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Combination of dual JAK/HDAC inhibitor with regorafenib synergistically reduces tumor growth, metastasis, and regorafenib-induced toxicity in colorectal cancer
BackgroundTreatment with regorafenib, a multiple-kinase inhibitor, to manage metastatic colorectal cancers (mCRCs) shows a modest improvement in...
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HDAC inhibitor ITF2357 reduces resistance of mutant-KRAS non-small cell lung cancer to pemetrexed through a HDAC2/miR-130a-3p-dependent mechanism
BackgroundHistone deacetylases (HDAC) contribute to oncogenic program, pointing to their inhibitors as a potential strategy against cancers. We,...
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High-content analysis identified synergistic drug interactions between INK128, an mTOR inhibitor, and HDAC inhibitors in a non-small cell lung cancer cell line
BackgroundThe development of drug resistance is a major cause of cancer therapy failures. To inhibit drug resistance, multiple drugs are often...
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Circular RNA circ_0000741/miR-379-5p/TRIM14 signaling axis promotes HDAC inhibitor (SAHA) tolerance in glioblastoma
BackgroundHistone deacetylase (HDAC) inhibitor-based therapeutic drug tolerance is a major obstacle to glioblastoma (GBM) treatment. Meanwhile,...
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CUDC-101 as a dual-target inhibitor of EGFR and HDAC enhances the anti-myeloma effects of bortezomib by regulating G2/M cell cycle arrest
CUDC-101, an effective and multi-target inhibitor of epidermal growth factor receptor (EGFR), histone deacetylase (HDAC), and human epidermal growth...
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HDAC Inhibitor SAHA Alleviates Pyroptosis by up-regulating miR-340 to Inhibit NEK7 Signaling in Subarachnoid Hemorrhage
Background : Subarachnoid hemorrhage (SAH) is a cerebral hemorrhagic disease with a high disability and fatality rate. Cell pyroptosis is involved in...
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Overcoming doxorubicin resistance in triple-negative breast cancer using the class I-targeting HDAC inhibitor bocodepsin/OKI-179 to promote apoptosis
BackgroundTriple-negative breast cancer (TNBC) is an aggressive breast cancer subtype with a poor prognosis. Doxorubicin is part of standard curative...
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Design, synthesis and antitumor activity evaluation of novel benzamide HDAC inhibitors
In recent years, histone deacetylase (HDAC) has become one of the hottest and most effective targets for the treatment of cancer. In this work, we...
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HAT and HDAC: Enzyme with Contradictory Action in Neurodegenerative Diseases
In view of the increasing risk of neurodegenerative diseases, epigenetics plays a fundamental role in the field of neuroscience. Several...
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CDK4/6 inhibitors, PI3K/mTOR inhibitors, and HDAC inhibitors as second-line treatments for hormone receptor-positive, HER2-negative advanced breast cancer: a network meta-analysis
BackgroundThis study sought to compare the benefits and safety of agents including Cyclin-dependent kinase 4/6 (CDK4/6) inhibitors, phosphoinositide...
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ROS Modulatory Role of HDAC Inhibitors in Cancer Cells
Histone deacetylase (HDAC) inhibitors represent a novel class of therapeutic agents for cancer treatment. These enzymes play a pivotal regulatory...
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ROS Modulatory Role of HDAC Inhibitors in Cancer Cells
Histone deacetylase (HDAC) inhibitors represent a novel class of therapeutic agents for cancer treatment. These enzymes play a pivotal regulatory...
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HDAC inhibitor chidamide synergizes with venetoclax to inhibit the growth of diffuse large B-cell lymphoma via down-regulation of MYC, BCL2, and TP53 expression
Diffuse large B-cell lymphoma (DLBCL) is an aggressive type of non-Hodgkin’s lymphoma. A total of 10%–15% of DLBCL cases are associated with...
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Effects of HDAC inhibitors on neuroblastoma SH-SY5Y cell differentiation into mature neurons via the Wnt signaling pathway
Histone deacetylase (HDAC) inhibitors affect cell homeostasis, gene expression, and cell cycle progression and promote cell terminal differentiation...
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MYC drives platinum resistant SCLC that is overcome by the dual PI3K-HDAC inhibitor fimepinostat
BackgroundSmall cell lung cancer (SCLC) is an aggressive neuroendocrine cancer with an appalling overall survival of less than 5% (Zimmerman et al. J...
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Molecular docking of curcumin and curcuminoids as human Zn+ dependent histone deacetylase (HDAC) enzyme inhibitors
Chemotherapy is one of the most well-established and effective cancer treatments available. However, non-tumor-associated damage restrict the...
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Treatment with Histone Deacetylase Inhibitor Attenuates Peripheral Inflammation-Induced Cognitive Dysfunction and Microglial Activation: The Effect of SAHA as a Peripheral HDAC Inhibitor
It has been demonstrated that peripheral inflammation induces cognitive dysfunction. Several histone deacetylase (HDAC) inhibitors ameliorate...
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D1R-5-HT2AR Uncoupling Reduces Depressive Behaviours via HDAC Signalling
Dopamine and serotonin signalling are associated with major depressive disorder, which is a prevalent life-threatening illness worldwide. Numerous...
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Evaluation of 1,10-phenanthroline-based hydroxamate derivative as dual histone deacetylases/ribonucleotide reductase inhibitor with antitumor activities
BackgroundAberrant expression of histone deacetylases (HDACs) and ribonucleotide reductase (RR) enzymes are commonly observed in various cancers....
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4-Hexylresorcinol as Histone Deacetylase Inhibitor
This chapter investigates the role of 4-hexylresorcinol (4HR) as a histone deacetylase inhibitor (HDACi) specifically targeting Class I and IIa HDACs...