Antisense activity of an anti-HIV oligonucleotide conjugated to linear andbranched high molecular weight polyethylene glycols

An anti-HIV 12mer oligonucleotide (ODN) conjugated to two different high mo lecular 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 h as 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 12 mer, when conjugated to a branched (MPEG)(2), is fully inactive, as well as the native, unmodified ODN. (C) 1998 Elsevier Science S.A. All rights rese rved.