P-3A AND (-)-DESACETAMIDO P-3A - DEMONSTRATION AND STUDY OF THEIR EFFECTIVE FUNCTIONAL CLEAVAGE OF DUPLEX DNA

被引:15
作者
BOGER, DL
YANG, WJ
机构
[1] Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037
关键词
D O I
10.1016/S0960-894X(00)80449-7
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A study of the Fe(II) complexes of P-3A (1) and (-)-desacetamido P-3A (2) abilities to cleave duplex DNA was conducted through examination of single-strand and double-strand cleavage of supercoiled phiX 174 RFI DNA (Form I) in the presence of O2 to produce relaxed (Form II) and linear (Form III) DNA, respectively. Like Fe(II)-bleomycin A2 and deglycobleomycin A2, Fe(II)-1 and 2 effectively produced both single- and double-strand cleavage of supercoiled phiX174 DNA. Unlike Fe(II)-bleomycin A2 or deglycobleomycin A2, Fe(II)-l and 2 were found to cleave duplex w794 DNA with no discernible sequence selectively suggesting that the polynucleotide recognition of the C-terminus tetrapeptide S subunit of the bleomycins including the bithiazole may dominate the bleomycin A2 DNA cleavage selectivity.
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页码:1649 / 1654
页数:6
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