Abstract:
:P-glycoprotein (P-gp) is an active, ATP-dependent plasma membrane transporter which is responsible for the expulsion of various cytotoxic drugs with different chemical structures out of resistant (MDR) cells. It is also capable of transporting a number of other amphiphilic molecules, the so-called MDR-reversing agents, which belong to a very broad variety of chemical families. Moreover, P-gp can also play a role in steroid secretion and cellular detoxification by transporting various other substrates. In this review, we address the problem of the multiple recognition by P-gp of such a large number of amphiphilic molecules. This is both (i) from a basic viewpoint in order to discuss the underlying molecular mechanisms explaining how the general rule of substrate-enzyme specificity can be violated, and (ii) from a more applied pharmacological viewpoint to show in detail how the interaction of various drugs with P-gp leads to important consequences in terms of the relative effects of these drugs in the anticancer chemotherapy context, as well as for their pharmacokinetic distributions in the whole organism, rationalizing possible adverse drug reactions. In particular, we will present evidence that, independently of the technique used, the mutual interactions between P-gp transport substrates cannot always be reduced to simple competitive effects.
journal_name
Anticancer Resjournal_title
Anticancer researchauthors
Orlowski S,Garrigos Msubject
Has Abstractpub_date
1999-07-01 00:00:00pages
3109-23issue
4Beissn
0250-7005issn
1791-7530journal_volume
19pub_type
杂志文章,评审abstract:BACKGROUND:The present study investigated the mechanism underlying the apoptosis of MKN28 human gastric cancer cells induced by the phosphatidylinositol (PI) derivative 1,2-O-bis-[8-{2-(2-pentyl-cyclopropylmethyl)-cyclopropyl}-octanoyl]-sn-glycero-3-phosphatidyl-D-1-inositol (diDCP-LA-D-PI) and its enantiomer diDCP-LA-...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2015-12-01 00:00:00
abstract:BACKGROUND:Vascular endothelial growth factor (VEGF) is thought to be the most powerful angiogenic factor in many malignancies while and several reports have determined serum VEGF to be a prognostic indicator for various malignancies. However, serum VEGF may not be suitable for the measurement of circulating VEGF level...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2002-07-01 00:00:00
abstract::In order to define genes which mediate liver tropism of colon cancer metastasis we have compared the transcriptional profile of 5600 full-length genes using the Affymetrix HuGene FL array technology of the non-metastatic colon cancer cell lines KM12C and the two metastatic cell lines, KM12SM and KM12L4A, which are der...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2001-07-01 00:00:00
abstract:BACKGROUND/AIM:The transcription factor Y-box-binding protein 1 (YB1) is overexpressed in many types of human cancers. YB1 regulates the G1 phase of the cell cycle by controlling transcription of G1 regulators. Here, we report that YB1 is also involved in regulating G2/M phase. MATERIALS AND METHODS:YB1-depleted TKO c...
journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.11490
更新日期:2017-04-01 00:00:00
abstract:BACKGROUND:Transformed cells have abnormalities in the survival pathways contributing to drug resistance. These abnormalities include p53 mutations and increased focal adhesion kinase (FAK) expression. Because FAK regulates cell survival via p53-dependent and -independent pathways, it was hypothesized that combined the...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2006-07-01 00:00:00
abstract:BACKGROUND:Melanoma is characterized by high resistance to chemotherapy. The aim of this study was to investigate combined effects of doxorubicin and parthenolide on melanoma cells. MATERIALS AND METHODS:Thiazolyl blue tetrazolium bromide (MTT) assay and flow cytometry were used to evaluate viability. The p53 levels a...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2013-08-01 00:00:00
abstract::Calcitriol (1,25-dihydroxyvitamin D3), the active form of vitamin D, promotes growth inhibition and differentiation in prostate cancer (PCa) cells. To unravel the molecular pathways of calcitriol actions, cDNA microarray analysis was used to identify novel calcitriol target genes including two that play key roles in t...
journal_title:Anticancer research
pub_type: 杂志文章,评审
doi:
更新日期:2006-07-01 00:00:00
abstract::Matrix metalloproteinase-7 (MMP-7), MMP-9, MMP-13, and tissue inhibitor of matrix metalloproteinase-1 (TIMP-1) are considered to have important roles in the invasiveness and outcomes of colorectal cancer (CRC). This study examined the clinicopathological significance of the relative expression of these genes in patien...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2010-07-01 00:00:00
abstract:BACKGROUND:Despite many years of clinical research and development, nausea and vomiting remain challenging toxicities related to chemotherapy. The aim of our study was to clarify the significance of non-pharmacological, patient-related risk factors for chemotherapy-induced nausea and vomiting. Furthermore, we aimed to ...
journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.12798
更新日期:2018-08-01 00:00:00
abstract:BACKGROUND:Laparoscopic pelvic lymph node staging is widely used in patients with cervical cancer prior to the initiation of primary chemoradiation therapy. Data on the morbidity of this procedure are sparse. PATIENTS AND METHODS:Between 1995 and 2007, 71 patients with locally advanced cervical cancer (FIGO stage IB2-...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2008-05-01 00:00:00
abstract:BACKGROUND:This study sought to better define the immunological impact of combining neoadjuvant total androgen suppression (TAS) with radiotherapy (xRT) in treating prostate cancer. MATERIALS AND METHODS:Subjects selected (n = 37) were stage I-II prostate cancer patients meeting the eligibility requirements for RTOG p...
journal_title:Anticancer research
pub_type: 临床试验,杂志文章
doi:
更新日期:2005-07-01 00:00:00
abstract:BACKGROUND:Increasing evidence suggests that adjuvant systemic chemotherapy is necessary for the survival of breast cancer patients. Antitumor agents are more effective when used in combination with drugs exhibiting different mechanisms of action than when used alone. Previous studies from this laboratory have shown th...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2006-05-01 00:00:00
abstract::To elucidate the rates of appearance of hepatocellular carcinoma (HCC) and the prognosis of alcoholic liver cirrhosis upon infection with hepatitis virus, we retrospectively studied 190 consecutive patients. The patients were divided into three groups based on whether they were exposed either to hepatitis B virus (HBV...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2001-07-01 00:00:00
abstract::The recombinant plasmid pBHIV-1 carrying the long terminal repeat (LTR) of the human immunodeficiency virus 1 (HIV-1), linked to the reported chloramphenicol acetyl transferase (CAT) gene, was introduced into human and rat fibroblasts. Stable transfectants were obtained which were resistant to genetecin and expressed ...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1992-11-01 00:00:00
abstract::K-ras-NIH3T3 cells were more invasive than NIH3T3 cells in a chemotactic invasion assay. Conophylline, a new vinca alkaloid isolated as a ras function inhibitor, inhibited the invasion of K-ras-NIH3T3 cells, while it showed no effect on NIH3T3 cells. Conophylline did not increase expression of fibronectin but induced ...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1996-01-01 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::2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) is a widespread environmental contaminant that induces various types of immunotoxicity. One effect of exposure to this contaminant is alteration in cell adhesiveness. Leukocyte function-associated antigen-1 (LFA-1) plays an important role not only in T-cell recruitment into s...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2006-11-01 00:00:00
abstract:BACKGROUND:Studies have recommended a 21-gene recurrence score (RS) to optimize adjuvant treatment for patients with early-stage breast cancer (EBC) with hormone receptor-positive (HR+) and human epidermal growth factor receptor-2 negative (HER2-) tumors. This study aimed to prospectively evaluate the impact of this RS...
journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.11851
更新日期:2017-08-01 00:00:00
abstract:BACKGROUND/AIM:The aim of the present study was to clarify if the degree of hepatic infiltration and lymph node swelling of gallbladder carcinoma (GBC) should be held as deciding factors for T2-4 GBC patients to undergo surgery. PATIENTS AND METHODS:Fifty consecutive patients with T2-4 GBC who underwent surgery were r...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2016-06-01 00:00:00
abstract:BACKGROUND:Motility of cancer cells is a principal cellular parameter, essentially required in the invasion and formation of distant metastasis in human cancer. Measures to stimulate or inhibit motility of cancer cells may play an important part in the understanding of metastasis biology. The aim of this study was to d...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1998-07-01 00:00:00
abstract::Alterations in the p53 gene are frequently observed in a wide variety of human cancers. To elucidate the role of p53 in tumorigenesis of the dog, we analyzed nine mammary tumor cell lines, and the primary or metastatic tumors used for their establishment, for the presence of genomic p53 abnormalities. Possible genomic...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1996-11-01 00:00:00
abstract::Macrophages are thought to be the cells that initially respond to environmental information and transmit this information to other immune cells. We hypothesize that there is a "network system" consisting of various tissue macrophages; the macrophages respond to stimulation and transmit secondary information to neighbo...
journal_title:Anticancer research
pub_type: 杂志文章,评审
doi:
更新日期:2006-11-01 00:00:00
abstract:UNLABELLED:The aim of this study wsa to evaluate the additive effect of valproic acid (VPA) to γδ T-cell cytotoxicity against bladder cancer cells. MATERIALS AND METHODS:Human bladder cancer cell lines TCCSUP and 253J were treated with VPA and mRNA expression of natural killer group 2D (NKG2D) ligands was determined. ...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2010-11-01 00:00:00
abstract::The p53 gene product suppresses both tumor cell growth and the cellular transformation process promoted by oncogenes. Although several genes are known to be positively regulated by p53, it is unclear how many gene expression events are involved in p53-mediated growth arrest and apoptosis. Two-dimensional gel electroph...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1994-11-01 00:00:00
abstract::Despite progress in chemotherapeutic agents, non-small cell lung cancers (NSCLC) still have a poor survival rate. Thus, development of new therapeutic strategies, specifically against cancer cells is still required. For this purpose, we treated the non-small cell lung cancer cell line NSCLC-N6 with the natural product...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2014-09-01 00:00:00
abstract:BACKGROUND:MicroRNAs are able to control vital tumor biological processes, such as proliferation, tissue transformation and cell migration, as well as apoptosis. One of the micro RNAs, namely miR-1, has been classified as a tumor suppressor, however, preliminary data did not confirm this finding in ovarian cancer (OC) ...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2016-07-01 00:00:00
abstract::In 1992 The International Registry of Inferior Vena Cava (IVC) Leiomyosarcomas was established to study the pathogenesis and natural history of the tumor and to support the most rational treatment. We collected 218 patients through a literature review and personal communications. We corresponded with several Authors t...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:1996-09-01 00:00:00
abstract:BACKGROUND:Measurement of cell survival as performed by the differential staining cytotoxicity (DiSC) assay allows for a comprehensive prediction of individual chemotherapy response. This assay has not reached routine clinical application because of its several limitations. In order to improve the DiSC assay, we develo...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2013-06-01 00:00:00
abstract:BACKGROUND/AIM:The aim of this study was to evaluate the impact of laparoscopic gastrectomy (LG) for gastric cancer on long-term survival in patients with postoperative infectious complications (PIC). PATIENTS AND METHODS:A total of 608 patients who underwent gastrectomy were classified into two groups based on the su...
journal_title:Anticancer research
pub_type: 杂志文章
doi:10.21873/anticanres.14740
更新日期:2020-12-01 00:00:00
abstract:BACKGROUND:Gemcitabine (2'-deoxy-2'-difluorodeoxycytidine: Gemzar) (GEM) appears to be the only effective anticancer drug for pancreatic cancer, but it has little impact on outcome due to a high level of inherent and acquired tumor resistance. Our previous proteomic study demonstrated that the expression of three spots...
journal_title:Anticancer research
pub_type: 杂志文章
doi:
更新日期:2010-07-01 00:00:00