ADS-J1 inhibits HIV-1 entry by interacting with gp120 and does not block fusion-active gp41 core formation

Antimicrob Agents Chemother. 2010 Oct;54(10):4487-92. doi: 10.1128/AAC.00359-10. Epub 2010 Jul 19.

Abstract

We had shown that virus resistance to ADS-J1 was associated with amino acid changes in the envelope glycoprotein, mostly located in the gp120 coding region. Time-of-addition and endocytic virus transfer assays clearly demonstrated that ADS-J1 behaved as a gp120 inhibitor. ADS-J1-resistant virus was cross-resistant to the polyanion dextran sulfate, and recombination of gp120 recovered only the ADS-J1-resistant phenotype. In summary, ADS-J1 blocks an early step of virus entry that appears to be driven by gp120 alone.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / metabolism
  • Anti-HIV Agents / pharmacology*
  • Cell Line
  • HIV Envelope Protein gp120 / metabolism*
  • HIV Envelope Protein gp41 / metabolism*
  • HIV-1 / drug effects*
  • HIV-1 / metabolism*
  • Humans
  • Naphthalenesulfonates / metabolism
  • Naphthalenesulfonates / pharmacology*
  • Triazines / metabolism
  • Triazines / pharmacology*
  • Virus Internalization / drug effects*

Substances

  • Anti-HIV Agents
  • HIV Envelope Protein gp120
  • HIV Envelope Protein gp41
  • Naphthalenesulfonates
  • Triazines
  • ADS J1