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- W118018003 abstract "DNA binding appears to be a necessary albeit not sufficient condition for antitumor activity in the anthracyclines. Apparently, a step different from that of intercalation, as for instance interaction of the complex with an enzyme like topoisomerase II, should be responsible with bioactivity. The latter might be related with the presence of GC rich sequences. This hypothesis stems from both experimental and computational results coupled with structure-activity relationships. Distamycin and related compounds owe their pharmacological effects to an interaction at the level of transcription and this property is related with the high affinity for AT/TA rich sequences. Derivatives containing alkylating functions are endowed with high antitumor activity. Among the different biochemical consequences of the peculiar DNA binding ability of distamycin the interference with the binding of nuclear transacting factors to cis elements of the eukariotic genes is exemplified in recent experimental investigations.KeywordsIntercalation ComplexAntitumor AntibioticIntercalation SiteRecent Experimental InvestigationAnthracycline DerivativeThese keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves." @default.
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- W118018003 date "1990-01-01" @default.
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- W118018003 title "Antitumor Antibiotics Endowed with DNA Sequence Specificity" @default.
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