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与DNA嵌入是柔红霉素、阿霉素及其同系物抑制DNA酶I的一个先决条件。

Intercalation with DNA is a prerequisite for daunomycin, adriamycin and its congeners in inhibiting DNAase I.

作者信息

Facchinetti T, Mantovani A, Cantoni L, Cantoni R, Salmona M

出版信息

Chem Biol Interact. 1978 Jan;20(1):97-102. doi: 10.1016/0009-2797(78)90084-4.

Abstract

DNAase I from bovine pancreas is inhibited by Daunomycin, Adriamycin, Adriamycin-14-acetate and Adriamycin-14-octanoate, whereas it is not inhibited by N-trifluoroacetyladriamycin-14-valerate or N-trifluoroacetyl-adriamycin. The present study suggests that these inhibitors act not directly on the enzyme, but on DNA, forming stable complexes and thus interfering with enzyme activity. The correlation between DNA binding and enzyme inhibition is demonstrated by the fact that the compounds forming complexes with DNA inhibit DNAase I activity, whereas those which do not form complexes with DNA cause no inhibition.

摘要

来自牛胰腺的脱氧核糖核酸酶I受到柔红霉素、阿霉素、阿霉素-14-乙酸酯和阿霉素-14-辛酸酯的抑制,而不受N-三氟乙酰阿霉素-14-戊酸酯或N-三氟乙酰阿霉素的抑制。本研究表明,这些抑制剂并非直接作用于酶,而是作用于DNA,形成稳定的复合物,从而干扰酶的活性。与DNA形成复合物的化合物抑制脱氧核糖核酸酶I的活性,而那些不与DNA形成复合物的化合物则不产生抑制作用,这一事实证明了DNA结合与酶抑制之间的相关性。

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