DNA结合活性及对DNA-蛋白质相互作用的抑制作用。四对脒基苯氧基新戊烷及其2'-溴衍生物的不同效应。

DNA binding activity and inhibition of DNA-protein interactions. Differential effects of tetra-p-amidino-phenoxyneopentane and its 2'-bromo derivative.

作者信息

Nastruzzi C, Menegatti E, Pastesini C, Cortesi R, Esposito E, Spano M, Biagini R, Cordelli E, Feriotto G, Gambari R

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Italy.

出版信息

Biochem Pharmacol. 1992 Nov 17;44(10):1985-94. doi: 10.1016/0006-2952(92)90101-n.

DOI:10.1016/0006-2952(92)90101-n

PMID:1449517

Abstract

In the present study are reported the differential DNA binding activity of the anti-tumor polyamidine tetra-p-amidinophenoxyneopentane (TAPP-H) and its 2'-halo derivative (TAPP-Br), and their effects on the binding of the recombinant Epstein-Barr virus (EBV) nuclear antigen to a synthetic oligonucleotide mimicking the target DNA sequence present in the EBV genome. In addition, the proliferation kinetics and cell cycle analysis of human leukemia K562 cells treated with TAPP-H and TAPP-Br are reported. The possible in vivo relationship between DNA binding affinity and cytotoxicity is also discussed.

摘要

本研究报道了抗肿瘤聚脒四 - 对 - 脒基苯氧基新戊烷（TAPP - H）及其2'-卤代衍生物（TAPP - Br）的差异DNA结合活性，以及它们对重组爱泼斯坦 - 巴尔病毒（EBV）核抗原与模拟EBV基因组中靶DNA序列的合成寡核苷酸结合的影响。此外，还报道了用TAPP - H和TAPP - Br处理的人白血病K562细胞的增殖动力学和细胞周期分析。还讨论了DNA结合亲和力与细胞毒性之间可能的体内关系。