Abstract
Gp41 is regarded as an attractive target for development of HIV-1 entry inhibitors since it mediates the fusion process of HIV- 1 entry into the target cell through the six-helix bundle (6-HB) formation between its N-heptad repeat (NHR) and C-heptad repeat (CHR). Any chemical entity that disrupts the six-helix bundle formation may inhibit the fusion process, thereby blocking HIV-1 entry into the target cells. A brief review of discovering small molecule inhibitors targeting gp41 is presented here, including the development of assay methods, current known small molecule inhibitors and their binding mode studies. Lessons learned and challenges remained in view of blocking protein-protein interaction between NHR and CHR are also discussed.
Keywords: gp41, HIV-1, assay, small molecule inhibitor, protein-protein interaction
Current Pharmaceutical Design
Title:Discovery of Small Molecule Fusion Inhibitors Targeting HIV-1 gp41
Volume: 19 Issue: 10
Author(s): Guangyan Zhou and Shidong Chu
Affiliation:
Keywords: gp41, HIV-1, assay, small molecule inhibitor, protein-protein interaction
Abstract: Gp41 is regarded as an attractive target for development of HIV-1 entry inhibitors since it mediates the fusion process of HIV- 1 entry into the target cell through the six-helix bundle (6-HB) formation between its N-heptad repeat (NHR) and C-heptad repeat (CHR). Any chemical entity that disrupts the six-helix bundle formation may inhibit the fusion process, thereby blocking HIV-1 entry into the target cells. A brief review of discovering small molecule inhibitors targeting gp41 is presented here, including the development of assay methods, current known small molecule inhibitors and their binding mode studies. Lessons learned and challenges remained in view of blocking protein-protein interaction between NHR and CHR are also discussed.
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Cite this article as:
Zhou Guangyan and Chu Shidong, Discovery of Small Molecule Fusion Inhibitors Targeting HIV-1 gp41, Current Pharmaceutical Design 2013; 19 (10) . https://dx.doi.org/10.2174/1381612811319100006
DOI https://dx.doi.org/10.2174/1381612811319100006 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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