ArticleBritish journal of pharmacology2008
Mono-galloyl glucose derivatives are potent poly(ADP-ribose) glycohydrolase (PARG) inhibitors and partially reduce PARP-1-dependent cell death.
Article in British journal of pharmacology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 46 citations in OpenAlex.
- ADP-ribose hydrolases: biological functions and potential therapeutic targets.Expert reviews in molecular medicine · 2024Review
- PARP-1-Associated Pathological Processes: Inhibition by Natural Polyphenols.International journal of molecular sciences · 2021Review
- Therapeutic Strategies and Biomarkers to Modulate PARP Activity for Targeted Cancer Therapy.Cancers · 2020Review
- Multi-targeted Effect of Nicotinamide Mononucleotide on Brain Bioenergetic Metabolism.Neurochemical research · 2019Review
- Targeting dePARylation selectively suppresses DNA repair-defective and PARP inhibitor-resistant malignancies.Science advances · 2019Article
- Emerging roles of eraser enzymes in the dynamic control of protein ADP-ribosylation.Nature communications · 2019Review
- Article
- Tannic acid-inspired paclitaxel nanoparticles for enhanced anticancer effects in breast cancer cells.Journal of colloid and interface science · 2019Article
- Comprehensive analysis of telomerase inhibition by gallotannin.Oncotarget · 2018Article
- Ibrutinib synergizes with poly(ADP-ribose) glycohydrolase inhibitors to induce cell death in AML cells via a BTK-independent mechanism.Oncotarget · 2016Article
- An assay to measure poly(ADP ribose) glycohydrolase (PARG) activity in cells.F1000Research · 2016Article
- Poly(ADP-ribosyl) glycohydrolase prevents the accumulation of unusual replication structures during unperturbed S phase.Molecular and cellular biology · 2015Article
- Host cell poly(ADP-ribose) glycohydrolase is crucial for Trypanosoma cruzi infection cycle.PloS one · 2013Article
- Insight into molecular and functional properties of NMNAT3 reveals new hints of NAD homeostasis within human mitochondria.PloS one · 2013Article
- Article
- Effect of silencing PARG in human colon carcinoma LoVo cells on the ability of HUVEC migration and proliferation.Cancer gene therapy · 2012Article
- Poly(ADP-ribose)glycohydrolase is an upstream regulator of Ca2+ fluxes in oxidative cell death.Cellular and molecular life sciences : CMLS · 2011Article
- The ups and downs of tannins as inhibitors of poly(ADP-ribose)glycohydrolase.Molecules (Basel, Switzerland) · 2011Review
- PARP and PARG inhibitors--new therapeutic targets in cancer treatment.Pathology oncology research : POR · 2010Review
- A specific isoform of poly(ADP-ribose) glycohydrolase is targeted to the mitochondrial matrix by a N-terminal mitochondrial targeting sequence.Experimental cell research · 2009Article
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Authors and funding
10 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeMaintenance of poly(ADP-ribose) (PAR) polymers at homoeostatic levels by PAR glycohydrolase (PARG) is central in cell functioning and survival. Yet the pharmacological relevance of PARG inhibitors is still debated. Gallotannin, a complex mixture of hydrolysable tannins from oak gall, inhibits PARG but which of its constituents is responsible for the inhibition and whether the pharmacodynamic properties are due to its antioxidant properties, has not yet been established. EXPERIMENTAL APPROACH: A structure-activity relationship study was conducted on different natural and synthetic tannins/galloyl derivatives as potential PARG inhibitors, using a novel in vitro enzymic assay. Cytotoxicity was assayed in cultured HeLa cells. KEY
resultsMono-galloyl glucose compounds were potent inhibitors of PARG, with activities similar to that of ADP-(hydroxymethyl) pyrrolidinediol, the most potent PARG inhibitor yet identified. When tested on HeLa cells exposed to the PAR polymerase (PARP)-1-activating compound 1-methyl-3-nitro-1-nitrosoguanidine (MNNG), 3-galloyl glucose weakly inhibited PAR degradation. Conversely, the more lipophilic, 3-galloyl-1,2-O-isopropylidene glucose, despite being inactive on the pure enzyme, efficiently prolonged the half-life of the polymers in intact HeLa cells. Also, PARG inhibitors, but not radical scavengers, reduced, in part, cell death caused by MNNG. CONCLUSIONS AND IMPLICATIONS: Taken together, our findings identify mono-galloyl glucose derivatives as potent PARG inhibitors, and emphasize the active function of this enzyme in cell death.
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