Deng
Esophageal squamous cancer is one of the most fatal malignancies and often suffer recurrence after radiotherapy. Downregulation of miRNA-200c is associated with radiotolerance. We aim to investigate the role of miRNA-200c in radiosensitivity and develop a systemic treatment strategy for esophageal squamous cancer. Overexpression of miRNA-200c by transfection was determined by RT-PCR. Radiosensitizing effect of miRNA-200c on esophageal squamous cancer cells was determined by clonogenic assay and xenograft model...
June 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28389620/exploiting-tumor-associated-dendritic-cell-heterogeneity-for-novel-cancer-therapies
#13
REVIEW
Jiri Keirsse, Helena Van Damme, Jo A Van Ginderachter, Damya Laoui
Dendritic cells (DCs) are specialized APCs present in all tissues, including tumors. They play a major role in orchestrating immune responses and were shown to occur in various functional states in tumors. In this respect, immunogenic tumor-associated DCs (TADCs) are required to initiate and sustain T cell-dependent anti-cancer immunity, whereas regulatory TADCs harbor robust immunosuppressive potential and accelerate malignant growth. Importantly, the heterogeneity of the DC compartment in tumors has been dissected recently in murine and human cancers and was shown to consist of developmentally distinct subsets, including conventional DC (cDC)1, cDC2, and monocyte-derived DCs (Mo-DCs)...
April 7, 2017: Journal of Leukocyte Biology
https://www.readbyqxmd.com/read/28387732/bioactive-metabolites-from-the-deep-subseafloor-fungus-oidiodendron-griseum-ubocc-a-114129
#14
Marion Navarri, Camille Jégou, Arnaud Bondon, Sandrine Pottier, Stéphane Bach, Blandine Baratte, Sandrine Ruchaud, Georges Barbier, Gaëtan Burgaud, Yannick Fleury
Four bioactive compounds have been isolated from the fungus Oidiodendron griseum UBOCC-A-114129 cultivated from deep subsurface sediment. They were structurally characterized using a combination of LC-MS/MS and NMR analyses as fuscin and its derivatives (dihydrofuscin, dihydrosecofuscin, and secofuscin) and identified as polyketides. Albeit those compounds were already obtained from terrestrial fungi, this is the first report of their production by an Oidiodendron species and by the deepest subseafloor isolate ever studied for biological activities...
April 7, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28386672/malignancy-in-pheochromocytoma-or-paraganglioma-integrative-analysis-of-176-cases-in-tcga
#15
Yong Joon Suh, Ji-Young Choe, Hyo Jin Park
Methods of diagnosing malignant pheochromocytoma (PCC) or paraganglioma (PGL) are needed. However, there are no reliable histopathologic criteria to distinguish malignant PCC/PGLs. The recent genomic analysis of The Cancer Genome Atlas (TCGA) provides in-depth information enabling more accurate diagnosis of disease entities. Therefore, we investigated genomic expression differences and mutational differences of malignant PCC/PGLs with TCGA. As of December 2014, TCGA had acquired multigenomic analysis of 176 PCC/PGL samples...
June 2017: Endocrine Pathology
https://www.readbyqxmd.com/read/28386317/alisertib-induces-g2-m-arrest-apoptosis-and-autophagy-via-pi3k-akt-mtor-and-p38-mapk-mediated-pathways-in-human-glioblastoma-cells
#16
Zheng Liu, Feng Wang, Zhi-Wei Zhou, He-Chun Xia, Xin-Yu Wang, Yin-Xue Yang, Zhi-Xu He, Tao Sun, Shu-Feng Zhou
Glioblastoma (GBM) is the most common brain tumor with poor response to current therapeutics. Alisertib (ALS), a second-generation selective Aurora kinase A (AURKA) inhibitor, has shown potent anticancer effects on solid tumors in animal studies. This study aimed to investigate the killing effect of ALS on GBM cell line DAOY and the possible underlying mechanisms using both bioinformatic and cell-based approaches. Our molecular docking showed that ALS preferentially bound AURKA over AURKB via hydrogen bond formation, charge interaction, and π-π stacking...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28384515/pm2-5-induced-alterations-of-cell-cycle-associated-gene-expression-in-lung-cancer-cells-and-rat-lung-tissues
#17
Hui Zhao, Biao Yang, Jia Xu, Dong-Mei Chen, Chun-Ling Xiao
The aim of the current study was to investigate the expression of cell cycle-associated genes induced by fine particulate matter (PM2.5) in lung cancer cell line and tissues. The pulmonary lymph node metastasis cells (H292) were treated with PM2.5in vitro. Wistar rats were used to perform an in vivo study. Rats were randomly assigned to experiment and control groups and those in the experiment group were exposed to PM2.5 once every 15 d, while those in the control group were exposed to normal saline. The cell cycle-associated genes expression was analyzed by real-time PCR...
March 24, 2017: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/28370201/a-phase-1-study-of-amg-900-an-orally-administered-pan-aurora-kinase-inhibitor-in-adult-patients-with-acute-myeloid-leukemia
#18
Hagop M Kantarjian, Michael W Schuster, Nitin Jain, Anjali Advani, Elias Jabbour, Erick Gamelin, Erik Rasmussen, Gloria Juan, Abraham Anderson, Vincent F Chow, Greg Friberg, Florian D Vogl, Mikkael A Sekeres
Aurora kinases are involved in the pathophysiology of several cancers including acute myeloid leukemia (AML). In this phase 1 study, we investigated the safety and efficacy of AMG 900, an orally administered, highly potent, selective, small-molecule inhibitor of both Aurora kinase A and B, in patients with AML. Patients with pathologically documented AML who either declined standard treatments or had relapsed from or were refractory to previous therapies were enrolled. Two every-2-week dose-escalation schedules using a modified 3 + 3+3 design were used: AMG 900 given daily for 4 days with 10 days off (4/10 schedule), and AMG 900 given daily for 7 days with 7 days off (7/7 schedule)...
March 28, 2017: American Journal of Hematology
https://www.readbyqxmd.com/read/28352336/anthelmintic-drug-albendazole-arrests-human-gastric-cancer-cells-at-the-mitotic-phase-and-induces-apoptosis
#19
Xuan Zhang, Jing Zhao, Xiangyang Gao, Dongsheng Pei, Chao Gao
As microtubules have a vital function in the cell cycle, oncologists have developed microtubule inhibitors capable of preventing uncontrolled cell division, as in the case of cancer. The anthelmintic drug albendazole (ABZ) has been demonstrated to inhibit hepatocellular, ovarian and prostate cancer cells via microtubule targeting. However, its activity against human gastric cancer (GC) cells has remained to be determined. In the present study, ABZ was used to treat GC cells (MKN-45, SGC-7901 and MKN-28). A a CCK-8 cell proliferation assay was performed to assess the effects of ABZ on cell viability and cell cycle changes were assessed using flow cytometry...
February 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28352193/cdkl1-promotes-tumor-proliferation-and-invasion-in-colorectal-cancer
#20
Chunzhi Qin, Li Ren, Meiling Ji, Shixu Lv, Ye Wei, Dexiang Zhu, Qi Lin, Pingping Xu, Wenju Chang, Jianmin Xu
BACKGROUND: CDKL1 is a member of the cell division cycle 2 (CDC2)-related serine threonine protein kinase family and is overexpressed in malignant tumors such as melanoma, breast cancer, and gastric cancer. OBJECTIVE: This study aimed to evaluate whether CDKL1 can serve as a potential molecular target for colorectal cancer therapy. MATERIALS AND METHODS: Expression of CDKL1 in colorectal cancer tissues and cell lines was measured by immunohistochemistry and Western blot, respectively...
2017: OncoTargets and Therapy
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