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Induction of a nonproductive conformational change in gp120 by a small molecule HIV type 1 entry inhibitor.

Publication ,  Journal Article
Huang, L; Lai, W; Ho, P; Chen, CH
Published in: AIDS Res Hum Retroviruses
January 2007

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.

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Published In

AIDS Res Hum Retroviruses

DOI

ISSN

0889-2229

Publication Date

January 2007

Volume

23

Issue

1

Start / End Page

28 / 32

Location

United States

Related Subject Headings

  • Virology
  • Triterpenes
  • Transfection
  • Protein Conformation
  • Protein Binding
  • Neutralization Tests
  • Humans
  • HIV-1
  • HIV Fusion Inhibitors
  • HIV Envelope Protein gp41
 

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Huang, L., Lai, W., Ho, P., & Chen, C. H. (2007). Induction of a nonproductive conformational change in gp120 by a small molecule HIV type 1 entry inhibitor. AIDS Res Hum Retroviruses, 23(1), 28–32. https://doi.org/10.1089/aid.2006.0137
Huang, Li, Weihong Lai, Phong Ho, and Chin Ho Chen. “Induction of a nonproductive conformational change in gp120 by a small molecule HIV type 1 entry inhibitor.AIDS Res Hum Retroviruses 23, no. 1 (January 2007): 28–32. https://doi.org/10.1089/aid.2006.0137.
Huang L, Lai W, Ho P, Chen CH. Induction of a nonproductive conformational change in gp120 by a small molecule HIV type 1 entry inhibitor. AIDS Res Hum Retroviruses. 2007 Jan;23(1):28–32.
Huang, Li, et al. “Induction of a nonproductive conformational change in gp120 by a small molecule HIV type 1 entry inhibitor.AIDS Res Hum Retroviruses, vol. 23, no. 1, Jan. 2007, pp. 28–32. Pubmed, doi:10.1089/aid.2006.0137.
Huang L, Lai W, Ho P, Chen CH. Induction of a nonproductive conformational change in gp120 by a small molecule HIV type 1 entry inhibitor. AIDS Res Hum Retroviruses. 2007 Jan;23(1):28–32.
Journal cover image

Published In

AIDS Res Hum Retroviruses

DOI

ISSN

0889-2229

Publication Date

January 2007

Volume

23

Issue

1

Start / End Page

28 / 32

Location

United States

Related Subject Headings

  • Virology
  • Triterpenes
  • Transfection
  • Protein Conformation
  • Protein Binding
  • Neutralization Tests
  • Humans
  • HIV-1
  • HIV Fusion Inhibitors
  • HIV Envelope Protein gp41