Aktywny doustnie, silny i selektywny inhibitor deacetylazy histonowej HDAC1/2/3/11 o skuteczności przeciwnowotworowej u myszy in vivo.
MGCD0103 (Mocetinostat) jest aktywnym doustnie, silnym i selektywnym inhibitorem deacetylazy histonowej (HDAC) (IC50: klasa I HDAC1/2/3 = 0,15/0,29/1,66 μM, klasa IV HDAC11 = 0.59 μM, HDAC4/5/7/8 >10 μM), który skutecznie hamuje komórkową aktywność HDAC (IC50 = 450 nM; Du145, HCT15, HCT116), powodując zwiększoną acetylację histonów H3 i H4, ale nie tubuliny. MGCD0103 podawany codziennie doustnie (60-120 mg/kg) jest skuteczny przeciwko wzrostowi guza A549 i H1437 u myszy in vivo.
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BioMed research international, 2020, 4705615-4705615 (2020-08-11)
The use of histone deacetylase (HDAC) inhibitor is a novel therapeutic strategy for cardiovascular disease. Studies have shown that many HDAC inhibitors have the ability to reduce the aortic remodeling in various animal models. We hypothesized that the HDAC inhibitor
Molecular cancer therapeutics, 7(4), 759-768 (2008-04-17)
Nonselective inhibitors of human histone deacetylases (HDAC) are known to have antitumor activity in mice in vivo, and several of them are under clinical investigation. The first of these, Vorinostat (SAHA), has been approved for treatment of cutaneous T-cell lymphoma.
European review for medical and pharmacological sciences, 25(9), 3396-3396 (2021-05-19)
The article "Mocetinostat suppresses epidural fibrosis following laminectomy by inhibiting myofibroblast activation and increasing apoptosis, by W.-J. Wu, J. Wang, J. Liang, Q. Zhou, Y. Liang, published in Eur Rev Med Pharmacol Sci 2020; 24 (8): 4467-4475-DOI: 10.26355/eurrev_202004_21029-PMID: 32373984" has
European review for medical and pharmacological sciences, 24(8), 4467-4475 (2020-05-07)
To investigate the effect and mechanism of mocetinostat on diminishing epidural fibrosis. Dysregulated wound repair usually occurs after injury or surgery and is featured by excessive scar tissue contributed by fibrosis. Increasing researches demonstrated that histone acetylation, an epigenetic alteration
Background: Liver cancer is a common cause of cancer-related death all over the world. MGCD0103, a histone deacetylase inhibitor, exerts antitumor effect on various cancers. However, its role in liver cancer remains unclear. Methods: The effect of MGCD0103 on HepG2
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