Multifunctional Antiviral Poly=DNP-Oligonucleotides

摘要

Monofunctional,bifunctional and trifunctional poly-2'-(2,4-dinitrophenyl)-oligoribonucleotides have been designed and synthesized as inhibitors of retroviruses. These compounds are membrane-permeable,ribonuclease-resistant, and apparently mutation-insensitive inhibitors of reverse transcriptases. These inhibitors have been tested for the treatment of murine leukemia as an animal model related to AIDS. Although the monofunctional inhibitor is already 100% effective for the treatment of murine leukemia, its efficacy can be increased by two orders of magnitude by introducing antisense sequences in the nucleotide backbone so that the resulting multifunctional inhibitor can also disrupt the synthesis of specific viral proteins. The entripy advantage of multifuncionality in the design of antiviral agents is discussed.