ArticleAntimicrobial agents and chemotherapy2012
Antimalarial activity of the anticancer histone deacetylase inhibitor SB939.
Article in Antimicrobial agents and chemotherapy, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 83 citations in OpenAlex.
- Hydroxamic Acids as HDAC Inhibitor Drug Leads for Malaria.Medicinal research reviews · 2026Review
- Repurposing 6‑Anilinopurine Derivatives That Exhibit PfHDAC1 Inhibition and Antimalarial Activity against Asexual and Sexual Stages ofACS omega · 2026Article
- Effects of SB939 are mediated by STAT3 to inhibit breast cancer cell metastasis-related genes.Oncology letters · 2025Article
- Marine-DerivedMicroorganisms · 2023Article
- The potential for histone deacetylase (HDAC) inhibitors as cestocidal drugs.PLoS neglected tropical diseases · 2021Article
- Antitheilerial Activity of the Anticancer Histone Deacetylase Inhibitors.Frontiers in microbiology · 2021Article
- A novel multistage antiplasmodial inhibitor targeting Plasmodium falciparum histone deacetylase 1.Cell discovery · 2020Article
- An ELISA method to assess HDAC inhibitor-induced alterations to P. falciparum histone lysine acetylation.International journal for parasitology. Drugs and drug resistance · 2020Article
- Discovery of FNDR-20123, a histone deacetylase inhibitor for the treatment of Plasmodium falciparum malaria.Malaria journal · 2020Article
- Disruption of theACS infectious diseases · 2020Article
- Epigenetic inhibitors target multiple stages of Plasmodium falciparum parasites.Scientific reports · 2020Article
- Histone deacetylase inhibitors with high in vitro activities against Plasmodium falciparum isolates collected from Gabonese children and adults.Scientific reports · 2019Article
- Structure-Activity and Structure-Toxicity Relationships of Peptoid-Based Histone Deacetylase Inhibitors with Dual-Stage Antiplasmodial Activity.ChemMedChem · 2019Article
- One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.European journal of medicinal chemistry · 2018Article
- In silico identification of inhibitors against Plasmodium falciparum histone deacetylase 1 (PfHDAC-1).Journal of molecular modeling · 2018Article
- Development of a Cell-Based High-Throughput Screening Assay to Identify Porcine Host Defense Peptide-Inducing Compounds.Journal of immunology research · 2018Article
- Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti-MedChemComm · 2017Article
- Effect of clinically approved HDAC inhibitors on Plasmodium, Leishmania and Schistosoma parasite growth.International journal for parasitology. Drugs and drug resistance · 2017Article
- Transcriptional Profiling Defines Histone Acetylation as a Regulator of Gene Expression during Human-to-Mosquito Transmission of the Malaria ParasiteFrontiers in cellular and infection microbiology · 2017Article
- Alternatives to currently used antimalarial drugs: in search of a magic bullet.Infectious diseases of poverty · 2016Review
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Histone deacetylase (HDAC) enzymes posttranslationally modify lysines on histone and nonhistone proteins and play crucial roles in epigenetic regulation and other important cellular processes. HDAC inhibitors (e.g., suberoylanilide hydroxamic acid [SAHA; also known as vorinostat]) are used clinically to treat some cancers and are under investigation for use against many other diseases. Development of new HDAC inhibitors for noncancer indications has the potential to be accelerated by piggybacking onto cancer studies, as several HDAC inhibitors have undergone or are undergoing clinical trials. One such compound, SB939, is a new orally active hydroxamate-based HDAC inhibitor with an improved pharmacokinetic profile compared to that of SAHA. In this study, the in vitro and in vivo antiplasmodial activities of SB939 were investigated. SB939 was found to be a potent inhibitor of the growth of Plasmodium falciparum asexual-stage parasites in vitro (50% inhibitory concentration [IC(50)], 100 to 200 nM), causing hyperacetylation of parasite histone and nonhistone proteins. In combination with the aspartic protease inhibitor lopinavir, SB939 displayed additive activity. SB939 also potently inhibited the in vitro growth of exoerythrocytic-stage Plasmodium parasites in liver cells (IC(50), ~150 nM), suggesting that inhibitor targeting to multiple malaria parasite life cycle stages may be possible. In an experimental in vivo murine model of cerebral malaria, orally administered SB939 significantly inhibited P. berghei ANKA parasite growth, preventing development of cerebral malaria-like symptoms. These results identify SB939 as a potent new antimalarial HDAC inhibitor and underscore the potential of investigating next-generation anticancer HDAC inhibitors as prospective new drug leads for treatment of malaria.
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