ADS-J1 inhibits HIV-1 entry by interacting with gp120 and does not block fusion-active gp41 core formation.
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.
González-Ortega
Emmanuel
E
Retrovirology Laboratory IrsiCaixa, Hospital Universitari Germans Trias i Pujol, Universitat Auto´noma de Barcelona, 08916 Barcelona, Spain.
Mena
Maria-Pau
MP
Permanyer
Marc
M
Ballana
Ester
E
Clotet
Bonaventura
B
Esté
José A
JA
D019380:Anti-HIV Agents / Q000378:metabolism / Q000494:pharmacology*; D002460:Cell Line; D015699:HIV Envelope Protein gp120 / Q000378:metabolism*; D015700:HIV Envelope Protein gp41 / Q000378:metabolism*; D015497:HIV-1 / Q000187:drug effects* / Q000378:metabolism*; D006801:Humans; D009282:Naphthalenesulfonates / Q000378:metabolism / Q000494:pharmacology*; D014227:Triazines / Q000378:metabolism / Q000494:pharmacology*; D053586:Virus Internalization / Q000187:drug effects*
D019380:Anti-HIV Agents; D015699:HIV Envelope Protein gp120; D015700:HIV Envelope Protein gp41; D009282:Naphthalenesulfonates; D014227:Triazines; C407145:ADS J1