Nucleotide dimers suppress HIV expression in vitro

M. Busso, A. M. Mian, E. F. Hahn, L. Resnick

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Abstract

A series of nucleotide homo- and heterodimers [3'-azido-3'-deoxythymidilyl-(5',5')-2',3'-dideoxy-5'adenylic acid (AZT-P-ddA), [3'-azido-3'-deoxythymidilyl-(5',5')-2',3'-dideoxy;-5'adenylic acid, 2-cyanoethyl ester [AZT-P(CyE)-ddA], [3'-azido-3'-deoxythymidilyl-(5',5')-2',3'-dideoxy-5'-inosinic acid (AZT-P-ddI), and [3'-azido-3'-deoxythymidilyl-(5',5')-3'-azido-3'-deoxy-5'thymidilic acid (AZT-P-AZT)] were synthesized and compared with respect to their anti-HIV and cytotoxic properties to their component monomers in vitro. MT-2 cells were infected with HIV (TM) followed by the addition of drug. The dimers and their respective monomers inhibited HIV-induced syncytia formation, reverse transcriptase production, and the expression of HIV p24 antigen. However, on an equimolar basis, greater anti-HIV potency and enhanced cytotherapeutic indices were observed with the heterodimers when compared with their monomers. Nucleotide dimers, such as AZT-P-ddA, should be actively considered for further evaluation as anti-HIV agents.

Original languageEnglish
Pages (from-to)449-455
Number of pages7
JournalAIDS Research and Human Retroviruses
Volume4
Issue number6
StatePublished - Dec 1 1988

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ASJC Scopus subject areas

  • Immunology
  • Virology

Cite this

Busso, M., Mian, A. M., Hahn, E. F., & Resnick, L. (1988). Nucleotide dimers suppress HIV expression in vitro. AIDS Research and Human Retroviruses, 4(6), 449-455.