ArticleInternational journal for parasitology. Drugs and drug resistance2015
Profiling the anti-protozoal activity of anti-cancer HDAC inhibitors against Plasmodium and Trypanosoma parasites.
Article in International journal for parasitology. Drugs and drug resistance, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 49 papers.
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Who cites it
49 citing papers in PubMed, 94 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
- A propidium iodide-basedAntimicrobial agents and chemotherapy · 2025Article
- Targeting histone acetylation to overcome drug resistance in the parasitebioRxiv : the preprint server for biology · 2025Article
- PfHDAC1 is an essential regulator ofmBio · 2024Article
- Epigenetic regulation as a therapeutic target in the malaria parasite Plasmodium falciparum.Malaria journal · 2024Review
- 1,3-Diphenylureido hydroxamate as a promising scaffold for generation of potent antimalarial histone deacetylase inhibitors.Scientific reports · 2023Article
- Epidrugs as Promising Tools to EliminatePharmaceutics · 2023Article
- A Subset Screen of the Compounds Australia Scaffold Library Identifies 7-Acylaminodibenzoxazepinones as Potent and Selective Hits for Anti-Biomedicines · 2022Article
- New Transmission-Selective Antimalarial Agents through Hit-to-Lead Optimization of 2-([1,1'-Biphenyl]-4-carboxamido)benzoic Acid Derivatives.Chembiochem : a European journal of chemical biology · 2022Article
- Effectiveness of anAnimals : an open access journal from MDPI · 2022Article
- Histone Deacetylase (HDAC) Inhibitors for the Treatment of Schistosomiasis.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Article
- Antimalarial Natural Products.Progress in the chemistry of organic natural products · 2022Article
- Antimalarial Inhibitors Targeting Epigenetics or Mitochondria inMolecules (Basel, Switzerland) · 2021Review
- Antiplasmodial activity of the natural product compounds alstonine and himbeline.International journal for parasitology. Drugs and drug resistance · 2021Article
- An Overview on Target-Based Drug Design against Kinetoplastid Protozoan Infections: Human African Trypanosomiasis, Chagas Disease and Leishmaniases.Molecules (Basel, Switzerland) · 2021Review
- Identification of benzamide inhibitors of histone deacetylase 1 from Babesia and Theileria species via high-throughput virtual screening and molecular dynamics simulations.Parasitology research · 2021Article
- 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
Corrections and comments
- Erratum issuedErratum to "Profiling the anti-protozoal activity of anti-cancer HDAC inhibitors against Plasmodium and Trypanosoma parasites" [Int. J. Parasitol. Drugs Drug Res. 5 (2015) 117-126].2016 · Adams, Tina S [corrected to Skinner-Adams, Tina]
Authors and funding
8 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Histone deacetylase (HDAC) enzymes work together with histone acetyltransferases (HATs) to reversibly acetylate both histone and non-histone proteins. As a result, these enzymes are involved in regulating chromatin structure and gene expression as well as other important cellular processes. HDACs are validated drug targets for some types of cancer, with four HDAC inhibitors clinically approved. However, they are also showing promise as novel drug targets for other indications, including malaria and other parasitic diseases. In this study the in vitro activity of four anti-cancer HDAC inhibitors was examined against parasites that cause malaria and trypanosomiasis. Three of these inhibitors, suberoylanilide hydroxamic acid (SAHA; vorinostat(®)), romidepsin (Istodax(®)) and belinostat (Beleodaq(®)), are clinically approved for the treatment of T-cell lymphoma, while the fourth, panobinostat, has recently been approved for combination therapy use in certain patients with multiple myeloma. All HDAC inhibitors were found to inhibit the growth of asexual-stage Plasmodium falciparum malaria parasites in the nanomolar range (IC50 10-200 nM), while only romidepsin was active at sub-μM concentrations against bloodstream form Trypanosoma brucei brucei parasites (IC50 35 nM). The compounds were found to have some selectivity for malaria parasites compared with mammalian cells, but were not selective for trypanosome parasites versus mammalian cells. All compounds caused hyperacetylation of histone and non-histone proteins in P. falciparum asexual stage parasites and inhibited deacetylase activity in P. falciparum nuclear extracts in addition to recombinant PfHDAC1 activity. P. falciparum histone hyperacetylation data indicate that HDAC inhibitors may differentially affect the acetylation profiles of histone H3 and H4.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.