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Medicinal Chemistry Reviews - Online (Discontinued)


ISSN (Print): 1567-2034
ISSN (Online): 1567-2034

The Molecular Targets of Anti-HIV-1 Triterpenes, An Update

Author(s): Li Huang and Chin Ho Chen

Volume 2, Issue 5, 2005

Page: [423 - 427] Pages: 5

DOI: 10.2174/156720305774330449

Price: $65


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.

Keywords: hiv, triterpene, targets, entry, maturation, protease, reverse transcriptase

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