Constant J F, O'Connor T R, Lhomme J, Laval J
LEDSS (UA CNRS 332), Chimie Recherche, Université Scientifique et Médicale de Grenoble, Saint-Martin d'Heres, France.
Nucleic Acids Res. 1988 Mar 25;16(6):2691-703. doi: 10.1093/nar/16.6.2691.
The incision of DNA at apurinic/apyrimidinic sites (AP-sites) by chloro-6-methoxy-2 [(adenyl-9)-11)-4,8 diazadecyl]amino-9 acridine (Ade-Z-Acr), a 9-aminoacridine linked to an adenine, at nanomolar concentrations is described. Moreover, this drug, Ade-Z-Acr, is one of the most efficient drugs which cleaves DNA at AP-sites. The high activity is the result of the composition of the drug, since the individual components have no incising activity in the concentration range studied. The termini left by the Ade-Z-Acr molecule are a 3'deoxyribose and a 5'nucleotide. The termini and the inability of the Ade-Z-Acr to incise DNA with reduced AP-sites suggest that the mechanism of cleavage is beta-elimination.
描述了纳米摩尔浓度的氯-6-甲氧基-2-[(腺嘌呤-9)-11)-4,8-二氮杂癸基]氨基-9-吖啶（Ade-Z-Acr，一种与腺嘌呤相连的9-氨基吖啶）在无嘌呤/无嘧啶位点（AP位点）切割DNA的情况。此外，这种药物Ade-Z-Acr是在AP位点切割DNA最有效的药物之一。其高活性是药物组成的结果，因为在所研究的浓度范围内，各个组分没有切割活性。Ade-Z-Acr分子留下的末端是一个3'-脱氧核糖和一个5'-核苷酸。这些末端以及Ade-Z-Acr在AP位点减少时无法切割DNA的情况表明，切割机制是β-消除。
