Cuenoud Bernard, Casset Florence, Hüsken Dieter, Natt François, Wolf Romain M, Altmann Karl-Heinz, Martin Pierre, Moser Heinz E
Novartis Horsham Research Centre, Wimblehurst road, Horsham, West Sussex, RH12 4AB (UK), Fax: (+44) 1403-32 33 07.
Novartis Pharma Ltd., Basel (Switzerland).
Angew Chem Int Ed Engl. 1998 May 18;37(9):1288-1291. doi: 10.1002/(SICI)1521-3773(19980518)37:9<1288::AID-ANIE1288>3.0.CO;2-U.
Simultaneous interaction of the 2'-aminoethoxy-modified oligonucleotides with the phosphodiester backbone (shown on the right, A) and with the bases through Hoogsteen base contacts (B) is seen at each base-pair step of the duplex DNA target. The electrostatic interaction between the protonated amino group and the negatively charged phosphate group provides for a dramatic increase in the binding affinity and the association rate constant.
在双链DNA靶标的每个碱基对步骤中,可以看到2'-氨基乙氧基修饰的寡核苷酸与磷酸二酯主链(如右侧A所示)以及通过Hoogsteen碱基接触与碱基同时发生相互作用。质子化氨基与带负电荷的磷酸基团之间的静电相互作用使得结合亲和力和缔合速率常数显著增加。