Immunostimulatory activity of CpG containing phosphorothioate oligodeoxynucleotide is modulated by modification of a single deoxynucleoside.
Phosphorothioate oligodeoxynucleotides (PS-oligos) containing the CpG motif have immunostimulatory properties. Our earlier study had shown that the immunostimulatory activity of PS-oligos containing the CpG motif can be modulated by incorporation of 2'-O-methylribonucleosides (Zhao, Q.; Yu, D.; Agrawal, S. Bioorg. Med. Chem. Lett. 1999, 9, 3453). Here we show that the immunostimulatory activity of a PS-oligo containing a CpG motif can be modulated by substitution of a single deoxynucleoside at specific sites with either 2'-O-methylribonucleoside or 3'-O-methylribonucleoside in the flanking region to CpG motif. Furthermore, substitution of deoxynucleosides with 2'-O-methoxyethoxyribonucleosides also results in modulating immunostimulatory activity of PS-oligos.
Zhao
Q
Q
Hybridon, Inc., Milford, MA 01757, USA.
Yu
D
D
Agrawal
S
S
D000818:Animals; D001483:Base Sequence; D002478:Cells, Cultured; D018899:CpG Islands; D007155:Immunologic Factors / Q000737:chemistry* / Q000494:pharmacology*; D008214:Lymphocytes / Q000187:drug effects; D051379:Mice; D009838:Oligodeoxyribonucleotides / Q000737:chemistry* / Q000494:pharmacology*; D009946:Organothiophosphorus Compounds / Q000737:chemistry / Q000494:pharmacology; D013154:Spleen / Q000187:drug effects / Q000276:immunology; D013329:Structure-Activity Relationship; D013873:Thionucleotides / Q000737:chemistry* / Q000494:pharmacology
D007155:Immunologic Factors; D009838:Oligodeoxyribonucleotides; D009946:Organothiophosphorus Compounds; D013873:Thionucleotides