Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.6.3.44 (P-glycoprotein)
 13,344 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Toremifene, apart from its partial estrogen antagonism, exerts multiple and varied effects on a variety of genes involved in the control of signalling and apoptosis. After three weeks of exposure of R3230AC hosting rats to therapeutical oral doses of toremifene distinct changes in steroid receptors, P-glycoprotein, p53 and Bc1-2 expression and protein S100 levels occurred, which may contribute to our understanding of the mechanisms of action of this antiestrogen.
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PMID:The effect of toremifene on the expression of genes in a rat mammary adenocarcinoma. 889 31

MS-209 is a newly synthesised multidrug-resistance (MDR)-reversing agent with few side-effects. In this study, we evaluated the effect of MS-209 on P-glycoprotein (Pgp)-positive tumours in mice by means of technetium-99m methoxyisobutylisonitrile (MIBI) imaging. Mice received Pgp-negative KB-3-1 or Pgp-positive KB-C1 cell xenografts. KB-3-1-bearing mice were administered 0 or 100 mg/kg of MS-209 (groups S0 and S100, respectively), and KB-C1-bearing mice 0, 50, 100 or 200 mg/kg (groups R0, R50, R100 and R200, respectively), 30 min before imaging studies. Dynamic 99mTc-MIBI images were acquired for 30 min, followed by biodistribution studies. Washout of 99mTc-MIBI from the tumours was faster in group R0 than in group S0 on visual analysis, and the washout half-time estimated by region of interest analysis was shorter in group R0 than in group S0. Biodistribution studies revealed that 99mTc-MIBI accumulation in tumours (expressed as %ID/g) was also lower in group R0 than in group S0. MS-209 delayed the 99mTc-MIBI washout from KB-C1 tumours. Washout half-time was longer in groups R50, R100 and R200 than in group R0. A higher %ID/g was observed in groups R100 and R200 than in group R0. In KB-3-1 tumours, MS-209 had no effect on the washout half-time or the %ID/g. This study demonstrated that MS-209 increases the 99mTc-MIBI accumulation in Pgp-positive tumours. The MDR-reversing effect of MS-209 could be effectively evaluated with 99mTc-MIBI visually and non-invasively in vivo. 99mTc-MIBI imaging with MS-209 prior to chemotherapy should contribute significantly to the treatment strategy in patients with multidrug-resistant tumours.
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PMID:Evaluation of MS-209, a novel multidrug-resistance-reversing agent, in tumour-bearing mice by technetium-99m-MIBI imaging. 1200 1

From an undifferentiated soft tissue sarcoma (STS) a cell line designated US8-93 has been established. At subcloning the cell line US8-93 three different lines (US8-93A, B and C) could be set up. In a subsequent study characteristics for ultrastructure, growth, cell cycle distribution, karyotype, protein overexpression detected by immunohistochemistry (IHC) and p53 mutational status were determined. The cell line US8-93 as well as subclones contain mainly bipolar spindle-shaped cells and additionally some polygonal and multinucleated cells. Cells possess the characteristics of primitive mesenchymal cells based on their positive reactions with anti-vimentin and negative reactions for desmin, cytokeratin, myoglobin, S100, and NSE, implying a classification as an undifferentiated STS. Cytogenetic analysis revealed nearly diploid cells with several structural and numerical aberrations for chromosomes 1, 3, 4, 6, 9, 10, 12, 13, 15 and 18. IHC positivity was found for the tumor suppressor proteins p53 and Rb, the oncogene products Bcl-2, K-ras, N-ras, P-glycoprotein Mdr-1 and MDM-2. In the p53 gene a nonsense mutation in exon 4 was detected, that was confirmed in the original primary tumor and in three derivative clonal lines. The described STS cell line represents a valuable supplementation to the relatively small number of human STS cell lines currently available and may also provide a good in vitro model for studies of STS tumorigenesis in respect to a mutated p53 gene.
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PMID:Morphological and molecular characterization of an undifferentiated soft tissue sarcoma cell line and derivative clones. 2152 41