Study on suitable analysis method for HIV-1 non-catalytic integrase inhibitor

Abstract Background Integrase (IN) is an essential protein for HIV replication that catalyzes insertion of the reverse-transcribed viral genome into host chromosome during early steps infection. Highly active anti-retroviral therapy a HIV/AIDS treatment method combines three or more antiviral drugs often formulated from compounds inhibit activities reverse transcriptase and protease enzymes. Early IN inhibitors (INIs) mainly serve as integrase strand transfer (INSTI) disrupt by binding catalytic core domain IN. However, mutations can confer resistance to INSTI. Therefore, non-catalytic (NCINI) have been developed next-generation INIs. Methods In this study, we evaluated compared activity INSTI NCINI according analysis method. Antiviral was using p24 ELISA with MT2 cell TZM-bl luciferase system cell. Each drug serially diluted treated TZM-b1 cells, infected HIV-1 AD8 strain incubated 5 2 days, respectively. Additionally, analyze properties NCINI, inhibition assay 3′-processing were performed. Results During screening INIs systems, found inconsistent result drugs. Following infection cells T-tropic strain, both treatments induced significant reduction in cells. showed no system, indicating widely used convenient antiretroviral not suitable target second round replication. Conclusion Accordingly, recommend application other procedures, such transcription activity, lieu preliminary screening. Utilization appropriate analytical methods based on underlying mechanisms necessary accurate assessment efficacy.