Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative

M. Baba, H. Tanaka, E. De Clercq, R. Pauwels, J. Balzarini, D. Schols, H. Nakashima, C. F. Perno, R. T. Walker, T. Miyasaka

Research output: Contribution to journalArticle

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Abstract

A novel 6-substituted acyclouridine derivative, 1-[(2-hydroxy-ethoxy) methyl]-6-phenylthiothymine (HEPT), has proved to be a potent and selective inhibitor of human immunodeficiency virus type 1 (HIV-1) in vitro. HEPT inhibits HIV-1 replication in various T4 cell cultures as well as peripheral blood lymphocytes and macrophages. The 50% antiviral effective concentration for HIV-1 (HTLV-IIIB) in MT-4 cells is 7.0 μM, while the 50% cytotoxic concentration for mock-infected MT-4 cells is 740 μM. Although HEPT is inhibitory to various strains of HIV-1, it has no effect on the replication of other retroviruses including HIV type 2. In contrast with the dideoxynucleoside (i.e. azidothymidine) 5′-triphosphates, the triphosphate of HEPT does not interact with HIV-1 reverse transcriptase. The mechanism of action of HEPT remains subject of further study.

Original languageEnglish
Pages (from-to)1375-1381
Number of pages7
JournalBiochemical and Biophysical Research Communications
Volume165
Issue number3
DOIs
Publication statusPublished - Dec 30 1989

Fingerprint

Viruses
HIV-1
Derivatives
Dideoxynucleosides
Lymphocytes
Zidovudine
Macrophages
CD4-Positive T-Lymphocytes
Cell culture
HIV-2
Antiviral Agents
Retroviridae
Virus Replication
Blood
Cell Culture Techniques
triphosphoric acid

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology

Cite this

Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative. / Baba, M.; Tanaka, H.; De Clercq, E.; Pauwels, R.; Balzarini, J.; Schols, D.; Nakashima, H.; Perno, C. F.; Walker, R. T.; Miyasaka, T.

In: Biochemical and Biophysical Research Communications, Vol. 165, No. 3, 30.12.1989, p. 1375-1381.

Research output: Contribution to journalArticle

Baba, M, Tanaka, H, De Clercq, E, Pauwels, R, Balzarini, J, Schols, D, Nakashima, H, Perno, CF, Walker, RT & Miyasaka, T 1989, 'Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative', Biochemical and Biophysical Research Communications, vol. 165, no. 3, pp. 1375-1381. https://doi.org/10.1016/0006-291X(89)92756-3
Baba, M. ; Tanaka, H. ; De Clercq, E. ; Pauwels, R. ; Balzarini, J. ; Schols, D. ; Nakashima, H. ; Perno, C. F. ; Walker, R. T. ; Miyasaka, T. / Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative. In: Biochemical and Biophysical Research Communications. 1989 ; Vol. 165, No. 3. pp. 1375-1381.
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