CYCLIC POLYAMIDES FOR RECOGNITION IN THE MINOR-GROOVE OF DNA

被引:51
作者
CHO, JY [1 ]
PARKS, ME [1 ]
DERVAN, PB [1 ]
机构
[1] CALTECH,BECKMAN INST,PASADENA,CA 91125
关键词
D O I
10.1073/pnas.92.22.10389
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
Small molecules that specifically bind with high affinity to any designated DNA sequence in the human genome would be useful tools in molecular biology and potentially in human medicine. Simple rules have been developed to rationally alter the sequence specificity of minor groove-binding polyamides containing N-methylimidazole and N-methylpyrrole amino acids. Crescent-shaped polyamides bind as antiparallel dimers with each polyamide making specific contacts with each strand on the floor of the minor groove. Cyclic polyamides have now been synthesized that bind designated DNA sequences at subnanomolar concentrations.
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页码:10389 / 10392
页数:4
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