1988
DOI: 10.1021/tx00001a004
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Bleomycin congeners exhibiting altered DNA cleavage specificity

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Cited by 44 publications
(41 citation statements)
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“…Although it is known not to impact on the cleavage selectivity (5'-GC, 5'-GT), it does account for subtle differences in the relative selectivity among the available sites. [76,96] It is also known to enhance biological potency and efficacy and make significant contributions to the DNA cleavage efficiency and ratio of ds to ss cleavage. Although there are many plausible explanations, the mannose C3-carbamoyl group had been implicated in the metal complexation that affected the structure and reactivity of the metal complexes.…”
Section: The Carbohydrate Domainmentioning
confidence: 99%
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“…Although it is known not to impact on the cleavage selectivity (5'-GC, 5'-GT), it does account for subtle differences in the relative selectivity among the available sites. [76,96] It is also known to enhance biological potency and efficacy and make significant contributions to the DNA cleavage efficiency and ratio of ds to ss cleavage. Although there are many plausible explanations, the mannose C3-carbamoyl group had been implicated in the metal complexation that affected the structure and reactivity of the metal complexes.…”
Section: The Carbohydrate Domainmentioning
confidence: 99%
“…The C2-acetamido side chain is not intimately involved in the key metal chelation and subsequent oxygen activation and yet appears to be important to the natural product since epibleomycin A 2 [47] exhibits diminished biological activity and a reportedly altered DNA cleavage selectivity. [96] Studies on ()-P-3A and related agents also revealed a significant role for the C2-acetamido side chain in the DNA cleavage efficiency.…”
Section: ()-P-3a Epi-(à)-p-3a and (à)-Desacetamido P-3amentioning
confidence: 99%
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“…The metal binding domain lacking the disaccharide moiety failed to have any DNA cleavage activity above the background level (36). Bleomycinic acid, which only lacks of the terminal amine moiety compared with BLM A2, was only 35% effective on total DNA cleavage compared to that mediated by BLM A2 (37). The "extended" metal chelating unit, which includes the linker region, has not been synthesized yet and, thus, leaves us the question about the DNA cleavage activity of this key partial structure.…”
Section: Discussionmentioning
confidence: 99%
“…1999, 111, 470 ± 500 nicht stark auf die Spaltungsselektivität (5'-GC, 5'-GT) aus, ist aber für feine Unterschiede in der relativen Selektivität hinsichtlich der verfügbaren Bindungsstellen verantwortlich. [76,96] Es ist auch bekannt, daû die Disaccharid-Einheit die biologische Wirksamkeit erhöht und wesentliche Beiträge zur Effizienz der DNA-Spaltung und zum Verhältnis von ds-DNA-zu ss-DNA-Spaltung leistet. Wenngleich es viele andere plausible Erklärungen gibt, ist die Carbamoylgruppe am C3-Atom der Mannose mit der Metallionenkomplexierung in Zusammenhang gebracht worden; sie soll die Struktur und Reaktivität der Metallkomplexe beeinflussen.…”
Section: Die Kohlenhydratdomäneunclassified