Discovery and in Vitro Development of AIDS Antiviral Drugs as Biopharmaceuticals

Inhibition of G-protein-coupled Receptor Function by Disruption of Transmembrane Domain Interactions

“…Anti-HIV-1 Assay-The effects of various TM peptides on HIV-1 replication were determined with CEM-SS cells infected with HIV-1 RF utilizing the XTT (2,3-bis(2-methoxy-4-nitro-5-sulfophenyl)-5-[(phenylamino)carbonyl]-2H-tetrazolium hydroxide) cell assay as described previously (27).…”

“…Anti-HIV-1 activity was assessed in a cytoprotection assay utilizing CEM-SS cells infected with HIV-1 RF as described (27). ND, not determined.…”

“…Anti-HIV efficacy and toxicity of CXCR4-4-2 in cytoprotection assay. CEM-SS cells were infected with RF strain of HIV-1, which causes cell death in the absence of an effective inhibitor (27). Cell survival was assessed with the help of the XTT (2,3-bis(2-methoxy-4-nitro-5-sulfophenyl)-5-[(phenylamino)carbonyl]-2H-tetrazolium hydroxide) assay (27).…”

“…Given that CXCR4 represents one of the principal coreceptors for HIV-1 cell entry (reviewed in Ref. 26) and that the TM domain peptides of CXCR4 interfere with receptor functions, we tested TM peptide analogs (corresponding to TM domains 2, 4, 6, or 7) as possible inhibitors of HIV-1 RF replication in a cell-based cytoprotection assay (27). As shown in Table III, the most potent peptide, CXCR4-4-2, inhibited infection at concentrations below 1 M (IC 50 Ϸ 300 nM) (see also Fig.…”

5α-Reductase inhibitors, antiviral and anti-tumor activities of some steroidal cyanopyridinone derivatives

“…Test In vitro antiviral assays. Evaluation of the antiviral activity of compounds against HIV-1RF infection in CEM-SS cells was performed using the MTS cytoprotection assay as previously described [25]. Evaluation of the antiviral activity of the compounds against HIV-1 strain IIIB and HIV-2 strain (ROD) in MT-4 cells was performed using the MTT assay as previously described [27,28].…”