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Studies of Site Specific DNA Binding of Small Peptides by Competitive Assays with Hoechst 33258

小肽对Hoechst33258与DNA特异部位结合的竞争性作用
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摘要 With a view to finding out precisely how small peptides recognize a particular binding site of DNA, we have accomplished DNA binding studies of two peptides, H-Tyr-Arg-OH (YR) and H-Gly-Gly-His-OH (GGH) by using measurements in comparison with the binding between DNA and Hoechst 33258. The inhibition mode by YR and GGH to DNA binding of Hoechst 33258 was analyzed by Lineweaver-Burk plot which shows the plot of typical competitive inhibition at concentration of Hoechst 33258 from 3.66 ( 10-9 mol / L to 1.09 ( 10-8 mol / L. And it is concluded that YR binds to DNA in its minor groove (AT rich regions) with a binding constant K = 1.02 ( 108 (mol / L)-1. The GGH(s specificity is reduced at high concentration because it can also bind GC base pair. 为了了解小肽如何识别DNA特异的结合位点,我们研究了两个小肽YR和GGH对DNA与Hoechst33258特异结合的竞争性抑制作用。对Lineweaver-Burk图的分析显示当Hoechst33258的浓度在3.66(10-9mol/L(1.09(10-8mol/L范围内,这种作用是典型的竞争性抑制作用,YR结合在DNA小沟区(AT富集区),结合常数为1.02(108(mol/L)-1,而GGH的AT富集区结合特异性在浓度高时明显减弱。
出处 《Journal of Chinese Pharmaceutical Sciences》 CAS 1996年第3期141-146,共6页 中国药学(英文版)
关键词 DNA PEPTIDE Competitive inhibitor Site specific binding DNA 小肽 竞争性抑制剂 部位特异性结合
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