ADS-J1 inhibits HIV-1 entry by interacting with gp120 and does not block the fusion-active gp41 core formation.
Antimicrobial agents and chemotherapy 2010 Jul 19; In press
González-Ortega E, Mena M MP, Permanyer M, Ballana E, Clotet B, Esté J JA
Retrovirology Laboratory IrsiCaixa, Hospital Universitari Germans Trias i Pujol, Universitat Autónoma de Barcelona, 08916 Barcelona, Spain.
We had shown that virus resistance to ADS-J1 was associated to 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 only recovered the ADS-J1-resistant phenotype. In summary, ADS-J1 blocks an early step of virus entry that appears to be driven by gp120 alone.
