A mid-throughput HBV replication inhibition assay capable of detecting ribonuclease H inhibitors

Antiviral Evaluation of Dispirotripiperazines against Hepatitis B Virus

“…Cytotoxicity was measured using an MTS assay as described previously. 47 Capsid Quantification. HBV nucleocapsid levels were measured in HepDES19 cells replicating HBV after 5 days of compound treatment.…”

“…HBV inhibition potential was measured in HepDES19 cells, a HepG2 derivative carrying a tetracycline-repressible HBV genomic expression cassette . Replication was detected after 3 days of compound exposure in cells induced to replicate HBV by tetracycline withdrawal using a strand-preferential quantitative PCR assay described to help define the steps during HBV replication that were possible targets of the DSTPs. Cytotoxicity was measured using an MTS assay as described previously …”

Therapies against chronic hepatitis B infections: The times they are a-changin’, but the changing is slow!

“…NAs target the reverse transcription activity of the HBV polymerase. But HBV-pol contains also a RNAseH domain which is important to degrade RNA templates during the RT process (Edwards et al, 2019); this enzymatic activity is considered as a possible drug target, with the identification of three different chemical families that inhibit its activity (Edwards et al, 2019;Li et al, 2021a); Structure-activityrelationship studies are on-going to improve the potency and toxicological profile of these drugs, which are rather low as off today. Mechanistically speaking, these inhibitors should reinforce the inhibition of mature nucleocapsid formation, which can be obtained with NAs and/ or CpAMs (Fig.…”