Abstract:
:12-O-retinoylphorbol-13-acetate (RPA), an incomplete tumor promoter of the phorbol ester type and protein kinase C (PKC) activator, consists of two characteristic structural elements: the phorbol body and the retinoyl ester chain. Therefore, possible binding of the incomplete tumor promoter RPA to the human transport protein retinol-binding-protein (RBP) has been examined by molecular modeling methods and experimental binding studies. The calculated prediction of binding properties was primarily based on a comparative geometrical approach. It was shown that the beta-ionone-ring of RPA was not altered within the binding pocket of RBP (molecular modeling) compared to retinoic acid (X-ray crystallographic data). The torsion angle C5'-C6'-C7'-C8', determining the conformation of the RBP-beta-ionone-ring relative to the isoprene tail, is rotated by 42 degrees for RPA compared to retinol and to retinoic acid, respectively. Combining all the results from force field calculations, MD simulations and geometrical comparisons, the conclusion could be drawn that RPA should be able to bind to RBP. This interaction should be less strong than that with its natural ligand retinol or with retinoic acid. This prediction was proven experimentally. RPA was able to compete with retinoic acid for binding at RBP in human plasma. The binding properties were investigated using 3H-labeled retinoic acid in homologous and heterologous competition studies in a one-dimensional native polyacrylamide gel electrophoresis system. An approximately 2000-fold weaker binding of RPA to RBP as compared to retinoic acid was determined experimentally, confirming the prediction of the molecular modeling approach. The characteristic behaviour of RPA as an incomplete promoter, due to possible binding to PKC and RBP, is discussed.
journal_name
Anticancer Resjournal_title
Anticancer researchauthors
Schlatterer K,Gminski R,Schlatterer J,Hecker E,Chandra P,Schlatterer B,Krauter G,Chandra Asubject
Has Abstractpub_date
2005-09-01 00:00:00pages
3355-65issue
5eissn
0250-7005issn
1791-7530journal_volume
25pub_type
杂志文章abstract:BACKGROUND/AIM:Shortcomings of current methods of prostate cancer detection call for improved biomarkers. The transmembrane protease, serine 2:ets-related gene (TMPRSS2:ERG) gene fusion leads to the overexpression of ERG, an E-twenty six (ETS) family transcription factor, and is the most prevalent genetic lesion in pro...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2012-09-01 00:00:00
abstract:BACKGROUND:The purpose of this study was to determine the efficacy of a combination of gemcitabine and sirolimus in a mouse model of invasive bladder cancer. MATERIALS AND METHODS:Gemcitabine (50 mg/kg) and sirolimus (1.5 mg/kg) were administered to animals previously exposed to N-butyl-N-4(hydroxybutyl)nitrosamine in...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2011-05-01 00:00:00
abstract::Recent results concerning new antitumor metallocene derivatives have shown that not only numerous titanocene dihalides and bis(pseudohalides) exhibit antiproliferative activity, but that also some titanocene complexes (C5H5)2TiX2 containing carboxylates or hydrochlorinated aminothiophenolates as ligands X, are charact...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1986-03-01 00:00:00
abstract:BACKGROUND:Protein kinase C (PKC) activity is increased and gap junctional intercellular communication (GJIC) is decreased frequently in Ras-transformed cells. We investigated the roles of Ras and PKC in the deficient gap junctional intercellular communication (GJIC) of K-ras-transformed E9 mouse lung carcinoma cells. ...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1998-11-01 00:00:00
abstract::The relationship between serum and cytosolic levels of carcinoembryonic (CEA), squamous-cell carcinoma (SCC) and CA125 antigens was determined in 122 patients with non-small cell lung cancer. A pronounced serum-cytosol gradient and a high degree of dispersion in the distribution of serum and cytosol marker concentrati...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1995-11-01 00:00:00
abstract:BACKGROUND:Particularly interesting new cysteine-histidine-rich protein (PINCH) was found to be up-regulated in the stroma of colorectal carcinomas (CRCs) in our previous studies and was involved in angiogenesis through activation of fibroblasts in extracellular matrix (ECM) in response to tumors. Here, we examined PIN...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2011-12-01 00:00:00
abstract:BACKGROUND:Human herpesviruses types 4 and 6 (EBV, HHV-6) are frequently found in Hodgkin 's disease (HD) and--to a certain extent--in Kikuchi-Fujimoto's disease (KFD). Both viruses are apparently related to proliferative and/or apoptotic processes as represented by HD or KFD respectively. OBJECTIVE:To correlate frequ...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2001-05-01 00:00:00
abstract:UNLABELLED:We investigated the predictive value of the protein S100 as a tumor-marker in the post-surgical follow-up staging of patients with High Risk melanomas (Clark Levels IV/V, Thickness > 0.75 mm). METHODS:In 51 follow-up studies, performed in 50 patients, serum concentrations of the protein S100 were measured a...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1999-07-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1996-11-01 00:00:00
abstract:BACKGROUND:5-Aminolevulinic acid (5-ALA) has already been applied clinically as a photosensitizer. In this study, sonodynamically induced selective antitumour effect of 5-ALA for deep-seated lesions was evaluated. MATERIALS AND METHODS:First, normal rat brains were sonicated via a transducer placed on the dural surfac...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2011-07-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.14266
更新日期:2020-05-01 00:00:00
abstract:BACKGROUND:Interleukin-1alpha (IL-1) is known to radioprotect the gastrointestinal tract, but the mechanism by which this protection occurs remains unclear. These studies were undertaken to investigate whether the radioprotective potential of IL-1 may be linked to an ability to reduce apoptosis within the gastrointesti...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2008-11-01 00:00:00
abstract::Non-small-cell lung cancer (NSCLC) ranks as a leading cause of cancer-related death globally. Brain metastases are a frequent complication of NSCLC, with 25-40% of patients developing brain metastases during the course of the disease, often within the first 2 years after diagnosis of the primary tumor. Improvements in...
journal_title:Anticancer research
pub_type: 杂志文章,评审
doi:
更新日期:2015-11-01 00:00:00
abstract::Cathepsin B (CB) is involved in degradation of extracellular matrix proteins during tumor progression in human solid organ tumors (such as colorectal, bladder, and breast cancers), including human prostate cancer. Its activities are regulated by endogenous inhibitors (such as stefins or cystatins). Increased expressio...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1999-07-01 00:00:00
abstract::Exposure of human promyelocytic leukemic HL-60 cells to millimolar concentration of sodium ascorbate induced apoptotic cell death. The extent of apoptosis induction was a positive function of temperature at the time of exposure. The incorporation of [1-14C] ascorbic acid into the cytosolic fraction of HL-60 cells was ...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1998-07-01 00:00:00
abstract:AIM:Metastasis of unknown primary (MUP) is commonly treated with radiation therapy (RT) to the entire mucosal surfaces and bilateral neck nodes (LN). We report outcomes of oropharynx-targeted RT, retropharyngeal nodes (RPN) and bilateral LN in this context. PATIENTS AND METHODS:Single-Institution retrospective study o...
journal_title:Anticancer research
pub_type: 临床试验,杂志文章
doi:
更新日期:2014-01-01 00:00:00
abstract:BACKGROUND:Tetrandrine, a bisbenzylisoquinoline alkaloid, has cancer cell cytotoxicity. The effects of combined tetrandrine and radiation, alone or combined, on human SH-SY5Y neuroblastoma cells were examined. MATERIALS AND METHODS:A combination treatment, using either concomitant irradiation at the beginning or end o...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2009-08-01 00:00:00
abstract::Between January 1996 and June 2000, 192 men with prostate cancer underwent radical retropubic prostatectomy (RP) and bilateral pelvic node dissection in 26 centers participating in the Italian randomized prospective TAP study. The reviewing pathologist evaluated 145 RP specimens. Seventy-five cases had not been treate...
journal_title:Anticancer research
pub_type: 临床试验,杂志文章,多中心研究,随机对照试验
doi:
更新日期:2001-09-01 00:00:00
abstract::Ovarian cancer is the most lethal malignancy among gynaecological cancers. Although many anticancer agents have been developed for the treatment of ovarian cancer, it continues to have an extremely poor prognosis. Heparin-binding epidermal growth factor-like grown factor (HB-EGF) has been reported to be a rational the...
journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.11779
更新日期:2017-07-01 00:00:00
abstract::Chloroethyl-nitrosourea is a potent chemotherapeutic agent for brain tumors. However, acquired resistance to this drug has become a serious problem for the treatment of patients. Previously, we established an animal model resistant to nitrosourea (Anticancer Res 19: 5313-5318, 1999). In this study, we evaluate the eff...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2002-07-01 00:00:00
abstract:BACKGROUND:The prognostic impact of neutrophil to lymphocyte ratio (NLR) in non-small cell lung cancer (NSCLC) was examined using patients with a follow-up period more than 5 years. PATIENTS AND METHODS:Two hundred and eighty four consecutive resected NSCLC patients were reviewed retrospectively. In this study, patien...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2011-09-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1995-11-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2014-11-01 00:00:00
abstract:BACKGROUND/AIM:Interleukin-32 (IL32) has been newly-identified as a proinflammatory cytokine. In the present study, we aimed to clarify the clinical role of IL32-positive cells in esophageal squamous cell cancer (ESCC) and regulatory T-cell (Treg) infiltration in the stroma. A total of 179 patients with ESCC who underw...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2015-05-01 00:00:00
abstract:BACKGROUND/AIM:This cross-sectional study estimated direct cancer-related health care, productivity and informal care costs for a six-month period for different states of breast cancer (BC). PATIENTS AND METHODS:A total of 827 BC patients answered a questionnaire enquiring about informal care, work capacity, and demog...
journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.13119
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND:The epithelial-mesenchymal transition is a critical early event in the invasion and metastasis of many types of cancer, including colorectal cancer (CRC). Chronic inflammation is an inducer of several cancer types and inflammatory cytokines have been implicated in tumor invasion. MATERIALS AND METHODS:Human...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2009-11-01 00:00:00
abstract::Tissue-specific cancers originate in organ- or tissue-specific cells with the potential to proliferate. Recent reports have shown that every adult tissue may have its own stem cells. Cancer cells and organ- and tissue-specific stem cells and other progenitor cells are strikingly similar: both types self-renew, prolife...
journal_title:Anticancer research
pub_type: 杂志文章,评审
doi:
更新日期:2002-05-01 00:00:00
abstract::Three sublines have been derived from the parental line Mv1Lu by transfection with normal and mutated Ha-ras, and myc oncogenes, and subsequent cloning. All the oncogenes have increased the growth rate of the cell in vitro, increased their plating efficiency in monolayer and suspension, and reduced their serum depende...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1991-05-01 00:00:00
abstract:BACKGROUND/AIM:Cancer incidence and mortalities are growing worldwide, therefore research and development of more effective and less invasive treatments, such as photodynamic therapy, are needed. Herein, we investigated the methylene blue (MB) photoactivation effects in lung epithelial cells (BEAS-2B) and lung adenocar...
journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.13522
更新日期:2019-07-01 00:00:00
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journal_title:Anticancer research
pub_type: 杂志文章,评审
doi:
更新日期:2015-02-01 00:00:00