Preferential inhibition of the activity of a stimulatory protein of eukaryotic transcription by platinum (II) complexes.
The effect of platinum(II) complexes on RNA polymerase II was studied. (D-Glucuronato)(1R,2R-cyclohexanediamine)platinum(II) nitrate (II-GHP) preferentially inhibited RNA synthesis in the presence of S-II, an essential component of eukaryotic transcription. When DNA was pretreated with I-GHP, its template activity decreased significantly, especially when assayed in the presence of S-II. The target of platinum(II) complexes is probably DNA. When DNA is modified, regulatory proteins of transcription, such as S-II, seem to lose their function preferentially on such a template, resulting in the inhibition of RNA synthesis.
D006367:HeLa Cells / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D009363:Neoplasm Proteins / Q000037:antagonists & inhibitors*; D009944:Organoplatinum Compounds / Q000494:pharmacology*; D012319:RNA Polymerase II / Q000378:metabolism; D012334:RNA, Neoplasm / Q000235:genetics; D013698:Templates, Genetic; D014157:Transcription Factors / Q000037:antagonists & inhibitors*; D035165:Transcription Factors, General; D014158:Transcription, Genetic / Q000187:drug effects*; D035602:Transcriptional Elongation Factors
D009363:Neoplasm Proteins; D009944:Organoplatinum Compounds; D012334:RNA, Neoplasm; D014157:Transcription Factors; D035165:Transcription Factors, General; D035602:Transcriptional Elongation Factors; C018648:transcription factor S-II; C030111:platinum(II) 1,2-diaminocyclohexane glucuronate; D012319:RNA Polymerase II