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https://www.readbyqxmd.com/read/29453077/molecular-docking-simulation-synthesis-and-3d-pharmacophore-studies-of-novel-2-substituted-5-nitro-benzimidazole-derivatives-as-anticancer-agents-targeting-vegfr-2-and-c-met
#1
Heba A Ibrahim, Fadi M Awadallah, Hanan M Refaat, Kamilia M Amin
No abstract text is available yet for this article.
January 31, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29449529/gambogenic-acid-inhibits-fibroblast-growth-factor-receptor-signaling-pathway-in-erlotinib-resistant-non-small-cell-lung-cancer-and-suppresses-patient-derived-xenograft-growth
#2
Linfeng Xu, Xiaoxiao Meng, Naihan Xu, Wenwei Fu, Hongsheng Tan, Li Zhang, Qianjun Zhou, Jianan Qian, Shiwei Tu, Xueting Li, Yuanzhi Lao, Hongxi Xu
Erlotinib resistance causes a high degree of lethality in non-small-cell lung cancer (NSCLC) patients. The high expression and activation of several receptor tyrosine kinases, such as JAK/STAT3, c-Met, and EGFR, play important roles in drug resistance. The development of tyrosine kinase inhibitors is urgently required in the clinic. Our previous study found that Gambogenic acid (GNA), a small molecule derived from the traditional Chinese medicine herb gamboge, induced cell death in several NSCLC cell lines through JAK/STAT3 inhibition...
February 15, 2018: Cell Death & Disease
https://www.readbyqxmd.com/read/29435981/forty-nine-gastric-cancer-cell-lines-with-integrative-genomic-profiling-for-development-of-c-met-inhibitor
#3
Hyun Jeong Kim, Sun Kyoung Kang, Woo Sun Kwon, Tae Soo Kim, Inhye Jeong, Hei-Cheul Jeung, Michael Kragh, Ivan D Horak, Hyun Cheol Chung, Sun Young Rha
Receptor tyrosine kinase MET (c-MET) has received considerable attention as a potential target for gastric cancer (GC) therapy and a number of c-MET inhibitors have been developed. For successful drug development, proper preclinical studies especially using patient derived cancer cell lines are very important. We profiled MET and MET-related characteristics in 49 GC cell lines to utilize them as models in preclinical studies of GC. Forty-nine cell lines were analyzed for genetic, biological, and molecular status to characterize MET and MET-related molecules...
February 13, 2018: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/29435059/macc1-and-hgf-are-associated-with-survival-in-patients-with-gastric-cancer
#4
Guokai Dong, Man Wang, Guangfu Gu, Shanshan Li, Xiaoming Sun, Zhouru Li, Hongxing Cai, Zhengqiu Zhu
Metastasis-associsated in colon cancer 1 (MACC1), a newly identified oncogene, promotes tumor cell proliferation and invasion. In the present study, the expression of MACC1, hepatocyte growth factor (HGF) and its receptor, MET proto-oncogene (c-Met), was investigated in human gastric cancer tissues and adjacent normal tissues by immunohistochemistry. The association between the expression levels of the proteins and the clinicopathological parameters of the tumors were statistically analyzed. Furthermore, lentiviral particles expressing MACC1 were used to infect the hepatic satellite cell (HSC) line LX2...
March 2018: Oncology Letters
https://www.readbyqxmd.com/read/29434932/quercetin-reverses-the-doxorubicin-resistance-of-prostate-cancer-cells-by-downregulating-the-expression-of-c-met
#5
Yan Shu, Bo Xie, Zhen Liang, Jing Chen
Chemotherapy is an irreplaceable treatment for prostate cancer. However, the acquisition of chemoresistance is a common and critical problem that requires urgent solutions for the effective treatment of this disease. The aim of the present study was to determine whether the combination of quercetin with doxorubicin reversed the resistance of prostate cancer cells to doxorubicin-based therapy. A prostate cancer (PC)3 cell line (PC3/R) with acquired doxorubicin-resistance was established. A significant drug-resistance to doxorubicin and high activation of the phosphoinositide 3-kinase/protein kinase-B (PI3K/AKT) pathway in PC3/R cells, compared with normal PC3 cells, was demonstrated...
February 2018: Oncology Letters
https://www.readbyqxmd.com/read/29432847/ascitic-fluid-from-advanced-ovarian-cancer-patients-compromises-the-activity-of-receptor-tyrosine-kinase-inhibitors-in-3d-cell-clusters-of-ovarian-cancer-cells
#6
Wafaa Hassan, Kenny Chitcholtan, Peter Sykes, Ashley Garrill
Ovarian cancer patients in the advanced stages of the disease show clinical ascites, which is associated with a poor prognosis. There is limited understanding of the effect of ascitic fluid on ovarian cancer cells and their response to anticancer drugs. We investigated the antitumour effects of EGFR/Her-2 (canertinib) and c-Met (PHA665752) inhibitors in a 3D cell model of three ovarian cancer lines. Single and combined inhibitor treatments affected cell growth of OVCAR-5 and SKOV-3 cell lines but not OV-90 cell line...
February 9, 2018: Cancer Letters
https://www.readbyqxmd.com/read/29431476/design-synthesis-and-molecular-modeling-study-for-some-new-2-substituted-benzimidazoles-as-dual-inhibitors-for-vegfr-2-and-c-met
#7
Heba A Ibrahim, Fadi M Awadallah, Hanan M Refaat, Kamilia M Amin
AIM: Computer-aided drug design techniques were adopted to design three series of 2-substituted-5-nitrobenzimidazole derivatives hybridized with piperzine 5a,b, oxadiazole 7a,b, 9, 14a-c and triazolo-thiadiazole moieties 12a-d, as VEGFR-2/c-Met kinase inhibitors. MATERIALS & METHODS: The designed compounds were synthesized adopting the chemical pathways outlined in schemes 1 and 2 to afford the desired three series followed by evaluating their inhibitory activities against VEGFR-2 and c-Met and in vitro anticancer activities...
February 12, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29427222/long-noncoding-rna-gaplinc-promotes-cells-migration-and-invasion-in-colorectal-cancer-cell-by-regulating-mir-34a-c-met-signal-pathway
#8
Yuqi Luo, Jun Ouyang, Donggen Zhou, Shizhen Zhong, Minjie Wen, Wentao Ou, Haitao Yu, Lin Jia, Yaoxin Huang
BACKGROUND: Gastric adenocarcinoma predictive long intergenic noncoding RNA (GAPLINC) has been detected in colorectal cancer (CRC) cells and reportedly performs many functions related to tumor proliferation and metastasis. Aim The present study aimed to comprehensively explore the biological functions of GAPLINC and their underlying mechanism in CRC cell. METHODS: The human cancer LncRNA PCR array was used to detect the differentially expressed long noncoding RNAs in human CRC samples...
February 9, 2018: Digestive Diseases and Sciences
https://www.readbyqxmd.com/read/29426928/lamb3-mediates-metastatic-tumor-behavior-in-papillary-thyroid-cancer-by-regulating-c-met-akt-signals
#9
Seung-Nam Jung, Hyun Sil Lim, Lihua Liu, Jae Won Chang, Young Chang Lim, Ki Sang Rha, Bon Seok Koo
Laminin subunit beta-3 (LAMB3) encodes one of the three subunits of LM-332, a protein of the extracellular matrix secreted by cultured human keratinocytes. While LAMB3 is involved in the invasive and metastatic abilities of several tumor types, including those found in the colon, pancreas, lung, cervix, stomach, and prostate, its mechanism of action in thyroid cancer has not been investigated previously. Our results show that LAMB3 is up-regulated in papillary thyroid cancer, and that its suppression reduces cell migration/invasion via down-regulation of epithelial‒mesenchymal transition-associated proteins (N-cadherin, vimentin, slug) and inhibition of matrix metalloproteinase 9...
February 9, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29422968/clinical-value-of-caga-c-met-pi3k-and-beclin-1-expressed-in-gastric-cancer-and-their-association-with-prognosis
#10
Xiaojun Huang, Chaoqun Wang, Jinmin Sun, Jun Luo, Jiangzhou You, Linchuan Liao, Mingyuan Li
Gastric cancer (GC) is the fourth most common type of malignant tumor worldwide, and causes the second highest number of cancer-associated mortalities in 2012. Gastric tumorigenesis is a multistep and multifactorial process. In the present study, tissue microarray and immunohistochemistry analysis were used to detect cytotoxin-associated gene A (CagA), c-Met, phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) and Beclin-1 expression in 121 GC tumors and 120 normal gastric tissues. The clinical relevance and prognostic implications of CagA, c-Met, PI3K and Beclin-1 expression in GC patients were analyzed...
January 2018: Oncology Letters
https://www.readbyqxmd.com/read/29421713/discovery-of-thinopyrimidine-triazole-conjugates-as-c-met-targeting-and-apoptosis-inducing-agents
#11
Linxiao Wang, Shan Xu, Xiaobo Liu, Xiuying Chen, Hehua Xiong, Shanshan Hou, Wensheng Zou, Qidong Tang, Pengwu Zheng, Wufu Zhu
Five series of N-methylpicolinamide moiety and thienopyrimidine moiety bearing triazole (21-26, 27-34, 35-41, 42-47 and 48-54) were designed and synthesized. And all the target compounds were evaluated for the IC50 values against three cancer cell lines (A549, HepG2 and MCF-7) and some selected compounds (43, 49 and 52) were further evaluated for the activity against c-Met, Flt-3, VEGFR-2, c-Kit and EGFR kinases. Moreover, SARs and docking studies indicated that thieno[3,2-d]pyrimidine bearing triazole moiety was privileged structure for the activity...
January 31, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29416931/single-oral-dose-acute-and-subacute-toxicity-of-a-c-met-tyrosine-kinase-inhibitor-and-cdk-4-6-inhibitor-combination-drug-therapy
#12
Brian Smith, Yi-Hsin Hsu, Rene Flores, Mihai Gagea, Suzanne Craig, Mien-Chie Hung
c-MET inhibitor, crizotinib, and CDK 4/6 inhibitor, palbociclib, have been evaluated in combination as cancer treatment in vitro. Because the toxicological data for the combination of these drugs is limited, we investigated the toxicity of the crizotinib and palbociclib combination in 80 ICR (CD-1) mice (average age = ~20 weeks). Treatments were arranged as a 2 × 2 × 2 factorial and included sex (female vs. male), crizotinib (0 or 4 mg), and palbociclib (0 or 1 mg). Drugs were administered to mice by oral gavage 24 hours (n = 40) and 7 days (n = 40) prior to the collection of blood and tissue samples to determine serum chemistry, hematology, and histopathology...
2018: American Journal of Cancer Research
https://www.readbyqxmd.com/read/29416799/correlation-among-genetic-variations-of-c-met-in-chinese-patients-with-non-small-cell-lung-cancer
#13
Jianchun Duan, Xiaodan Yang, Jun Zhao, Minglei Zhuo, Zhijie Wang, Tongtong An, Hua Bai, Jie Wang
Background: The purpose of our research was to determine the correlation of amplification, protein expression and somatic mutation of c-MET in IIIb-IV stage NSCLC (Non-small cell lung cancer). We also explored correlation of c-MET variation with clinical outcome. Results: c-MET expression was observed in 28.6% (56/196) cases, and among those 13.8% (27/196) were shown to be FISH positive. Only 2.67% patients in this study carried the c-MET mutation. Cases with c-MET FISH positive were all IHC positive ,but in IHC positive cases, only half were FISH positive...
January 5, 2018: Oncotarget
https://www.readbyqxmd.com/read/29416603/deguelin-suppresses-angiogenesis-in-human-hepatocellular-carcinoma-by-targeting-hgf-c-met-pathway
#14
Ming Li, Xinfang Yu, Wei Li, Ting Liu, Gang Deng, Wenbin Liu, Haidan Liu, Feng Gao
Angiogenesis plays a crucial role in the development of human hepatocellular carcinoma (HCC). In the present study, we found a natural compound, deguelin, has a profound anti-angiogenesis effect on HCC. Deguelin suppressed vascular endothelial growth factor (VEGF)-induced human umbilical vascular endothelial cells (HUVECs) proliferation, migration, invasion, and capillary-like tube formation in vitro and reduced tumor angiogenesis in vivo. We discovered that VEGF receptor-mediated signal transduction cascades in HUVECs were inhibited by deguelin...
January 2, 2018: Oncotarget
https://www.readbyqxmd.com/read/29411527/heterogeneity-based-multiple-mechanisms-in-the-resistance-to-osimertinib-azd9291-a-case-report
#15
Yutao Liu, Xuezhi Hao, Xingsheng Hu, Junling Li, Yan Wang, Hongyu Wang, Puyuan Xing, Weihua Li, Jianming Ying, Xiaohong Han, Yuankai Shi
Osimertinib is a novel, irreversible, mutant-selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor targeting EGFR mutations and the EGFR T790 mutation. Here, we report a woman with EGFR-mutated lung adenocarcinoma who, after 23-month treatment with gefitinib, developed the EGFR T790M mutation, which converted the T790M status from positive to negative before osimertinib treatment and developed MET amplification, leading to rapid progression on osimertinib in two months. Subsequent treatment with crizotinib and c-Met inhibitor plus gefitinib also failed to improve the clinical outcome, suggesting the potential existence of another resistance mechanism...
February 7, 2018: Thoracic Cancer
https://www.readbyqxmd.com/read/29409568/the-effect-of-selective-c-met-inhibitor-on-hcc-in-the-met-active-%C3%AE-catenin-mutated-mouse-model
#16
Na Zhan, Adeola Adebayo Michael, Kaiyuan Wu, Gang Zeng, Aaron Bell, Junyan Tao, Satdarshan P Monga
Simultaneous mutations in CTNNB1 and activation of c-MET occurs in 9-12.5% of patients with hepatocellular cancer (HCC). Co-expression of c-MET-V5 and mutant-β-catenin-Myc in mouse liver by sleeping beauty transposon/transposase and hydrodynamic tail vein injection (SB-HTVI) led to development of HCC with 70% molecular identity to the clinical subset. Using this model, we investigated the effect of EMD1214063, a highly selective c-MET inhibitor. Five weeks after SB-HTVI when tumors were established, EMD1214063 (10mg/kg) was administered by gastric lavage as a single-agent on 5-days-on/3-days-off schedule, compared to vehicle only control...
February 6, 2018: Gene Expression
https://www.readbyqxmd.com/read/29407963/identification-of-novel-n1-2-aryl-1-3-thiazolidin-4-one-n3-aryl-ureas-showing-potent-multi-tyrosine-kinase-inhibitory-activities
#17
Baohui Qi, Ying Yang, Huan He, Xupeng Yue, Yuting Zhou, Xing Zhou, Yuying Chen, Min Liu, Anmian Zhang, Fachang Wei
A total of 29 novel compounds bearing N1-(2-aryl-1, 3-thiazolidin-4-one)-N3-aryl ureas were designed, synthesized and evaluated for their biological activities. The structure-activity relationships (SARs) and binding modes of this series of compounds were clarified together. Compound 29b was identified possessing high potency against multi-tyrosine kinases including Ron, c-Met, c-Kit, KDR, Src and IGF-1R, etc. In vitro antiproliferation and cytotoxicity of compound 29b against A549 cancer cell line were confirmed by IncuCyte live-cell imaging...
January 27, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29405820/the-irreversible-erbb1-2-4-inhibitor-neratinib-interacts-with-the-parp1-inhibitor-niraparib-to-kill-ovarian-cancer-cells
#18
Laurence Booth, Jane L Roberts, Peter Samuel, Francesca Avogadri-Connors, Richard E Cutler, Alshad S Lalani, Andrew Poklepovic, Paul Dent
The irreversible ERBB1/2/4 inhibitor neratinib has been shown to rapidly down-regulate the expression of ERBB1/2/4 as well as the levels of c-MET, PDGFRα and mutant RAS proteins via autophagic degradation. Neratinib interacted in an additive to synergistic fashion with the approved PARP1 inhibitor niraparib to kill ovarian cancer cells. Neratinib and niraparib caused the ATM-dependent activation of AMPK which in turn was required to cause mTOR inactivation, ULK-1 activation and ATG13 phosphorylation. The drug combination initially increased autophagosome levels followed later by autolysosome levels...
February 6, 2018: Cancer Biology & Therapy
https://www.readbyqxmd.com/read/29400000/correlation-analysis-of-mesenchymal-epithelial-transition-factor-protein-and-human-epidermal-growth-receptor%C3%A2-2-protein-expression-in-1479-cases-of-lung-adenocarcinoma-in-china
#19
Lin Yang, Yiqun Che, Lei Guo, Bo Zheng, Bingning Wang, Zhenxi Yang, Yixiang Zhu, Junling Li
BACKGROUND: To investigate the correlation between mesenchymal-epithelial transition factor (C-Met) and human epidermal growth receptor 2 (HER2) protein expression in primary lung adenocarcinoma tissues. METHOD: A total of 1479 resected primary lung adenocarcinoma patients were enrolled in the present study for detecting of C-Met and HER2 protein by immunohistochemistry, and correlation analysis was made between the above two biomarkers and related clinicopathological features...
February 4, 2018: Thoracic Cancer
https://www.readbyqxmd.com/read/29399387/analysis-of-pd1-pdl1-pdl2-expression-and-t-cells-infiltration-in-1014-gastric-cancer-patients
#20
Xiaofang Xing, Jianping Guo, Xianzi Wen, Guangyu Ding, Bo Li, Bin Dong, Qin Feng, Shen Li, Jian Zhang, Xiaojing Cheng, Ting Guo, Hong Du, Ying Hu, Xiaohong Wang, Lin Li, Qingda Li, Meng Xie, Liting Li, Xiangyu Gao, Fei Shan, Ziyu Li, Xiaomin Ying, Tao Zhou, Jiping Wang, Jiafu Ji
Although immune checkpoint blockade have demonstrated promising results, their effects on gastric cancer (GC) are under investigation. Understanding the clinical significance of PD1 and its ligands' expression, together with T cell infiltration might provide clues for biomarkers screening in GC immunotherapy. Immunohistochemistry were performed on a tissue microarray including 1,014 GC specimens using PD1, PDL1 and PDL2 antibodies. T cell markers CD3 and CD8 were also stained and quantified by automated image analysis...
2018: Oncoimmunology
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