摘要 |
<p>This invention provides oligonucleotides having a region of four or more G nucleotides at or near their 5' end and in which from one to all of the 5'-most nucleotides bears a 2' substituent, preferably methoxy, the 3'-terminal nucleotide of the oligonucleotide bears a hydrophobic moiety, preferably cholesterol, or both the 3'-terminal nucleotide bears a hydrophobic moiety and the 5'-most nucleotides are 2'-substituted. Both attachment of a hydrophobic moiety to the 3'-terminal nucleotide of the oligonucleotide and 2'-substitution at the 5'-end results in increased tetraplex stability. The presence of these Hoogsteen base-paired G-quartet structures, however, does not hamper their ability to recognize and form Watson-Crick base-paired duplexes with complementary oligonucleotides. Accordingly, the invention also provides methods of using the disclosed oligonucleotides for nucleic acid expression inhibition.</p> |