MAN-DESIGNED BLEOMYCINS - SIGNIFICANCE OF THE BINDING-SITES AS ENZYME MODELS AND OF THE STEREOCHEMISTRY OF THE LINKER MOIETY

被引：57

作者：

OWA, T

HAUPT, A

OTSUKA, M

KOBAYASHI, S

TOMIOKA, N

ITAI, A

OHNO, M

SHIRAKI, T

UESUGI, M

SUGIURA, Y

MAEDA, K

机构：

[1] UNIV TOKYO,FAC PHARMACEUT SCI,BUNKYO KU,TOKYO 113,JAPAN

[2] KYOTO UNIV,INST CHEM RES,UJI,KYOTO 611,JAPAN

[3] INST MICROBIAL CHEM,SHINAGAWA KU,TOKYO 141,JAPAN

来源：

TETRAHEDRON | 1992年 / 48卷 / 07期

关键词：

BLEOMYCIN; DNA CLEAVAGE; METAL BINDING SITE; DNA BINDING SITE; LINKER MOIETY;

D O I：

10.1016/S0040-4020(01)90783-5

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Comparison of the DNA cleavage activity of man-designed bleomycins demonstrates that bleomycins are small enzymes comprised of a catalytic site and a binding site. The linker moiety is shown to be significant for DNA binding, and inversion of its stereochemistry results in a dramatic decrease in the DNA-cleaving efficiency. One of the man-designed BLMs shows excellent cytotoxicity against L1210.

引用

页码：1193 / 1208

页数：16

共 29 条

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