The molecular targets of anti-HIV-1 triterpenes, an update


Journal Article (Review)

Pentacyclic triterpenes have been found in many plants and can be isolated from any parts of the plant. Triterpene derivatives were shown to have biological activities including anti-HIV-1 and anti-cancer. The modes of action of the anti-HIV-1 triterpenes have been reported to be associated with virus entry, reverse transcription, virus assembly, and maturation. This review will focus on the mechanisms of action of anti-HIV triterpenes and the structural features that contribute to their anti-HIV-1 activity. Two classes of triterpenes are particularly potent and highly selective: one inhibits HIV-1 entry and the other interferes with HIV-1 maturation. Significant progresses have been made in identifying the mechanisms of action for these two classes of anti-HIV-1 triterpenes. The anti-HIV-1 entry activity is associated with a side chain at position 28 and the anti-HIV-1 maturation activity is associated with the pharmacophore at position 3. Compounds containing both of the pharmacophores at 3 and 28 positions can potently inhibit HIV-1 through their anti-HIV-1 entry and maturation activities. Although the detail mechanisms of action remains unclear, the anti-entry triterpenes target HIV-1 envelope glycoprotein, and the anti-maturation triterpenes affect the processing of the HIV-1 gag protein, CA-SP1. © 2005 Bentham Science Publishers Ltd.

Full Text

Duke Authors

Cited Authors

  • Huang, L; Chen, CH

Published Date

  • January 1, 2005

Published In

Volume / Issue

  • 2 / 5

Start / End Page

  • 423 - 427

Electronic International Standard Serial Number (EISSN)

  • 1567-2700

International Standard Serial Number (ISSN)

  • 1567-2700

Digital Object Identifier (DOI)

  • 10.2174/156720305774330449

Citation Source

  • Scopus