ArticleThe Journal of biological chemistry2019
Benzolactam-related compounds promote apoptosis of HIV-infected human cells via protein kinase C-induced HIV latency reversal.
Article in The Journal of biological chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 38 citations in OpenAlex.
- World free HIV: the novel therapeutic approaches for eliminating latent HIV infection.Virology journal · 2026Review
- Hybrid immunity from bivalent vaccination and prior infection enhances humoral and innate protection against Omicron XBB.1.16 and EG.5.1.1 variants in Japan.Frontiers in immunology · 2026Article
- Effects of Oxygen Atom Position in Linear Side Chains of Ansellone Analogues on HIV Latency-Reversing Activity.ACS medicinal chemistry letters · 2025Article
- A high-throughput, microplate reader-based method to monitor in vitro HIV latency reversal in the absence of flow cytometry.Virology · 2025Article
- HIV Reservoirs and Treatment Strategies toward Curing HIV Infection.International journal of molecular sciences · 2024Review
- Synthesis and evaluation of DAG-lactone derivatives with HIV-1 latency reversing activity.European journal of medicinal chemistry · 2023Article
- Medicinal Chemistry of Anti-HIV-1 Latency Chemotherapeutics: Biotargets, Binding Modes and Structure-Activity Relationship Investigation.Molecules (Basel, Switzerland) · 2022Review
- A widely distributed HIV-1 provirus elimination assay to evaluate latency-reversing agentsCell reports methods · 2021Article
- Article
- Selective elimination of host cells harboring replication-competent human immunodeficiency virus reservoirs: a promising therapeutic strategy for HIV cure.Chinese medical journal · 2021Article
- Selective cell death in HIV-1-infected cells by DDX3 inhibitors leads to depletion of the inducible reservoir.Nature communications · 2021Article
- Review
- Inducible HIV-1 Reservoir Quantification: Clinical Relevance, Applications and Advancements of TILDA.Frontiers in microbiology · 2021Article
- A Therapeutic Strategy to Combat HIV-1 Latently Infected Cells With a Combination of Latency-Reversing Agents Containing DAG-Lactone PKC Activators.Frontiers in microbiology · 2021Article
- Structural insights into C1-ligand interactions: Filling the gaps by in silico methods.Advances in biological regulation · 2021Review
- Article
- Strategies to eradicate HIV from infected patients: elimination of latent provirus reservoirs.Cellular and molecular life sciences : CMLS · 2019Review
- Arsenic Trioxide Impacts Viral Latency and Delays Viral Rebound after Termination of ART in Chronically SIV-Infected Macaques.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2019Article
- Discovery and Development of Anti-HIV Therapeutic Agents: Progress Towards Improved HIV Medication.Current topics in medicinal chemistry · 2019Review
Corrections and comments
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Authors and funding
12 authors at 5 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Latency-reversing agents (LRAs) are considered a potential strategy for curing cells of HIV-1 infection. Certain protein kinase C (PKC) activators have been previously reported to be LRAs because they can reverse HIV latency. In the present study, we examined the activities of a panel of benzolactam derivatives against cells latently infected with HIV. Using determination of p24 antigen in cell supernatants or altered intracellular GFP expression to measure HIV reactivation from latently infected cells along with a cytotoxicity assay, we found that some of the compounds exhibited latency-reversing activity, which was followed by enhanced release of HIV particles from the cells. One derivative, BL-V8-310, displayed activity in ACH-2 and J-Lat cells latently infected with HIV at a concentration of 10 nm or higher, which was superior to the activity of another highly active PKC activator, prostratin. These results were confirmed with peripheral blood cells from HIV-infected patients. We also found that these drugs up-regulate the expression of caspase 3 and enhance apoptosis specifically in latently HIV-infected cells. Moreover, combining BL-V8-310 with a bromodomain-containing 4 (BRD4) inhibitor, JQ1, not only enhanced HIV latency-reversing activity, but also reduced the effect on cytotoxic cytokine secretion from CD4
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