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Anti-cancer Drugs

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https://www.readbyqxmd.com/read/29120871/a-srsf1-self-binding-mechanism-restrains-mir505-3p-from-inhibiting-proliferation-of-neural-tumor-cell-lines
#1
Kan Yang, Li Tong, Kai Li, Yuxun Zhou, Junhua Xiao
Srsf1 has currently been demonstrated to be an oncogene that is precisely autoregulated for normal physiology. Although Mir505-3p has been reported as one of the regulatory miRNAs of Srsf1 in mouse embryonic fibroblast (MEF), the inhibitory effect of Mir505-3p on Srsf1 is poorly described in neural tumors. Whether SRSF1 autoregulation interferes with miRNA targeting on the Srsf1 transcript is unclear. In this work, we screened out one target site, out of three potential target sites on 3' UTR of Srsf1 transcript, that was required for Mir505-3p targeting...
November 8, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29099418/temozolomide-treatment-of-a-malignant-pheochromocytoma-and-an-unresectable-max-related-paraganglioma
#2
Alfonso M Ferrara, Giuseppe Lombardi, Ardi Pambuku, Domenico Meringolo, Roberta Bertorelle, Margherita Nardin, Francesca Schiavi, Maurizio Iacobone, Giuseppe Opocher, Vittorina Zagonel, Stefania Zovato
Pheochromocytomas (PCCs) and paragangliomas (PGLs) are neuroendocrine tumors with a strong genetic background. The mainstay of treatment for PCC/PGLs is surgery. However, for unresectable lesions, no curative treatment is currently available. Temozolomide (TMZ) has been shown to determine radiological and biochemical response in malignant PCC/PGLs. We report two cases of PCC/PGLs treated with TMZ. Case 1 is a 51-year-old man with local and distant recurrence (liver and bone metastases) of right adrenal PCC...
November 2, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29099417/cell-cycle-dependent-translocation-and-regulatory-mechanism-of-cacybp-sip-in-gastric-cancer-cells
#3
Yang Chen, Kun Zhang, Xiaosu Wang, Qiaoneng Li, Qingfeng Wu, Xiaoxuan Ning
Our previous results showed that calcyclin-binding protein/Siah-1-interacting protein (CacyBP/SIP) inhibits the proliferation and tumorigenicity of gastric cancer; however, the exact mechanism remains unclear, especially from the aspect of cell cycle. The subcellular localization of CacyBP/SIP, Siah-1, and Skp1 in SGC7901 gastric cancer cells was assessed by immunofluorescence after cell cycle synchronization. Levels of CacyBP/SIP, Siah-1, Skp1, β-catenin, and p-ERK1/2 were analyzed by western blotting. CacyBP/SIP phosphorylation (p-CacyBP/SIP) and the combining capacity of Siah-1 and Skp1 with CacyBP/SIP in nucleoprotein were determined by immunoprecipitation...
November 2, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29099416/autophagy-and-doxorubicin-resistance-in-cancer
#4
Chao Chen, Lu Lu, Shichao Yan, Huimei Yi, Hui Yao, Di Wu, Guangchun He, Xiaojun Tao, Xiyun Deng
Doxorubicin (DOX), also known as adriamycin, is a DNA topoisomerase II inhibitor and belongs to the family of anthracycline anticancer drugs. DOX is used for the treatment of a wide variety of cancer types. However, resistance among cancer cells has emerged as a major barrier to effective treatment using DOX. Currently, the role of autophagy in cancer resistance to DOX and the mechanisms involved have become one of the areas of intense investigation. More and more preclinical data are being obtained on reversing DOX resistance through modulation of autophagy as one of the promising therapeutic strategies...
November 2, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29084003/a-genome-wide-comprehensive-analysis-of-alterations-in-driver-genes-in-non-small-cell-lung-cancer
#5
Jun Yi, Xiang Wei, Xinqiang Li, Lei Wan, Jiashou Dong, Rui Wang
Lung cancer is one of the most common malignancies and the leading cause of cancer-related deaths worldwide. Although many oncogenes and tumor suppressors have been uncovered in the past decades, the pathogenesis and mechanisms of lung tumorigenesis and progression are unclear. The advancement of high-throughput sequencing technique and bioinformatics methods has led to the discovery of some unknown important protein-coding genes or noncoding RNAs in human cancers. In this study, we tried to identify and validate lung cancer driver genes to facilitate the diagnosis and individualized treatment of patients with this disease...
October 27, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29049036/histone-deacetylase-inhibitor-bg45-mediated-ho-1-expression-induces-apoptosis-of-multiple-myeloma-cells-by-the-jak2-stat3-pathway
#6
Sishi Tang, Bingqing Cheng, Nana Zhe, Dan Ma, Jibing Xu, Xinyao Li, Yongling Guo, Weibing Wu, Jishi Wang
Multiple myeloma (MM) is a hematological malignancy that is characterized by the clonal expansion of plasma cells in the bone marrow. Histone deacetylases (HDACs) represent a new type of molecular targeted therapy for different types of cancers and promising targets for myeloma therapy. We showed that HDAC3 mRNA and protein levels of CD138 mononuclear cells from MM patients were higher than those in healthy donors. Therefore, we investigated the effects of a novel class I HDAC inhibitor BG45 on MM cells in vitro...
October 18, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29023248/anticancer-effect-of-acid-ceramidase-inhibitor-ceranib-2-in-human-breast-cancer-cell-lines-mcf-7-mda-mb-231-by-the-activation-of-sapk-jnk-p38-mapk-apoptotic-pathways-inhibition-of-the-akt-pathway-downregulation-of-er%C3%AE
#7
Helen S Vethakanraj, Binny P Sesurajan, Vishnu P Padmanaban, Madhumathi Jayaprakasam, Suganthi Murali, Ashok K Sekar
Acid ceramidase is the key enzyme of the ceramide metabolic pathway, which plays a vital role in regulating ceramide - sphingosine-1-phosphate rheostat. Ceramide acts as a proapoptotic molecule, but its metabolite sphingosine-1-phosphate, in contrast, signals for cell proliferation, cell survival, and angiogenesis. Acid ceramidase is highly upregulated in breast tumors and treatment with an acid ceramidase inhibitor, ceranib-2, significantly induced apoptosis in human breast cancer cell lines. However, the mechanisms underlying the induction of apoptosis remain ambiguous to date...
October 11, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28984684/influence-of-the-alkylating-function-of-aldoifosfamide-on-the-antitumor-activity
#8
Georg Voelcker
The present work investigates the influence of different DNA damages caused by different isophosphoramide mustards on the 3-hydroxypropanal-assisted apoptotic antitumor activity of oxazaphosphorine cytostatics using I-aldophosphamide-perhydrothiazine (IAP) and mesyl-I-aldophosphamide-perhydrothiazine (SUM-IAP) for in-vitro and in-vivo experiments. IAP and SUM-IAP hydrolyze spontaneously to the corresponding I-aldophosphamide derivatives. They differ in the chemical structure of the alkylating moiety, whereas IAP has two chlorethyl groups in the SUM-IAP molecule, one chlorethyl group is substituted by a mesylethyl group...
October 3, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28984683/reversine-induces-autophagic-cell-death-through-the-amp-activated-protein-kinase-pathway-in-urothelial-carcinoma-cells
#9
Chiung-Yao Fang, Jeng-Sheng Chen, Shun-Kai Chang, Cheng-Huang Shen
Urothelial carcinoma is one of the most common malignancies of the urinary tract. Effective treatment of advanced urothelial carcinoma remains a clinical challenge with poor outcomes in these patients. Previous reports have shown that the expression of aurora kinase is associated with clinical stage and prognosis; hence, aurora kinases are potential targets in urothelial carcinoma therapy. Reversine, an aurora kinase inhibitor, was analyzed for its cytotoxicity in this study. Cell proliferation, flow cytometry, western blotting, and immunofluorescent assay were used to determine the effect of reversine on urothelial carcinoma cells...
October 3, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29045271/rhabdomyosarcoma-cells-are-susceptible-to-cell-death-by-ldk378-alone-or-in-combination-with-sorafenib-independently-of-anaplastic-lymphoma-kinase-status
#10
Nadezda Dolgikh, Simone Fulda
Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase that is often overexpressed in rhabdomyosarcoma (RMS). However, its oncogenic and functional role in RMS remains unclear. Therefore, we investigated the antitumor activity of LDK378 (ceritinib), a new second-generation ALK inhibitor approved for patients with ALK-positive non-small-cell lung cancers. Here, we report that LDK378 reduces cell viability and induces cell death in RMS cell lines at low micromolar IC50 concentrations irrespective of ALK expression levels or phosphorylation status...
November 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29023247/mir-449a-a-potential-therapeutic-agent-for-cancer
#11
He Yong-Ming, Ji Ai-Jun, Xu Xiao-Yue, Lu Jian-Wei, Yu Chen, Chen Ye
MicroRNAs (miRNAs) have been reported to be associated with cancer progression and carcinogenesis. They are small, highly conserved, noncoding RNA molecules consisting of 19-25 nucleotides. By binding to complementary binding sites within the 3'-untranslated region of target mRNAs, miRNAs inhibit the translation of mRNAs or promote their degradation. miRNAs play critical roles in cancer initiation and development by functioning either as oncogenes or as tumor suppressors. Similarly, several studies have shown that miRNAs are involved in regulating various biological processes, including apoptosis, proliferation, cellular differentiation, signal transduction, and carcinogenesis...
November 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28938245/gallic-acid-induces-g1-phase-arrest-and-apoptosis-of-triple-negative-breast-cancer-cell-mda-mb-231-via-p38-mitogen-activated-protein-kinase-p21-p27-axis
#12
Hsiang-Lin Lee, Chun-Shiang Lin, Shao-Hsuan Kao, Ming-Chih Chou
Gallic acid (GA) possesses potential antitumoral activity on different types of malignancies. In this study, we aimed to explore the antitumoral effects of GA on triple-negative breast cancer (TNBC) cells, the breast cancer cells showing resistance to hormonal therapy or HER2 receptor targeting therapy. We observed that GA treatment significantly decreased the cell viability of human TNBC cell line MDA-MB-231 and HS578T in a dose-dependent manner. In addition, GA exerted a relative lower cytotoxicity on noncancer breast fibroblast MCF-10F...
November 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28926423/a-noninterventional-multicenter-prospective-phase-iv-study-of-trabectedin-in-patients-with-advanced-soft-tissue-sarcoma
#13
Angela Buonadonna, Charlotte Benson, Jose Casanova, Bernd Kasper, Antonio López Pousa, Filomena Mazzeo, Thomas Brodowicz, Nicolas Penel
This prospective, noninterventional study is the first phase IV trial designed to evaluate trabectedin in patients with advanced soft tissue sarcoma in real-life clinical practice across Europe. To be included in the study, patients must have received more than or equal to one cycle of trabectedin and be currently on treatment. The primary endpoint was progression-free survival as defined by investigators. The secondary endpoints included objective response rate, disease control rate, time to progression and the growth modulation index (GMI), overall survival, and an assessment of the cancer-related symptoms and safety...
November 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28926422/two-faces-of-hippo-activate-or-suppress-the-hippo-pathway-in-cancer
#14
Jingwen Cao, Wenlong Huang
The Hippo pathway has generated considerable interest in recent years because of its involvement in several key hallmarks of cancer progression and metastasis. Research on the Hippo signaling pathway in cancer has been used to determine the activity of yes-associated protein (YAP) in tumorigenesis and disease progression. Previous studies have shown that the Hippo pathway can be used as a target to inhibit YAP activity and is a viable treatment for cancer. However, more studies are required to further advance our understanding of the Hippo signaling pathway in cancer...
November 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28926421/a-novel-hydroxyphenyl-hydrazone-derivate-ycl0426-inhibits-cancer-cell-proliferation-through-sequestering-iron
#15
Feifei Li, Long Long, Junhai Xiao, Chen Wang, Wei Li, Song Li, Changqi Zhao, Lili Wang
Cancer cells have an increased requirement for iron than normal cells, and iron chelators are under active consideration for cancer treatment. The metal-sequestering potential and antiproliferative mechanisms of a novel hydroxyphenyl hydrazone derivate YCL0426 were investigated here. Antiproliferative activity of YCL0426 was detected by MTT assay. The iron-sequestering potential was evaluated by ferrozine-Fe(II) sequestering assay and Fe(II) titration assay. Cell-cycle-arresting profile was checked by flow cytometry and the DNA synthesis status was evaluated by BrdU incorporation assay...
November 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28906258/early-tumor-shrinkage-indicates-a-favorable-response-to-bevacizumab-based-first-line-chemotherapy-for-metastatic-colorectal-cancer
#16
Mamoru Ito, Hitoshi Kusaba, Satomi Mukaide, Junji Kishimoto, Hozumi Shimokawa, Shingo Tamura, Akitaka Makiyama, Gen Hirano, Hisanobu Oda, Tsuyoshi Shirakawa, Masato Komoda, Keita Uchino, Risa Tanaka, Kenji Mitsugi, Taito Esaki, Shuji Arita, Hiroshi Ariyama, Koichi Akashi, Eishi Baba
A close correlation between early tumor shrinkage (ETS) and overall survival (OS) has been shown in antiepidermal growth factor receptor antibody-based chemotherapies for metastatic colorectal cancer (mCRC), but the clinical impact of ETS in bevacizumab-based chemotherapy has not been adequately clarified. Clinical data of mCRC patients who started initial chemotherapy without antiepidermal growth factor receptor antibody from 2005 to 2010 were retrospectively evaluated. The relative change in tumor size after 8 weeks of chemotherapy expected from the first image assessment [estimated ETS (EETS)] and the relative change in the tumor size at the nadir compared with the baseline [depth of response (DPR)] were examined...
November 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28901962/ability-of-polymer-bound-p-glycoprotein-inhibitor-ritonavir-to-overcome-multidrug-resistance-in-various-resistant-neuroblastoma-cell-lines
#17
Eva Koziolová, Petr Chytil, Tomáš Etrych, Olga Janoušková
Polymer prodrugs can considerably improve the treatment of tumors with multidrug resistance, often caused by overexpression of P-glycoprotein (P-gp). Here, we present the effect of the N-(2-hydroxypropyl) methacrylamide-based polymer conjugate with P-gp inhibitor ritonavir (RIT) on the increase of free doxorubicin (DOX) and polymer-bound DOX cytotoxicity in the human neuroblastoma 4 cell line and its resistant clones to different cytostatics. The increase in cytotoxicity after polymer-RIT conjugate pretreatment was higher for the lines overexpressing P-gp and less pronounced for those with decreased P-gp levels...
November 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28885268/n1-guanyl-1-7-diaminoheptane-enhances-the-chemosensitivity-of-acute-lymphoblastic-leukemia-cells-to-vincristine-through-inhibition-of-eif5a-2-activation
#18
Yanhui Liu, Fei Xue, Yin Zhang, Pingchong Lei, Zhen Wang, Zunmin Zhu, Kai Sun
N1-guanyl-1,7-diaminoheptane (GC7), a deoxyhypusine synthase inhibitor, has been shown to exert antiproliferation effects in many solid tumors by regulating eukaryotic translation initiation factor 5a2 (eif5a-2). However, little is known about the role of GC7 and eif5a-2 in drug resistance in acute lymphoblastic leukemia (ALL). In the present study, we investigated the effect of GC7 on drug-resistant ALL and its potential mechanism. We found that using the CCK-8 assay that combined treatment with GC7 and vincristine (VCR) significantly inhibited the cell viability of two ALL cell lines...
November 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28885267/bcl-2-and-bcl-xl-mediate-resistance-to-receptor-tyrosine-kinase-targeted-therapy-in-lung-and-gastric-cancer
#19
Junfei Jin, Ying Xiong, Bo Cen
Promising clinical efficacy has been observed with receptor tyrosine kinase inhibitors (TKIs) particularly in lung and gastric cancers with mutations or amplifications in the targeted receptor tyrosine kinases (RTKs). However, the efficacy and the duration of the response to these inhibitors are limited by the emergence of drug resistance. Here, we report treatment of RTK-dependent lung and gastric cancer cell lines with TKIs increased protein levels of Bcl-2 and Bcl-xL. The combination of the Bcl-2 and Bcl-xL inhibitor ABT-263 and TKIs was superior to TKIs alone in reducing cell viability and capacity of resistant colony formation...
November 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28857767/extended-topoisomerase-1-inhibition-through-liposomal-irinotecan-results-in-improved-efficacy-over-topotecan-and-irinotecan-in-models-of-small-cell-lung-cancer
#20
Shannon C Leonard, Helen Lee, Daniel F Gaddy, Stephan G Klinz, Nancy Paz, Ashish V Kalra, Daryl C Drummond, Daniel C Chan, Paul A Bunn, Jonathan B Fitzgerald, Bart S Hendriks
Liposomal irinotecan (irinotecan liposome injection, nal-IRI), a liposomal formulation of irinotecan, is designed for extended circulation relative to irinotecan and for exploiting discontinuous tumor vasculature for enhanced drug delivery to tumors. Following tumor deposition, nal-IRI is taken up by phagocytic cells followed by irinotecan release and conversion to its active metabolite, SN-38. Sustained inhibition of topoisomerase 1 by extended SN-38 exposure as a result of delivery by nal-IRI is hypothesized to enable superior antitumor activity compared with traditional topoisomerase 1 inhibitors such as conventional irinotecan and topotecan...
November 2017: Anti-cancer Drugs
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