Abstract：
:Electron-affinic compounds with strong DNA intercalating properties have demonstrated less than the expected radiosensitization due to restriction of their mobility along the DNA backbone and their lower extravascular diffusion in tumors. A 2-nitroimidazole linked 1,2,3,4-tetrahydroacridine derivative (THNLA-1) has been synthesized as a hypoxia-selective cytotoxin and radiosensitizer with presumably lower DNA-binding affinity due to the perturbation of the planarity in the acridine ring. THNLA-1 is a good hypoxia-selective cytotoxin with a differential toxicity of approximately equal to 11 in V79 cells, but it is approximately equal to 2 times less potent on a concentration basis than NLA-1 (the 2-nitroimidazole linked acridine analog). However, THNLA-1 is a very efficient radiosensitizer, showing a sensitization enhancement ratio (SER) of 3.04 +/- 0.05 at 100 microM at 25 degrees C, and the concentration giving an SER of 1.6(C1.6) is 19.0 +/- 0.5 microM. The therapeutic index, defined as the ratio of the clonogenic IC50 under aerobic conditions for 1-h exposure (IC50A,1h) to the C1.6 value, is 20 for THNLA-1 vs. 11 for NLA-1. THNLA-1's partition coefficient in octanol/water is 0.14 +/- 0.02. Topoisomerase I and II interaction studies with THNLA-1 showed that topoisomerase I-mediated relaxation of supercoiled DNA was inhibited at relatively high THNLA-1 concentrations (> or = 1000 microM), while topoisomerase II-mediated decatenation of kinetoplast DNA remained unaffected even in concentrations toxic in vitro under aerobic conditions. Uptake studies under aerobic conditions showed high intracellular drug concentrations, compatible with the required ones for topoisomerase I inhibition.
journal_name
Oncol Resjournal_title
Oncology researchauthors
Papadopoulou MV,Rosenzweig HS,Doddi M,Bloomer WDsubject
Has Abstractpub_date
1994-01-01 00:00:00pages
439-48issue
9eissn
0965-0407issn
1555-3906journal_volume
6pub_type
杂志文章abstract：:Sixteen desmuramyl analogs of muramyl dipeptide (MDP) were tested for their abilities to stimulate cytotoxic factor secretion by mouse peritoneal macrophages. Among them, the pseudohexapeptide Boc-Gly psi [CH2O]-D-Ala-Ala-D-Glu[Lys(H-Gly)NHEt]-NH2 appeared to be four times more effective than MDP. From this study, the...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：1992-01-01 00:00:00
abstract：:Accumulating evidence indicates that microRNA-205 (miR-205) is involved in tumor initiation, development, and metastasis in various cancers. However, its functions in neuroblastoma (NB) remain largely unclear. Here we found that miR-205 was significantly downregulated in human NB tissue samples and cell lines. miR-205...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504017X14974834436195
更新日期：2018-04-10 00:00:00
abstract：:Claudin18 (CLDN18) is necessary for intercellular junctions and is reported to be involved in cell migration and metastasis, making it like an oncogene in various cancer types. However, the biological function and regulatory mechanisms of CLDN18 in lung adenocarcinoma are not yet clear. In this study, we found downreg...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504017X15112639918174
更新日期：2018-05-07 00:00:00
abstract：:Oncogene Bmi-1 (B-cell-specific Moloney murine leukemia virus integration site 1) has attracted much attention for its involvement in the initiation of a variety of tumors. Our previous study showed that Bmi-1 was highly expressed in gastric cancer and correlated with patient prognosis. However, whether aberrant Bmi-1...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504013X13786659070316
更新日期：2013-01-01 00:00:00
abstract：:The regular RIN1 gene is a molecule located on chromosome 1lq13.2, and contains a coding region of 2352 bp with a 3' domain that binds to H-Ras protein, suggesting that it is an important molecule in the intracellular signaling pathway. In this study, we confirmed the existence of a novel form of the RIN1 gene with a ...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504009789745566
更新日期：2009-01-01 00:00:00
abstract：:Medroxyprogesterone (MPA) is used for the conservative treatment of endometrial cancer. Unfortunately, progesterone resistance seriously affects its therapeutic effect. The purpose of the current study was to investigate the influence of deletion of AT-rich interactive domain 1A (ARID1A) in progesterone resistance in ...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504019X15561873320465
更新日期：2019-09-23 00:00:00
abstract：:Genistein is an inhibitor of the enzymes protein tyrosine kinase and topoisomerase-II. It induces G2-phase arrest in human Jurkat and murine P388 leukemia cells at concentrations at which it is also cytotoxic. The effects of genistein have been investigated on Jurkat and P388 leukemia sublines that manifest multidrug ...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：1994-01-01 00:00:00
abstract：:Epidermal growth factor receptor (EGFR) is commonly overexpressed in non-small cell lung cancer (NSCLC) and its tyrosine kinase phosphorylation is thought to be an ideal target in the treatment of patients with NSCLC. In the present study, we examined surgically obtained specimens from a series of 36 NSCLC patients fo...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504003108748348
更新日期：2003-01-01 00:00:00
abstract：:The pre-mRNA splicing regulator serine-arginine protein kinase 1 (SRPK1), a member of the SR kinase family, plays an essential role in cancer development and various pathophysiological processes. However, its expression pattern and functions in renal cell carcinoma (RCC) remain unknown. Therefore, the aim of this stud...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504016X14743324568129
更新日期：2017-03-13 00:00:00
abstract：:HL-60 cells isolated for resistance to vincristine are multidrug resistant and defective in the cellular accumulation of drug. Further studies demonstrate that these cells are also highly defective in 12-O-tetradecanoylphorbol-13-acetate (TPA) induced differentiation to macrophages. Analysis of this system demonstrate...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：1992-01-01 00:00:00
abstract：:Colorectal cancer is an aggressive malignancy for which there are limited treatment options. Oncolytic vaccinia virus isbeing developed as a novel strategy for cancer therapy. Arming vaccinia virus with immunostimulatory cytokines can enhance the tumor cell-specific replication and antitumor efficacy. Interleukin-24 (...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504020X15942028641011
更新日期：2020-07-08 00:00:00
abstract：:Increasing evidence shows that beyond its role in coagulation, thrombosis interferes with carcinogenesis. Endothelial cell protein C receptor (EPCR) is a cellular receptor for protein C and activated protein C (APC). Such EPCR-induced signal transduction promotes cancer cell migration, invasion, and angiogenesis and i...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504013x13589503482932
更新日期：2012-01-01 00:00:00
abstract：:EO9 [3-hydroxy-5-aziridinyl-1-methyl-2-(1H-indole-4,7-indione)-prop-be ta- en-alpha-ol] is a new bioreductive alkylating indoloquinone with a distinct antitumor activity against solid tumors, excellent activity under hypoxic conditions, and lack of bone marrow toxicity in preclinical models. Clinical phase I studies w...
journal_title：Oncology research
pub_type： 临床试验,杂志文章
doi：
更新日期：1994-01-01 00:00:00
abstract：:Spinal osteosarcoma (OS) is a malignant tumor that has a poor outcome. MicroRNA-520b (miR-520b) acts as a cancer suppressor in various types of cancer. Because of the limited amount of literature on OS, we aimed to identify the role of miR-520b in OS. The miR-520b level in clinical spinal OS tissues and adjacent nontu...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504017X14873430389189
更新日期：2017-09-21 00:00:00
abstract：:Numerous studies have observed that workers in ferriferous industries have an elevated risk of respiratory tract neoplasia. Research at the cellular and animal model levels indicates that iron compounds, per se, are carcinogenic. However, some investigators have suggested that inhaled iron compounds are merely carrier...
journal_title：Oncology research
pub_type： 杂志文章,评审
doi：
更新日期：1999-01-01 00:00:00
abstract：:Mutational inactivation of the cyclin-dependent kinase inhibitors (CDKIs) (p16INK4A/MTS1) tumor suppressor gene has been found in a variety of human tumor types. To investigate the involvement of CDKI abnormality in mesenchymal chondrosarcoma, alterations of CDKIs were examined in human mesenchymal chondrosarcoma tiss...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/000000001108747381
更新日期：2000-01-01 00:00:00
abstract：:Ovarian cancer is the most lethal disease among gynecological malignancies. More effective therapy is required to counter high recurrence rates and chemotherapy resistance. We investigated the efficacy and molecular mechanisms of three combined treatments (TCTs)-a novel histone deacetylase (HDAC) inhibitor OBP-801/YM7...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504017X14850164661097
更新日期：2017-09-21 00:00:00
abstract：:Human telomerase is a ribonucleoprotein that maintains telomeres by adding TTAGGG tandem repeat sequences using RNA template of the enzyme. Telomerase activity is highly expressed in immortalized cells but not in most somatic cells, except for some renewal tissues, such as hematopoietic stem cells. Therefore, telomera...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：1998-01-01 00:00:00
abstract：:DT-diaphorase [also called NAD(P)H:menadione oxidoreductase; NAD(P)H:(quinone acceptor) oxidoreductase; quinone reductase, azo-dye reductase] (EC.1.6.99.2) has been shown to have a role in activation of quinone-containing cancer chemotherapeutic prodrugs to their active form, as well as inactivation of a variety of xe...
journal_title：Oncology research
pub_type： 杂志文章,评审
doi：
更新日期：1997-01-01 00:00:00
abstract：:To elucidate the proteins related to the development and progress of esophageal squamous cell carcinoma (ESCC), we performed gene expression profile analysis of 14 ESCC tissues. We identified 182 genes that were commonly upregulated (p < 10(-5)) and 54 genes that were downregulated in ESCC tissues (p < 10(-6)). In ord...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504009790217407
更新日期：2009-01-01 00:00:00
abstract：:It has been reported that upregulated SIRT1 (NAD(+)-dependent class III histone deacetylase) deacetylates the p53 protein, represses its function, and allows for tumor cell growth in various cancers. Here we investigated antitumor effects of tenovin-6, a small-molecule inhibitor of SIRT1 and SIRT2, in various colon ca...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504013X13854886566598
更新日期：2013-01-01 00:00:00
abstract：:MTA1 was reported as a metastasis-associated gene. Tumors with higher MTA1 mRNA level were shown to have higher rates of invasion and lymph node metastasis and tended to have higher rates of vascular involvement. The majority of invasive breast carcinomas were demonstrated to overexpress MTA1 compared to surrounding n...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504007783338322
更新日期：2007-01-01 00:00:00
abstract：:Baicalein, a flavonoid derived from the root of Scutellaria baicalensis, has been reported to possess multiple pharmacological activities, such as anticancer and anti-inflammatory properties. This study investigated the effect of baicalein in cervical cancer cells. Cell growth curve and MTT assay were performed and re...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504017X15031557924141
更新日期：2018-05-07 00:00:00
abstract：:Thymosin-beta-4 (TB4) as an actin-sequestering peptide has been detected outside of cells in blood plasma or in wound fluid. TB4 induces tumor metastasis and paclitaxel resistance, which is the most significant obstacle to successful therapy in tumors. Here we investigated the inhibitory effect of TB4 peptides on tumo...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504007783438349
更新日期：2007-01-01 00:00:00
abstract：:Signal peptide CUB EGF-like domain-containing protein 2 (SCUBE2), a member of the SCUBE family of proteins, was recently found to play an important role in cancer development. However, little is known regarding its biological function in glioma. In the present study, we investigated the effect of SCUBE2 on glioma and ...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504016X14747335734344
更新日期：2017-03-13 00:00:00
abstract：:The human nucleolar protein p120 is highly expressed in human cancers. Its high expression in breast cancer correlates with a poor prognosis, and its overexpression in 3T3 mouse fibroblasts causes malignant transformation. This study reports that a combination of monoclonal anti-p 120 antibody (MAbp120), liposomes (Li...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：1996-01-01 00:00:00
abstract：:There is growing evidence on the clinical significance of Tumor Microenvironment (TME) cells in predicting prognosis and therapeutic effects. However, cell interactionsin tumor microenvironments have not been thoroughly studied or systematicallyanalyzed so far. In this study, 22 immune cell components in the lung aden...
journal_title：Oncology research
pub_type： 杂志文章
doi：10.3727/096504020X15907428281601
更新日期：2020-05-29 00:00:00
abstract：:Constitutive canonical Wnt signaling, resulting from mutations in the adenomatous polyposis coli (APC), beta-catenin, or axin genes, has been implicated in the initiation of most human colorectal cancers (CRCs). Some of the proposed approaches for CRC prevention and treatment involve the downregulation of canonical Wn...
journal_title：Oncology research
pub_type： 杂志文章,评审
doi：10.3727/096504008784046108
更新日期：2008-01-01 00:00:00
abstract：:A series of bis-aziridinylnaphthoquinone derivatives has been prepared. The cytotoxic activities and DNA alkylation abilities of these synthetic bis-aziridinylnaphthoquinone derivatives were investigated. They displayed significant cytotoxicity against human carcinomna cell lines and weak cytotoxic activities against ...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：2003-01-01 00:00:00
abstract：:Recently, there has been significant effort in developing techniques designed to detect disseminated tumor cells in the peripheral blood (PB). These techniques include immunocytochemical staining of cytocentrifuge slides, flow cytometry, and RT-PCR. Several authors reported various results concerning the sensitivity o...
journal_title：Oncology research
pub_type： 杂志文章
doi：
更新日期：1999-01-01 00:00:00
