ArticleOncotarget2014
A novel class I HDAC inhibitor, MPT0G030, induces cell apoptosis and differentiation in human colorectal cancer cells via HDAC1/PKCδ and E-cadherin.
Article in Oncotarget, 2014. 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, 32 citations in OpenAlex.
- Pharmacological Potential of Cinnamic Acid and Derivatives: A Comprehensive Review.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Regulatory Roles of Histone Deacetylation in Metabolic Stress-Induced Expression of Caspase Recruitment Domain-Containing Protein 9 (CARD9) in Pancreatic β-Cells.International journal of molecular sciences · 2023Article
- CHD4 as an important mediator in regulating the malignant behaviors of colorectal cancer.International journal of biological sciences · 2021Article
- SIRT2 Promotes the Migration and Invasion of Gastric Cancer through RAS/ERK/JNK/MMP-9 Pathway by Increasing PEPCK1-Related Metabolism.Neoplasia (New York, N.Y.) · 2018Article
- Prognosis Analysis of Histone Deacetylases mRNA Expression in Ovarian Cancer Patients.Journal of Cancer · 2018Article
- Downregulation of SIRT2 Inhibits Invasion of Hepatocellular Carcinoma by Inhibiting Energy Metabolism.Translational oncology · 2017Article
- Down-regulation of HDAC3 inhibits growth of cholangiocarcinoma by inducing apoptosis.Oncotarget · 2017Article
- Time dependent modulation of tumor radiosensitivity by a pan HDAC inhibitor: abexinostat.Oncotarget · 2017Article
- Histone deacetylase 3 overexpression in human cholangiocarcinoma and promotion of cell growth via apoptosis inhibition.Cell death & disease · 2017Article
- Suberoylanilide hydroxamic acid increases anti-cancer effect of tumor necrosis factor-α through up-regulation of TNF receptor 1 in lung cancer cells.Oncotarget · 2017Article
- Pinin facilitated proliferation and metastasis of colorectal cancer through activating EGFR/ERK signaling pathway.Oncotarget · 2016Article
- Inhibition of histone deacetylases by trans-cinnamic acid and its antitumor effect against colon cancer xenografts in athymic mice.Molecular medicine reports · 2016Article
- AR-42 induces apoptosis in human hepatocellular carcinoma cells via HDAC5 inhibition.Oncotarget · 2016Article
- The Role of E-Cadherin in Maintaining the Barrier Function of Corneal Epithelium after Treatment with Cultured Autologous Oral Mucosa Epithelial Cell Sheet Grafts for Limbal Stem Deficiency.Journal of ophthalmology · 2016Article
- Histone modifiers and marks define heterogeneous groups of colorectal carcinomas and affect responses to HDAC inhibitors in vitro.American journal of cancer research · 2016Article
- Anticancer activity of MPT0G157, a derivative of indolylbenzenesulfonamide, inhibits tumor growth and angiogenesis.Oncotarget · 2015Article
- Article
- Molecular Mechanism of the Cell Death Induced by the Histone Deacetylase Pan Inhibitor LBH589 (Panobinostat) in Wilms Tumor Cells.PloS one · 2015Article
- Expression of CD133, E-cadherin and WWOX in colorectal cancer and related analysis.Pakistan journal of medical sciencesArticle
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Accumulation of genetic and epigenetic changes contributes to cancer development and progression. Compared with gene mutations or deletions, epigenetic changes are reversible, which alter the chromatin structure remodeling instead of changes in DNA sequence, and therefore become a promising strategy for chemotherapy. Histone deacetylases (HDACs) are a class of enzymes that responsible for the epigenetic regulation of gene expression. MPT0G030 is a potent and selective class I HDAC inhibitor which showed broad-spectrum cytotoxicity against various human cancer cell lines. in vitro fluorometric HDAC activity assay showed that MPT0G030 effectively inhibited Class I HDACs (HDAC1~3), which were overexpressed in many malignant neoplasms. Interestingly, MPT0G030 not only induced histone acetylation and tumor suppressor p21 transcription, but also redistributed E-cadherin and activated Protein Kinase C δ (PKCδ), which was linked to cell apoptosis and differentiation. Further, activation of PKCδ was demonstrated to be modulated through HDAC1. The in vivo anticancer activity of MPT0G030 and the importance of PKCδ were confirmed in the HT-29 tumor xenograft models. Taken together, those results indicate that MPT0G030, a class I HDAC inhibitor, has great potential as a new drug candidate for cancer therapy.
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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.