Inhibition of HIV Tat-TAR interactions by an antisense oligo-2′-O-methylribonucleoside methylphosphonate

Tomoko Hamma, Anthony Saleh, Ikramul Huq, Tariq M. Rana, Paul S. Miller

Research output: Contribution to journalArticlepeer-review

Abstract

An antisense oligo-2′-O-methylribonucleotide having alternating methylphosphonate/phosphodiester linkages, 1676, whose sequence is complementary to the apical stem-loop of HIV-1 TAR RNA, was prepared to determine its effects on Tat protein-TAR interaction and Tat-mediated gene transactivation in cell culture. This oligomer and its all-phosphodiester analogue, 1707, were shown to: (1) bind to TAR at 37°C with Kd's in the low nM concentration range; (2) inhibit Tat-TAR complex formation; and (3) inhibit expression of a chloramphenicol reporter gene under control of the HIV LTR in HeLa HL3T1 cells in culture.

Original languageEnglish (US)
Pages (from-to)1845-1848
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume13
Issue number11
DOIs
StatePublished - Jun 2 2003

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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