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Issue 10, 2014
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Peptide HIV fusion inhibitors: modifications and conjugations

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HIV fusion inhibitors are a group of virus entry preventing drugs aimed at membrane fusion. Several peptide drugs are screened with potent capacity to block virus-host cell fusion efficiently, and researchers have begun to focus on peptide drug design. However, so far T-20 is the only fusion inhibitor that has been approved by the FDA and utilised in treating therapy-experienced AIDS patients. The application of conventional peptide drugs is often limited by their short in vivo half-life and heavy dose subcutaneous injection. Thus, it is necessary to design new types of peptides or alter the existing peptides in a modified form to reach lower EC50 values and obtain longer in vivo half-lives. Here, we summarise the inhibitory mechanisms of peptide fusion inhibitors designed with anti-HIV potency. Also, we further discuss the recent achievement in these peptide derivatives. Several approaches have been applied to optimise the peptide properties, and we provide examples of successful peptide conjugation strategies to provide hints for additional peptide therapeutic design.

Graphical abstract: Peptide HIV fusion inhibitors: modifications and conjugations

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The article was received on 16 May 2014, accepted on 27 Jul 2014 and first published on 29 Jul 2014

Article type: Review Article
DOI: 10.1039/C4MD00214H
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Med. Chem. Commun., 2014,5, 1472-1482

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    Peptide HIV fusion inhibitors: modifications and conjugations

    W. Liu, J. Tan, M. M. Mehryar, Z. Teng and Y. Zeng, Med. Chem. Commun., 2014, 5, 1472
    DOI: 10.1039/C4MD00214H

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