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Anti-cancer Drugs

Samantha X Y Wang, Bing M Zhang, Heather A Wakelee, Michael Z Koontz, MingGui Pan, Maximilian Diehn, Christian A Kunder, Joel W Neal
The mesenchymal-to-epithelial transition (MET) gene is altered and becomes a driver mutation in up to 5% of non-small-cell lung cancer (NSCLC). We report our institutional experience treating patients with MET exon 14 skipping (METex14) mutations, including responses to the MET inhibitors crizotinib and cabozantinib. We identified cases of NSCLC with METex14 mutations using an institutionally developed or commercial next-generation sequencing assay. We assessed patient and disease characteristics by retrospective chart review...
February 12, 2019: Anti-cancer Drugs
Eleana Hatzidaki, Panagiotis Parsonidis, Panagiotis Apostolou, Vasiliki Daikopoulou, Ioannis Papasotiriou
The Ras-Raf-MEK1/2-ERK1/2 pathway is an attractive target for the development of anticancer agents because of the high prevalence of ERK activation in human cancers. However, resistance is often developed despite initial clinical response, most likely because of activation of cross-talk pathways. In Research Genetic Cancer Center (RGCC), we are in the process of synthesizing a novel ERK inhibitor, targeting the final stage of the pathway, thus minimizing cross-talk. We have synthesized an intermediate molecule -RGCC416 - and tested its biological activity...
February 6, 2019: Anti-cancer Drugs
Rui Lou, Shuchen Dong, Chen Shi, Xiaoyue Xu, Rong Ma, Jianzhong Wu, Jifeng Feng, Haixia Cao
Liver X receptors are recognized as important regulators of cholesterol, fatty acid metabolism, inflammatory responses, and glucose homeostasis. The antineoplastic properties of synthetic liver X receptor (LXR) agonists (T0901317 and GW3965) have been reported in human carcinomas. Epidermal growth factor tyrosine kinase inhibitor (EGFR-TKI) is a first-line treatment for non-small-cell lung cancer patients with EGFR mutations. We used scratch and transwell assays to analyze cell migration and invasion. We evaluated tumor migration and invasion in vitro using a fluorescent orthotopic lung cancer model...
February 4, 2019: Anti-cancer Drugs
Rong Chen, Lu Zhang
Cervical cancer is the second most common gynecological malignancy worldwide and the tumorigenesis mechanisms of cervical cancer are still unclear. This study aimed to reveal the role of miR-29a in cervical cancer. The expression level of miR-29a and CDC42 was measured using qRT-PCR. Cell proliferation, apoptosis, migration, and invasion were detected using colony formation, flow cytometry analysis, wound-healing assay, and Transwell assay, respectively. Luciferase reporter assay was used to determine the binding of miR-29a with CDC42...
February 4, 2019: Anti-cancer Drugs
Kok-Tong Tan, Meng-Xian Lin, Shih-Chao Lin, Yu-Tang Tung, Sheng-Hao Lin, Chi-Chien Lin
The present study was carried out to explore the effect of sinensetin in human T-cell lymphoma Jurkat cells and to reveal the underlying molecular mechanisms. We found that sinensetin significantly impeded Jurkat cell proliferation in a dose-dependent and time-dependent manner. Additionally, sinensetin treatment triggered apoptosis and autophagy in Jurkat cells. The apoptosis induction was related to a loss of mitochondrial membrane potential and to increased caspase-3/-8/-9 and poly(ADP-ribose) polymerase (PARP) cleavage...
January 29, 2019: Anti-cancer Drugs
Jian Wang, Zhenyu Li, Hong Mei, Dejun Zhang, Gang Wu, Tao Zhang, Zhenyu Lin
Although both antiepidermal growth factor receptor and vascular endothelial growth factor therapies have been shown to be effective against colorectal cancer (CRC), their beneficial effects are limited to a small proportion of patients and are not sustainable. Cyclin-dependent kinase 7 (CDK7) is an important regulator of the transcriptional machinery. Use of small-molecule inhibitors of the transcriptional machinery has shown promising selectivity for cancer cells and potent antiproliferative effects. In this study, the effects of a covalent CDK7 inhibitor THZ1 as a potent anti-CRC compound were evaluated in vitro and in vivo...
January 28, 2019: Anti-cancer Drugs
Gerardo D Anaya-Eugenio, Tehane Ali, Liva Harinantenaina Rakotondraibe, Esperanza Carcache de Blanco
In our continuing effort to identify bioactive secondary metabolites from natural sources, the antiproliferative activity of 23 compounds, previously isolated from Penicillium concentricum, was assessed using the sulforhodamine B assay. The cytotoxic effect was determined against HeLa cervical, HT-29 colon, MDA-MB-321 breast, PC-3, and DU-145 prostate cancer cell lines. Compounds were also tested in the mitochondrial transmembrane potential (MTP) and nuclear factor kappa B (NF-κB) target-based assays. The results showed that 2-bromogentisyl alcohol (2) and 3-hydroxy-benzenemethanol (8) exhibited the highest cytotoxic activity against different cancer cell lines...
January 25, 2019: Anti-cancer Drugs
Jie Du
Esophageal cancer (EC) is a common cancer worldwide. Sine oculis homeobox homolog (SIX3) is a human transcription factor that regulates the progression of vertebrate eye and fetal forebrain. However, studies on the function of SIX3 in human tumorigenesis remain rare. In this study, we aim to evaluate the role and the significance of SIX3 in EC. The TCGA database and clinical samples were used to assess the expression of SIX3 in EC patients. The Kaplan-Meier method and Cox's proportional hazards model were performed to analyze the correlations between SIX3 expression and EC clinical outcomes...
January 21, 2019: Anti-cancer Drugs
Shenglong Li, Xixi Wu, Peng Chen, Yi Pei, Ke Zheng, Wei Wang, Enduo Qiu, Xiaojing Zhang
The US Food and Drug Association has approved interferon-α (IFN-α) and interleukin-2 (IL-2) as adjuvant therapy in malignant melanoma. The objective of the study was to compare efficacy and safety of subcutaneous interferon-α with continuous intravenous IL-2 in Chinese patients with malignant melanoma. A total of 250 patients with unresectable malignant melanoma were subjected to randomized in 1 : 1 ratio. Patients received subcutaneous 9×10 IU/m IFN-α (IFN-α group, n=125) or continuous intravenous 9×10 IU/m IL-2 (IL-2 group, n=125) at every 21 days for 4 months...
January 16, 2019: Anti-cancer Drugs
Juliane Liese, Tobias M Hinrichs, Matthias Lange, Simone Fulda
Hepatocellular carcinoma (HCC) is the most common liver malignancy, and the lack of effective chemotherapies underlines the need for novel therapeutic approaches for this disease. Recently, we discovered a novel synergistic induction of cell death by combining sorafenib, the only routinely used palliative chemotherapeutic agent, and the triterpenoid oleanolic acid (OA). However, the underlying mechanisms of action have remained obscure. Here, we report that sorafenib and OA acted in concert to trigger mitochondria-mediated apoptotic cell death, which is dependent on reactive oxygen species (ROS)...
January 11, 2019: Anti-cancer Drugs
Xiaoshu Zhou, Rui Zhou, Qianwen Li, Xiaohua Jie, Jiaxin Hong, Yan Zong, Xiaorong Dong, Sheng Zhang, Zhenyu Li, Gang Wu
Cardamonin, a natural chalcone compound, has been reported to exert anticancer effects in several cancers. However, the specific pharmacological actions of cardamonin on human non-small-cell lung cancer (NSCLC) and the potential mechanisms still remain obscure. Here, we investigated the antineoplastic role of cardamonin in NSCLC both in vitro and in vivo. The proliferation of five NSCLC cell lines was inhibited in a dose-dependent and time-dependent manner with cardamonin treatment. In A549 and H460 cells, cardamonin induced apoptosis by activating caspase-3, upregulating Bax, and downregulating Bcl-2...
January 11, 2019: Anti-cancer Drugs
Olga Nigro, Tiziana Tartaro, Alessandro Tuzi, Alice Giaquinto, Matteo B Suter, Graziella Pinotti
Neurofibromatosis type 2 (NF-2) is an autosomal dominant inherited disease caused by heterozygous mutations in the NF-2 tumor suppressor gene. It is characterized by the development of multiple benign tumors in the central nervous system. A majority of these tumors can be treated with surgery or radiotherapy in the case of the symptomatic disease. Cytotoxic chemotherapy has no established role in the treatment of NF-2. Vascular endothelial growth factor (VEGF) is a critical mediator of tumor angiogenesis and vessel permeability...
January 11, 2019: Anti-cancer Drugs
Tevhide Sahin, Omer Dizdar, Nuriye Ozdemir, Nurullah Zengin, Ozturk Ates, Berna Oksuzoglu, Mehmet A N Sendur, Burak Bilgin, Metin Demir, Utku B Bozbulut, Sadettin Kilickap, Suayib Yalcin
The purpose of this study was to identify the frequency of chemotherapy-induced amenorrhea and associated factors thereof in premenopausal female patients diagnosed with colon cancer. Premenopausal female patients under the age of 50 years who were diagnosed with stages I, II, and III colon cancer were included. A questionnaire surveying personal history including menarche, comorbidities, drugs, other clinical features, and menstrual history during and after completion of chemotherapy was filled by the patients during outpatient visits...
January 11, 2019: Anti-cancer Drugs
Olga Nigro, Alessia Pastore, Tiziana Tartaro, Elena Bolzacchini, Alessandro Tuzi, Graziella Pinotti
Renal cell carcinoma (RCC) is one of the most frequent malignancies of the adults. Its incidence has been increasing steadily by 2-4% each year. Up to 30% of patients present with metastases at diagnosis. It is a highly vascularized cancer because of the hypoxia-induced factor stabilization as a consequence of von Hippel-Lindau inactivation. Hypoxia-induced factor accumulation leads to transactivation of molecules involved in angiogenesis including vascular endothelial growth factor (VEGF) and platelet-derived growth factor...
January 11, 2019: Anti-cancer Drugs
Jan P Kleinjan, Ithamar Brinkman, Robbert Bakema, Jelmer J van Zanden, Johan M van Rooijen
OBJECTIVE: Certain polymorphisms of the DPYD gene encoding for the dihydropyrimidine dehydrogenase (DPD) enzyme are associated with fluoropyrimidine-induced toxicity. Dose reductions of the fluoropyrimidine prodrug capecitabine are recommended for patients carrying these DPYD variants to prevent toxicities. Capecitabine dose escalation after an initial genotype-guided dose reduction is advocated when treatment is well tolerated. However, practical guidelines on how to implement these dose escalations are lacking...
January 8, 2019: Anti-cancer Drugs
Ya Liu, Hongying Zhou, Tao Yi, Hongjing Wang
Pyrimethamine has been used principally to treat infections from protozoan parasites. Although previous studies have shown that pyrimethamine exhibited anticancer activity by inducing cellular apoptosis, there are none that show that pyrimethamine possesses anticancer activity with respect to ovarian cancer. We examined the roles of pyrimethamine on apoptosis and proliferation, DNA damage, and cell cycle distribution of human ovarian cancer cell lines in vitro. To investigate the antitumor efficacy of pyrimethamine in vivo, we established two intraperitoneal ovarian carcinoma models in nude mice...
January 5, 2019: Anti-cancer Drugs
Lihua Wang, Zhihua Wang, Liuye Huang, Chengrong Wu, Bo Zhang
Pancreatic cancer is one of the leading causes of solid carcinoma with the worst survival rate. The reasons for the worst survival rate include the lack of biomarkers for early detection, diagnosis at a late stage, and the limitation of the current therapy. Further study to investigate the underlying molecular mechanism in pancreatic cancer patients is necessary. A previous study showed that the miR-29b expression level is dysregulated, suggesting that it may serve an important function in pancreatic cancer...
December 31, 2018: Anti-cancer Drugs
Yinan Su, Mingqing Zhang, Lin Zhang, Shuo Chen, Dan Zhang, Xipeng Zhang
Colorectal cancer (CRC) is the third most common cancer worldwide. This study aimed to explore the regulatory mechanisms of miRNAs in CRC. Differentially expressed miRNAs (DEMs) and differentially expressed genes (DEGs) in CRC tissue samples compared with control samples in mRNA and miRNA datasets were screened. Functional and pathway enrichment analysis of the DEGs was carried out. Targets of the DEMs were identified. Overlaps between the DEGs and targets of DEMs were selected. The miRNA-mRNA regulatory network of these overlaps was constructed and visualized...
December 28, 2018: Anti-cancer Drugs
Pantelis Litsardopoulos, Christos Bikas, Dimitra Dimitropoulou, Chrysa Lykoura, Garifallia G Anastopoulou, Panagiotis Karanasios, Alexandra Makridou, Andreas A Argyriou
So far, very few cases describing an interrelation between chemotherapy and Guillain-Barré syndrome have been published. We describe the first case of a paraparetic, pure acute motor axonal neuropathy variant of Guillain-Barré syndrome, early complicating protein-bound paclitaxel (nab-paclitaxel/abraxane) chemotherapy (first and sole session at a 350 mg dose) in a female patient with metastatic breast cancer. Although our patient was treated with the standard regimen of intravenous immunoglobulin for 5 days, she showed no evidence of motor improvement and died 1 month after the onset of the neurological deficit...
December 26, 2018: Anti-cancer Drugs
Yuwen Zhou, Jing Zhang, Dan Pu, Feng Bi, Ye Chen, Jiyan Liu, Qiu Li, Hongfeng Gou, Bing Wu, Meng Qiu
This study aimed to explore the correlation between survival and tumor calcification in patients with metastatic colorectal cancer who received cetuximab combined with chemotherapy. The study was a single-center retrospective analysis that enrolled 111 patients who had received therapy between April 2011 and October 2016. Tumor calcification and treatment efficacy were evaluated independently by radiologists on the basis of computed tomography scans. Clinical characteristics and follow-up data were collected from electronic medical records...
December 18, 2018: Anti-cancer Drugs
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