Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:5.99.1.2 (topoisomerase)
 9,166 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A series of unsymmetrically substituted polyamine derivatives were prepared and their cytotoxicities in mouse leukemia L1210, melanoma B16, and HeLa cells were investigated. The in vitro cytotoxicity revealed that these conjugates could recognize the polyamine transporter, and the N-ethyl modified homospermidine moiety may be another efficient carrier as homospermidine even though the introduction of terminal alkyl groups led to reduced cytotoxicity in comparison with the un-substituted counterpart 1. The ornithine decarboxylase and topoisomerase II inhibition experiments indicated that ODC and TOPO II were potential, but not unique targets of these conjugates. Furthermore, the in vivo antitumor activities illustrated that the representative conjugate 2f and the homospermidine analogue 1 evidently inhibited the tumor growth and significantly increased the survival time of mice-bearing sarcoma 180 cells.
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PMID:Synthesis and evaluation of unsymmetrical polyamine derivatives as antitumor agents. 1853 36

The aim of this investigation was to analyze whether or not ionizing radiation can induce the expression of resistance- and oncoproteins in murine sarcoma 180 cells and several human carcinoma cell lines. For assessment of the proteins the streptavidin-biotin peroxidase-complex method was performed using specific antibodies. Expression of glutathione S-transferase-pi and thymidylate-synthase was increased after a single dose of irradiation which was accompanied by a lower sensitivity against cisplatin and 5-fluorouracil. No differences in protein expression could be detected for P-glycoprotein 170 and topoisomerase II. Differences in the expression of the oncoproteins c-Fos and c-ErbB1 were also found after irradiation. In contrast, a decreased expression of topoisomerase II was found after fractionated irradiation. This was confirmed by mRNA analysis.
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PMID:Induction of resistance-proteins and oncoproteins in murine and human tumor-cell lines after irradiation. 2159 37