Scriptaid, a novel histone deacetylase inhibitor, enhances the response of human tumor cells to radiation

Kuribayashi, Takashi; Ohara, Maki; Sora, Sakura; Kubota, Nobuo

doi:10.3892/ijmm_00000309

Cited by 11 publications

(2 citation statements)

References 24 publications

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“…This is in line with earlier published data by Jin et al [ 19 ] who showed a slightly increased radiosensitivity upon treatment of BON-1 and QGP-1 cells with CI-994. Similar results were demonstrated for several other cancer types [ 30 , 31 , 32 , 33 ]. This suggests that VPA may have a dual function; it increases both SSTR2 mRNA expression levels and uptake of [ 111 In]In-DOTATATE, and it increases radiosensitivity towards PRRT.…”

Section: Discussionsupporting

confidence: 87%

Comparing the Effect of Multiple Histone Deacetylase Inhibitors on SSTR2 Expression and [111In]In-DOTATATE Uptake in NET Cells

Klomp

Dalm

Koetsveld

et al. 2021

Cancers

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The aim of this study was to increase somatostatin type-2 receptor (SSTR2) expression on neuroendocrine tumor (NET) cells using histone deacetylase inhibitors (HDACis), potentially increasing the uptake of SSTR2-targeted radiopharmaceuticals and subsequently improving treatment efficacy of peptide receptor radionuclide therapy (PRRT). Human NET cell lines BON-1, NCI-H727, and GOT1 were treated with HDACis (i.e., CI-994, entinostat, LMK-235, mocetinostat, panobinostat, or valproic acid (VPA); entinostat and VPA were the HDACis tested in GOT1 cells) to examine SSTR2 mRNA expression levels and uptake of SSTR2-targeting radiotracer [111In]In-DOTATATE. Reversibility of the induced effects was examined after drug-withdrawal. Finally, the effect of VPA on radiosensitivity was investigated. A strong stimulatory effect in BON-1, NCI-H727, and GOT1 cells was observed after HDACi treatment, both on SSTR2 mRNA expression levels and [111In]In-DOTATATE uptake. The effects of the HDACis were largely reversible over a period of seven days, demonstrating largest reductions within the first day. The reversibility profile of the induced effects suggests that proper timing of HDACi treatment is most likely essential for a beneficial outcome. In addition to increasing SSTR2 expression levels, VPA enhanced the radiosensitivity of all cell lines. In conclusion, HDACi treatment increased SSTR2 expression, and radiosensitivity was also enhanced upon VPA treatment.

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Section: Discussionsupporting

confidence: 87%

Comparing the Effect of Multiple Histone Deacetylase Inhibitors on SSTR2 Expression and [111In]In-DOTATATE Uptake in NET Cells

Klomp

Dalm

Koetsveld

et al. 2021

Cancers

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“…The efficacy of Scriptaid in augmenting the radiosensitivity of SQ-20B human laryngeal squamous cell carcinoma cells through the inhibition of DNA damage repair has been demonstrated [144]. In an endeavor to enhance HDAC inhibition and metabolic stability, Professor Gyoonhee Han synthesized A1659 [145].…”

Section: Clinical Trialsmentioning

confidence: 99%

Targeting histone deacetylases in head and neck squamous cell carcinoma: molecular mechanisms and therapeutic targets

Xu,

Hou,

et al. 2024

J Transl Med

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The onerous health and economic burden associated with head and neck squamous cell carcinoma (HNSCC) is a global predicament. Despite the advent of novel surgical techniques and therapeutic protocols, there is an incessant need for efficacious diagnostic and therapeutic targets to monitor the invasion, metastasis and recurrence of HNSCC due to its substantial morbidity and mortality. The differential expression patterns of histone deacetylases (HDACs), a group of enzymes responsible for modifying histones and regulating gene expression, have been demonstrated in neoplastic tissues. However, there is limited knowledge regarding the role of HDACs in HNSCC. Consequently, this review aims to summarize the existing research findings and explore the potential association between HDACs and HNSCC, offering fresh perspectives on therapeutic approaches targeting HDACs that could potentially enhance the efficacy of HNSCC treatment. Additionally, the Cancer Genome Atlas (TCGA) dataset, CPTAC, HPA, OmicShare, GeneMANIA and STRING databases are utilized to provide supplementary evidence on the differential expression of HDACs, their prognostic significance and predicting functions in HNSCC patients. Graphical Abstract

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Histone acetyltransferases and deacetylases: molecular and clinical implications to gastrointestinal carcinogenesis

Sun

Zhou

Zheng

et al. 2012

ABBS

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Histone acetyltransferases and deacetylases are two groups of enzymes whose opposing activities govern the dynamic levels of reversible acetylation on specific lysine residues of histones and many other proteins. Gastrointestinal (GI) carcinogenesis is a major cause of morbidity and mortality worldwide. In addition to genetic and environmental factors, the role of epigenetic abnormalities such as aberrant histone acetylation has been recognized to be pivotal in regulating benign tumorigenesis and eventual malignant transformation. Here we provide an overview of histone acetylation, list the major groups of histone acetyltransferases and deacetylases, and cover in relatively more details the recent studies that suggest the links of these enzymes to GI carcinogenesis. As potential novel therapeutics for GI and other cancers, histone deacetylase inhibitors are also discussed.

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Scriptaid, a novel histone deacetylase inhibitor, enhances the response of human tumor cells to radiation

Cited by 11 publications

References 24 publications

Comparing the Effect of Multiple Histone Deacetylase Inhibitors on SSTR2 Expression and [111In]In-DOTATATE Uptake in NET Cells

Comparing the Effect of Multiple Histone Deacetylase Inhibitors on SSTR2 Expression and [111In]In-DOTATATE Uptake in NET Cells

Targeting histone deacetylases in head and neck squamous cell carcinoma: molecular mechanisms and therapeutic targets

Histone acetyltransferases and deacetylases: molecular and clinical implications to gastrointestinal carcinogenesis

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