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Current Cancer Drug Targets

Ling Ma, Xia Zhang, Zhiqiong Wang, Lifang Huang, Fankai Meng, Lihua Hu, Yan Chen, Jia Wei
Enhancer of zeste homolog-2 (EZH2), a histone methyltransferase that regulates histone H3 methylation of lysine27 (H3K27me3), is involved in the pathogenesis of myelodysplastic syndrome (MDS). Targeting epigenetic regulators has been identified as a potential treatment target in MDS chemotherapy. Curcumin, a natural compound extracted from turmeric, was found to possess a wide range of anticancer activities in various tumors. This study was designed to investigate the inhibitory effect and action mechanism of curcumin in myelodysplastic syndrome (MDS) in vitro and in vivo...
February 12, 2019: Current Cancer Drug Targets
Nousheen Bibi, Sajid Rashid, Judith Nicholson, Mark Malloy, Rob O'Neill, David Blake, Ted Hupp
BACKGROUND: The rapid expansion of genome wide profiling techniques offers the opportunity to utilize various types of information collectively in the study of human health and disease. Overexpression of Polo like kinase 1 (PLK1) is associated with oesophageal adenocarcinoma (OAC), however biological functions and molecular targets of PLK1 in OAC are still unknown. OBJECTIVES: Here we performed integrative analysis of two "omics" data sources to reveal high level interactions of PLK1 associated with OAC...
February 10, 2019: Current Cancer Drug Targets
Peihao Fan, Nanyi Wang, Lirong Wang, Xiang-Qun Xie
BACKGROUNDS: Autophagy and apoptosis are the basic physiological processes in cells that clean up aged and mutant cellular components or even the entire cells. Both autophagy and apoptosis are disrupted in most major diseases such as cancer and neurological disorders. Recently, increasing attention is paid to understand the crosstalk between autophagy and apoptosis due to their tightly synergetic or opposite functions in several pathological processes. OBJECTIVE: This study aims to assist autophagy and apoptosis-related drug research, clarify the intense and complicated connections between two processes, and provide a guide for novel drug development...
February 6, 2019: Current Cancer Drug Targets
Xiaohua Zhang, Fengbin Gao, Shan Zhong
BACKGROUND: Malignant pheochromocytoma (mPCC) is an uncommon tumor with poor prognosis, and no effective therapeutic strategy exists. Discovering new and effective therapeutic strategies to improve prognosis is an urgent need. OBJECTIVE: To investigate whether combinatorial inhibition of both mTORC2 and Hsp90 in PC12 cells could lead to a distinctly antitumor effect in vitro and in vivo that was greater than inhibition of mTORC2 or Hsp90 alone. METHODS: Targeting mTORC2 was assessed by knockdown of Rictor using shRNA, and 17-AAG was used to inhibit Hsp90 function...
February 6, 2019: Current Cancer Drug Targets
Yuanyuan Wang, Qian Xing, Xue Chen, Jianbo Wang, Shanghui Guan, Xuan Chen, Peng Sun, Mingxia Wang, Yufeng Cheng
BACKGROUND: Leucine-rich-alpha-2-glycoprotein1 (LRG1) is a new oncogene-related gene, which has been verified important to the development and poor prognosis of human cancers. However, whether it participates in esophageal squamous cell carcinoma (ESCC) progression remains unclear. OBJECTIVE: To investigate the expression level and functional influence of LRG1 in ESCC. METHOD: The expression of LRG1 was evaluated on the mRNA and protein level in ESCC patients...
February 3, 2019: Current Cancer Drug Targets
Laura Pietrovito, Giuseppina Comito, Matteo Parri, Elisa Giannoni, Paola Chiarugi, Maria Letizia Taddei
BACKGROUND: The bisphosphonate Zoledronic acid (ZA) is a potent osteoclast inhibitor currently used in the clinic to reduce osteoporosis and cancer-induced osteolysis. Moreover, ZA exerts an anti-tumor effect in several tumors. Despite this evidence, the relevance of ZA in prostate cancer (PCa) is not completely understood. OBJECTIVE: To investigate the effect of ZA administration on the invasive properties of PC3 cells, which are characterised by RhoA-dependent amoeboid motility...
January 15, 2019: Current Cancer Drug Targets
Subrata Laskar, Omar Espino, Debasish Bandyopadhyay
BACKGROUND: Abrus precatorius Linn. (Kunch in Bengali) is widely spread in tropical and sub-tropical regions. It is a typical plant species which is well-known simultaneously as folk medicine and for its toxicity. OBJECTIVE: Phytoceutical investigation of the white variety seeds of Abrus precatorius Linn. METHOD: Traditional extraction, separation, isolation, and purification processes were followed. The structure was elucidated by various spectral analyses and the solid-state structure of this indole-alkaloid has been determined by X-ray crystallographic analysis...
January 10, 2019: Current Cancer Drug Targets
Yufeng Wu, Zhen He, Shaomei Li, Hong Tang, Lili Wang, Sen Yang, Bing Dong, Jianjun Qin, Yue Sun, Han Yu, Yu Zhang, Yi Zhang, Yongjun Guo, Qiming Wang
BACKGROUND: Gefitinib is well-known as a tyrosine kinase inhibitor targeting non-small-lung-cancer (NSCLC) containing EGFR mutations. However, its effectiveness in treating mucoepidermoid carcinoma (MEC) without such EGFR mutations suggests additional targets. OBJECTIVE: The CRTC1-MAML2 (C1-M2) fusion typical for MEC has been proposed to be a gefitinib target. METHOD: To test this hypothesis, we developed a set of siRNAs to down-regulate C1-M2 expression...
January 3, 2019: Current Cancer Drug Targets
Qi-Zhe Gong, Di Xiao, Gui-Yi Gong, Jian Xu, Xiao-Dong Wen, Feng Feng, Wei Qu
BACKGROUND: Since signal transducer and activator of transcription 3 (STAT3) is aberrantly activated in hepatocellular carcinoma (HCC) and plays a key role in this tumor progression, inhibition of the STAT3 signaling pathway has been considered as an effective therapeutic strategy for suppressing HCC development. OBJECTIVE: In this study, we investigated the anti-cancer effects of EH-42 on HCC cells and tried to explain the underlying mechanism. METHODS: MTT assay, colon formation assay and AnnexinV-FITC/PI double-staining assay were performed to assess the effects of EH-42 on cell growth and survival...
December 25, 2018: Current Cancer Drug Targets
Bo-Shen Gong, Rui Wang, Hong-Xia Xu, Ming-Yong Miao, Zhen-Zhen Yao
Cancer is characterized by high mortality and low curability. Recent studies have shown that the mechanism of tumor resistance involves not only endogenous changes to tumor cells, but also to the tumor microenvironment (TME), which provides the necessary conditions for the growth, invasion, and metastasis of cancer cells, akin to Stephen Paget's hypothesis of "seed and soil." Hence, the TME is a significant target for cancer therapy via nanoparticles, which can carry different kinds of drugs targeting different types or stages of tumors...
December 19, 2018: Current Cancer Drug Targets
Tatsuya Nagano, Motoko Tachihara, Yoshihiro Nishimura
Lung cancer is the leading cause of cancer death worldwide. Molecular targeted therapy has greatly advanced the field of treatment for non-small cell lung cancer (NSCLC), which accounts for the majority of lung cancers. Indeed, gefitinib, which was the first molecular targeted therapeutic agent, has actually doubled the survival time of NSCLC patients. Vigorous efforts of clinicians and researchers have revealed that lung cancer develops through the activating mutations of many driver genes including the epidermal growth factor receptor (EGFR), anaplastic lymphoma kinase (ALK), c-ros oncogene 1 (ROS1), v-Raf murine sarcoma viral oncogene homolog B (BRAF), and rearranged during transfection (RET) genes...
December 9, 2018: Current Cancer Drug Targets
Xiaohui Pu, Jia Li, Peng Qiao, Mengmeng Li, Haiyan Wang, Lanlan Zong, Qi Yuan, Shaofeng Duan
BACKGROUND: With the development of nanotechnology, nanocarrier has widely applied in such fields as drug delivery, diagnostic and medical imaging and engineering in recent years. Among all of the available nanocarrier, mesoporous silica nanoparticles (MSNs) have become a hot issue because of their unique properties, such as large surface area and voidage, tunable drug loading capacity and release kinetics, good biosafety and easily modified surface. OBJECTIVES: We described the most recent progress in silica-assisted drug delivery and biomedical applications according to different types of Cargo in order to allow researchers to quickly learn about of the advance in this field...
December 5, 2018: Current Cancer Drug Targets
S Jemimah Naine, C Subathra Devi, C George Priya Doss, D Kumar Thirumal
BACKGROUND: The major attention has been received by the natural products in the prevention of diseases due to their pharmacological role. OBJECTIVE: The major focus of the study was to search for highly potential anti-cancer compounds from marine Streptomyces sp. VITJS4 (NCIM No. 5574). METHOD: Cytotoxic assay was examined by MTT assay on HepG2 cells. Bioassay-guided fractionation of the ethyl acetate extract from the fermented broth led to the isolation of the compound...
November 27, 2018: Current Cancer Drug Targets
Nousheen Bibi, Zahida Parveen, Muhammad Sulaman Nawaz, Mohammad Amjad Kamal
Cancer remains the one most serious disease worldwide. Robust metabolism is hallmark of the cancer. PPAT (phosphoribosyl pyrophosphate amidotransferase) catalyzes the first committed step of de novo purine biosynthesis. Hence PPAT, the key regulatory spot in De novo purine nucleotide biosynthesis is an attractive and credible drug target for leukemia and other cancer therapeutics. In the present study detailed computational analysis has been performed for PPAT protein the key enzyme in de novo purine biosynthesis is inhibited by many folate derivatives, hence we aimed to investigate and gauge the inhibitory effect of antifolate derivatives; lomexterol (LTX) methotrexate (LTX), and pipretixin (PTX) with human PPAT to effectively capture and inhibit De novo purine biosynthesis pathway...
November 26, 2018: Current Cancer Drug Targets
Konstantinos Sapalidis, Christoforos Kosmidis, Stela Laskou, Athanasios Katsaounis, Stylianos Mantalobas, Ioannis Passos, Nikolaos Michalopoulos, Aikaterini Amaniti, Chrysa Sardeli, Paul Zarogoulidis
No abstract text is available yet for this article.
2019: Current Cancer Drug Targets
Ruiwen Zhang
No abstract text is available yet for this article.
2019: Current Cancer Drug Targets
Lei Lei, Yuan Wang, Yi-Wen Zheng, Liang-Ru Fei, Hao-Yue Shen, Zhi-Han Li, Wen-Jing Huang, Juan-Han Yu, Hong-Tao Xu
Nemo-like kinase (NLK) is an evolutionarily conserved MAP kinase-related kinase involved in the pathogenesis of several human cancers. We examined the expression of NLK in lung cancer tissues through western blot analysis. We enhanced or knocked down NLK expression by gene transfection or RNA interference, respectively, in lung cancer cells and examined expression alterations of key proteins in the Wnt signaling pathway and in epithelial-mesenchymal transition (EMT). We also examined the roles of NLK in the proliferation and invasiveness of lung cancer cells by cell proliferation, colony formation, and Matrigel invasion assays...
November 19, 2018: Current Cancer Drug Targets
Omel Baneen Qallandar, Faeza Ebrahimi, Farhadul Islam, Riajul Wahab, Bin Qiao, Peter Reher, Vinod Gopalan, Alfred King-Yin Lam
BACKGROUND: Co-culture of cancer cells with alveolar bone cells could modulate bone invasion and destructions. However, the mechanisms of interaction between oral squamous cell carcinoma (OSCC) and bone cells remain unclear. OBJECTIVE: The aim of this study is to analyse the direct and indirect effects of OSCC cells in the stimulation of osteolytic activity and bone invasion. METHOD: Direct co-culture was achieved by culturing OSCC (TCA8113) with a primary alveolar bone cell line...
November 2, 2018: Current Cancer Drug Targets
Yige Qi, Ting Yan, Lu Chen, Qiang Zhang, Weishu Wang, Xu Han, Dangdang Li, Jinming Shi, Guangchao Sui
The oncoprotein binding (OPB) domain of Yin Yang 1 (YY1) consists of 26 amino acids between G201 and S226, and is involved in YY1 interaction with multiple oncogene products, including MDM2, AKT, EZH2 and E1A. Through the OPB domain, YY1 promotes the oncogenic or proliferative regulation of these oncoproteins in cancer cells. We previously demonstrated that a peptide with the OPB sequence blocked YY1-AKT interaction and inhibited breast cancer cell proliferation. In the current study, we characterized the OPB domain and determined a minimal region for peptide design to suppress cancer cells...
October 31, 2018: Current Cancer Drug Targets
Caixia Liang, Ningning Zhang, Qiaoyun Tan, Shuxia Liu, Rongrong Luo, Yanrong Wang, Yaunkai Shi, Xiaohong Han
BACKGROUND: Crizotinib established the position of anaplastic lymphoma kinase-tyrosine kinase inhibitors (ALK-TKI) in the treatment of non-small cell lung cancer(NSCLC) while the therapy-resistance hindered those patients from benefitting continuously from the treatment. CT-707 is an inhibitor of ALK/focal adhesion kinase (FAK) and IGFR-1. H2228CR (crizotinib resistance, CR) and H3122CR NSCLC cell lines were generated from the parental cell line H2228 (EML4-ALK, E6a/b:A20, variant 3) and H3122(EML4-ALK, E13:A20, variant 1), respectively...
October 31, 2018: Current Cancer Drug Targets
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