Histone Deacetylase Inhibitors

Compounds that inhibit HISTONE DEACETYLASES. This class of drugs may influence gene expression by increasing the level of acetylated HISTONES in specific CHROMATIN domains.

Also Known As:

HDAC Inhibitors; Histone Deacetylase Inhibitor; Deacetylase Inhibitor, Histone; Deacetylase Inhibitors, Histone; Inhibitor, HDAC; Inhibitor, Histone Deacetylase; Inhibitors, HDAC; Inhibitors, Histone Deacetylase; HDAC Inhibitor

Networked: 6571 relevant articles (510 outcomes, 1234 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Chemical Actions and Uses
- Pharmacologic Actions: 160
  - Molecular Mechanisms of Pharmacological Action: 24
    - Enzyme Inhibitors: 1659
      - Histone Deacetylase Inhibitors: 6571

Experts

1.	Grant, Steven: 58 articles (10/2021 - 02/2002)
2.	Atadja, Peter: 49 articles (01/2016 - 08/2003)
3.	Dent, Paul: 48 articles (01/2022 - 05/2003)
4.	Alam, Hasan B: 45 articles (01/2021 - 03/2006)
5.	Johnstone, Ricky W: 37 articles (01/2022 - 04/2002)
6.	Mai, Antonello: 32 articles (01/2022 - 05/2005)
7.	Li, Yongqing: 32 articles (01/2021 - 06/2007)
8.	Chen, Ching-Shih: 31 articles (01/2020 - 10/2004)
9.	Liu, Baoling: 30 articles (01/2021 - 06/2007)
10.	Marks, Paul A: 30 articles (04/2012 - 05/2002)

Related Diseases

1.	Neoplasms (Cancer) 11/01/2005 - "It also suggests an approach for the artificial control of transcriptional activation through the use of highly amphiphilic small molecules that would mimic the action of acetylated lysines; in view of the known association of aberrant transcription with cancer, this approach holds promise for advances in cancer etiology and treatment and represents an alternative to the approach that currently uses histone deacetylase inhibitors (some of which are in clinical trials)." 08/08/2013 - "Chimeric inhibitor 4 is further shown to be highly efficacious in cancer cell lines and significantly more efficacious than a dual-targeting strategy using discrete c-Src and HDAC inhibitors." 07/14/2011 - "3 is a potent pan-HDAC inhibitor with excellent druglike properties, is highly efficacious in in vivo tumor models (HCT-116, PC-3, A2780, MV4-11, Ramos), and has high and dose-proportional oral exposures and very good ADME, safety, and pharmaceutical properties. " 09/01/2010 - "A large number of HDAC inhibitors have been synthesized in the last few years, most being effective in vitro, inducing cancer cells differentiation or cell death. " 01/01/2019 - "In light of the increasing numbers of clinical trials involving HDAC inhibitors in human cancers, our observations strongly suggest that the BRCA1 status and tumor hypoxia should be considered as potentially important clinical parameters that may affect the therapeutic efficacy of HDAC inhibitors."
2.	Breast Neoplasms (Breast Cancer) 04/01/2012 - "Combination of pan-histone deacetylase inhibitor and autophagy inhibitor exerts superior efficacy against triple-negative human breast cancer cells." 06/01/2013 - "Taken together, these results provide novel mechanistic insight into the breast cancer subtype-dependent role of LSD1 in mediating HDAC activity and therapeutic efficacy of HDAC inhibitor." 11/01/2020 - "Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer." 01/01/2022 - "Previous studies have suggested that the feedback activation of JAK-STAT3 pathway represents a key mechanism leading to resistance to HDAC inhibitors in breast cancer, suggesting the therapeutic promise of JAK/HDAC dual inhibitors. " 01/01/2021 - "Herein, we demonstrate that histone deacetylase inhibitors (HDACi), which are in phase III clinical trials for breast cancer, epigenetically induced LIFR and activated a pro-dormancy program in breast cancer cells. "
3.	Inflammation (Inflammations) 09/07/2019 - "The diverse set of selective and non-selective HDAC inhibitors used in pre-clinical models of airway inflammation show promising results, but several challenges still need to be overcome. " 09/01/2023 - "Hence, HDAC inhibitors (HDACi) could serve as highly potent anti-inflammatory regulators in the uniform amelioration of inflammation. " 08/22/2022 - "HDACs regulate the expression of inflammatory genes, as evidenced by the potent anti-inflammatory activity of pan-HDAC inhibitors, which were implicated in several pathophysiologic states in the inflammation process. " 01/01/2019 - "HDAC inhibitors promote intestinal epithelial regeneration via autocrine TGFβ1 signalling in inflammation." 01/01/2019 - "Consequently, treatment with HDAC inhibitors may provide a new therapeutic strategy to stabilize vascular homeostasis in the context of inflammation by preventing RNase1 down-regulation in ECs.-Bedenbender, K., Scheller, N., Fischer, S., Leiting, S., Preissner, K. "
4.	Prostatic Neoplasms (Prostate Cancer) 02/15/2005 - "Given that prostate cancer is generally a multiclonal disease representing different cell lineages, it is important to develop HDAC inhibitors that will be effective against all of these cell types." 04/06/2012 - "These results, obtained with a reliable preclinical in vivo test, predict that combined therapeutic agents targeting the pathways governing DLC1 function and HDAC inhibitors may be beneficial in management of prostate cancer." 12/01/2022 - "These studies demonstrate that HDAC inhibitors reverse the radioresistance in prostate cancer through down-modulation of USF-1-mediated transactivation of target genes involved in cell proliferation and cell cycle." 01/01/2021 - "The effectiveness of HDAC inhibitors has been demonstrated by preclinical models, but not in clinical studies, probably due to the ineffectively accumulation of HDACI in prostate cancer cells. " 07/01/2013 - "In the present study, we synthesized a novel HDAC inhibitor, A248, and investigated its apoptotic activity and molecular target in the DU145 and PC3 human prostate cancer cell lines. "
5.	Lymphoma (Lymphomas) 10/01/2010 - "Histone deacetylase inhibitors, idiotype vaccination and other molecules show promising results in the lymphoma research that they are being verified in ongoing clinical trials." 01/01/2020 - "This study investigated the combined effects of MTX plus histone deacetylase inhibitors (HDACIs), which upregulate MTX polyglutamylation, in primary central nervous system lymphoma (PCNSL). " 03/01/2005 - "This study provides a mechanistic rationale for the use of HDAC inhibitors in the treatment of human t(14;18) lymphomas." 01/01/2022 - "To examine this concept, we enriched for autophagosomes from histone deacetylase inhibitor (HDACi)-sensitive U937 lymphoma cells and isogenic HDACi-resistant cells. " 10/23/2020 - "Histone deacetylase inhibitors (HDACIs) show anti-lymphoma activities and can be applied to treat DLBCL. "

Related Drugs and Biologics

1.	Histone Deacetylases (Histone Deacetylase)
2.	Vorinostat
3.	Valproic Acid (Depakote)
4.	DNA (Deoxyribonucleic Acid)
5.	Panobinostat
6.	trichostatin A (A 300)
7.	entinostat (MS 275)
8.	Histones (Histone)
9.	Methyltransferases
10.	theasinensin A

Related Therapies and Procedures

1.	Therapeutics
2.	Drug Therapy (Chemotherapy)
3.	Immunotherapy
4.	Radiotherapy
5.	Castration