BMS707035 / BMS - LARVOL DELTA

HIV INTEGRASE INHIBITOR MK-2048 INDUCES APOPTOSIS IN HTLV-1 INFECTED CELLS THROUGH THE UPR ACTIVATION. (EHA 2019) - "...A recent study demonstrated the strong cytotoxic effect of Abacavir, a nucleoside analog reverse transcriptase inhibitor for HIV-1, on ATL cells. Previous studies also reported that HIV integrase inhibitors (INIs) prevented HTLV-1 integration, but the effect of HIV IN inhibitors on HTLV-1-infected cell survival remains unclear.Aims To investigate the cytotoxic effect of MK-2048, a second-generation HIV-1 INI, on HTLV-1 infected cells.Methods HTLV-1 infected cell lines and ATL derived cell lines were treated with six different HIV INIs (BMS-707035, Raltegravir, Elvitegravir, Cabotegravir, Dolutegravir, and MK-2048) and the number of viable cells 0-4 days after the treatment was measured by a luminescence assay (Cell Titer)...We also found that MK-2048 specifically induced CHOP in HTLV-1-infected cells of HTLV-1 carrier PBMCs by immunostaining.Conclusion Our findings demonstrated that MK-2048 selectively induces HTLV-1-infected cell death through the UPR activation...."

PARP Biomarker

Structure Based Drug Design: Clinically relevant HIV1 Integrase Inhibitors. (PubMed, Curr Top Med Chem) - "...Several integrase inhibitors have reached later stages of clinical trials including S-1360, L870,810, L870,812 and BMS-707035. Into the bargain, Raltegravir, Elvitegravir and Dolutegravir have been approved by FDA as anti-HIV agents...Additionally, the structural features required for overcoming HIV resistance have been discussed. These insights will update the ongoing design of novel antiviral inhibitors."

Clinical • Journal • Review