Antisense activity of an anti-HIV oligonucleotide conjugated to linear and branched high molecular weight polyethylene glycols.
An anti-HIV 12mer oligonucleotide (ODN) conjugated to two different high molecular weight monomethoxy polyethylene glycols (MPEGs) has been tested for its antisense activity. The capacity of these conjugates to protect the MT-4 cells against HIV infection has been compared to the unmodified, native ODN, and the effect of the different structures of the supporting polymer has been discussed. It was found that only the ODN conjugated to the linear MPEG shows an anti-HIV activity in the investigated conditions. The same 12mer, when conjugated to a branched (MPEG)2, is fully inactive, as well as the native, unmodified ODN.
Bonora
G M
GM
Institute of Molecular Virology, Novosibirsk, Russia.
Tocco
G
G
Zaramella
S
S
Veronese
F M
FM
Pliasunova
O
O
Pokrovsky
A
A
Ivanova
E
E
Zarytova
V
V
D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D002470:Cell Survival / Q000187:drug effects; D002478:Cells, Cultured / Q000187:drug effects; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D008970:Molecular Weight; D016376:Oligonucleotides, Antisense / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D011092:Polyethylene Glycols / Q000737:chemistry*; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D016376:Oligonucleotides, Antisense; D011092:Polyethylene Glycols