Literature DB >> 35622308

The novel histone deacetylase inhibitor pracinostat suppresses the malignant phenotype in human glioma.

Mantao Chen1, Luyuan Zhang1, Renya Zhan2, Xiujue Zheng3.   

Abstract

INTRODUCTION: Glioma is the most common malignant brain tumor in adults. The effects of conventional treatment regimens are still limited to prolonging the survival of patients. Histone deacetylases (HDACs) are potential targets for tumor treatment. Pracinostat is a new type of HDAC inhibitor (HDACi) that has a significant antitumor effect on a variety of tumors. Thus, we aim to investigate the role of pracinostat in human glioma and explored its underlying mechanism.
METHODS: Cell viability, proliferation and apoptosis of human glioma cell lines were measured by Cell Counting kit 8 and flow cytometry. Pathway verification and protein interaction were determined by quantitative real-time polymerase chain reaction, Western blotting and immunofluorescence staining. Transwell technology was used to assess the migration and invasion of cells. Clinical significance of TIMP3, MMP9 and MMP2 in glioma was analyzed through The Cancer Genome Atlas (TCGA) database and the Genotype-Tissue Expression (GTEx) database.
RESULTS: Functionally, pracinostat not only inhibited proliferation and induced apoptosis but also inhibited migration and invasion in human glioma cell lines. Mechanistically, pracinostat increased the expression of TIMP3 and decreased the expression of MMP2, MMP9 and VEGF in human glioma cells in vitro and in vivo. In addition, pracinostat inhibited both the PI3K/Akt signaling pathway and the STAT3 pathway.
CONCLUSIONS: Our results strongly support the potential clinical use of pracinostat as a novel therapy for human glioma in the near future.
© 2022. The Author(s), under exclusive licence to Springer Nature B.V.

Entities:  

Keywords:  Glioma; HDACi; Pracinostat; TIMP3; Vascularization

Mesh:

Substances:

Year:  2022        PMID: 35622308     DOI: 10.1007/s11033-022-07559-y

Source DB:  PubMed          Journal:  Mol Biol Rep        ISSN: 0301-4851            Impact factor:   2.742


  30 in total

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Authors:  L Lloyd Morgan
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Journal:  Drug Metab Dispos       Date:  2011-08-26       Impact factor: 3.922

Review 4.  Tumor antigens in glioma.

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5.  SB939, a novel potent and orally active histone deacetylase inhibitor with high tumor exposure and efficacy in mouse models of colorectal cancer.

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6.  A Phase 2 Study of Concurrent Radiation Therapy, Temozolomide, and the Histone Deacetylase Inhibitor Valproic Acid for Patients With Glioblastoma.

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Journal:  Int J Radiat Oncol Biol Phys       Date:  2015-04-30       Impact factor: 7.038

Review 7.  Molecular targeted therapy of glioblastoma.

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9.  Phase II trial of vorinostat in recurrent glioblastoma multiforme: a north central cancer treatment group study.

Authors:  Evanthia Galanis; Kurt A Jaeckle; Matthew J Maurer; Joel M Reid; Matthew M Ames; James S Hardwick; John F Reilly; Andrey Loboda; Michael Nebozhyn; Valeria R Fantin; Victoria M Richon; Bernd Scheithauer; Caterina Giannini; Patrick J Flynn; Dennis F Moore; James Zwiebel; Jan C Buckner
Journal:  J Clin Oncol       Date:  2009-03-23       Impact factor: 44.544

10.  The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML.

Authors:  V Novotny-Diermayr; S Hart; K C Goh; A Cheong; L-C Ong; H Hentze; M K Pasha; R Jayaraman; K Ethirajulu; J M Wood
Journal:  Blood Cancer J       Date:  2012-05-04       Impact factor: 11.037

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