Induction of a nonproductive conformational change in gp120 by a small molecule HIV type 1 entry inhibitor.
Journal Article (Journal Article)
Conformational changes in HIV-1 envelope glycoproteins, gp120 and gp41, is a dynamic process essential for HIV-1 entry. Here we show that a small molecule HIV-1 entry inhibitor, IC9564, induces a conformational change in gp120. The conformational change in gp120 is evidenced by a significant increase in the binding of a conformational monoclonal antibody 17b. As a result of the conformational effect, IC9564 significantly enhances the neutralizing activity of 17b. Unlike CD4, IC9564 does not trigger conformational changes in gp41. In fact, IC9564 inhibits CD4-induced conformational changes in gp41. Thus, IC9564 exploits the dynamic nature of gp120 by inducing a nonproductive gp120 conformation that is not able to trigger a conformational change in gp41 for membrane fusion.
Full Text
Duke Authors
Cited Authors
- Huang, L; Lai, W; Ho, P; Chen, CH
Published Date
- January 1, 2007
Published In
Volume / Issue
- 23 / 1
Start / End Page
- 28 - 32
PubMed ID
- 17263629
International Standard Serial Number (ISSN)
- 0889-2229
Digital Object Identifier (DOI)
- 10.1089/aid.2006.0137
Language
- eng
Conference Location
- United States