Oligonucleotide (ODN) directed triplex formation has therapeutic importance and depends on Hoogsteen hydrogen bonds between a duplex DNA and a third strand. While T*AC are favoured at acidic pH.

Herein it is shown that 18-mer ODN containing spermine conjugated to 5-Me-dC at N4 (1-5), form triplexes with complementary 24-mer duplex 89 at neutral pH (7.3, 100 mM NaCl). Under such conditions, control ODN's carrying dC (6) or 5-Me-dC (7) did not show any triple helix formation. Remarkably, the triplexes from spermine-conjugates (1-5) have foremost stability at neutral pH (7.1), unlike the behavior of normal ODN's where optimal stability is at acidic pH (5.5). These results have importance in designing oligonucleotides for antigene applications.

译文

寡核苷酸(ODN)指导的三链体形成具有治疗重要性,并取决于双链体DNA和第三条链之间的Hoogsteen氢键。虽然T * AC在酸性pH下是有利的。

此处显示,在N4(1-5)处与5-Me-dC缀合的精胺的18-mer ODN形成与互补的24-mer双链体形成的三链体在中性pH(7.3,100 mM NaCl)下为89。在这种条件下,对照ODN带有dC(6)或5-Me-dC(7)不会显示任何三重螺旋结构。值得注意的是,与精胺结合物(1-5)形成的三链体在中性pH(7.1)时具有最强的稳定性,这与正常ODN在酸性pH(5.5)时具有最佳稳定性的行为不同。这些结果对于设计用于抗原的寡核苷酸具有重要意义。

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