Three inhibitors of type 1 human immunodeficiency virus long terminal repeat-directed gene expression and virus replication

  1. C J Li,
  2. L J Zhang,
  3. B J Dezube,
  4. C S Crumpacker, and
  5. A B Pardee
  1. Dana-Farber Cancer Institute, Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02115.

Abstract

Transcription of type 1 human immunodeficiency virus (HIV-1) provirus is governed by the viral long terminal repeat (LTR). Drugs can block HIV-1 replication by inhibiting activity of its LTR. We report that topotecan, beta-lapachone, and curcumin are potent and selective inhibitors of HIV-1 LTR-directed gene expression, at concentrations that have minor effects on cells. At these concentrations, each drug inhibited p24 antigen production in cells either acutely or chronically infected with HIV-1. Their target is transcriptional function of the LTR.

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  1. PNAS March 1, 1993 vol. 90 no. 5 1839-1842
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