The Search for Potent, Small‐Molecule HDACIs in Cancer Treatment: A Decade After Vorinostat
@article{Zagni2017TheSF, title={The Search for Potent, Small‐Molecule HDACIs in Cancer Treatment: A Decade After Vorinostat}, author={Chiara Zagni and Giuseppe Floresta and G. Monciino and A. Rescifina}, journal={Medicinal Research Reviews}, year={2017}, volume={37} }
Histone deacetylases (HDACs) play a crucial role in the remodeling of chromatin, and are involved in the epigenetic regulation of gene expression. In the last decade, inhibition of HDACs came out as a target for specific epigenetic changes associated with cancer and other diseases. Until now, more than 20 HDAC inhibitors (HDACIs) have entered clinical studies, and some of them (e.g., vorinostat, romidepsin) have been approved for the treatment of cutaneous T‐cell lymphoma. This review provides… Expand
Topics from this paper
47 Citations
Chimeric HDAC inhibitors: Comprehensive review on the HDAC‐based strategies developed to combat cancer
- Medicine
- Medicinal research reviews
- 2018
- 40
Discovery of class I histone deacetylase inhibitors based on romidpesin with promising selectivity for cancer cells.
- Chemistry, Medicine
- Future medicinal chemistry
- 2019
- 1
The Development Process: from SAHA to Hydroxamate HDAC Inhibitors with Branched CAP Region and Linear Linker
- Chemistry, Medicine
- Chemistry & biodiversity
- 2019
- 5
Structure-Based Inhibitor Discovery of Class I Histone Deacetylases (HDACs)
- Biology, Medicine
- International journal of molecular sciences
- 2020
- PDF
Development of a Bestatin-SAHA Hybrid with Dual Inhibitory Activity against APN and HDAC
- Chemistry, Medicine
- Molecules
- 2020
- PDF
Histone deacetylase (HDAC) inhibitors in cancer: a patent review (2017-present)
- Chemistry, Medicine
- Expert opinion on therapeutic patents
- 2020
- 12
Decreased DHRS2 expression is associated with HDACi resistance and poor prognosis in ovarian cancer
- Biology, Medicine
- Epigenetics
- 2019
- 1
Discovery of meta-sulfamoyl N-hydroxybenzamides as HDAC8 selective inhibitors.
- Chemistry, Medicine
- European journal of medicinal chemistry
- 2018
- 10
Development of a versatile DNMT and HDAC inhibitor C02S modulating multiple cancer hallmarks for breast cancer therapy.
- Chemistry, Medicine
- Bioorganic chemistry
- 2019
- 14
Discovery of a Novel Hybrid of Vorinostat and Riluzole as a Potent Antitumor Agent
- Chemistry, Medicine
- Frontiers in Cell and Developmental Biology
- 2020
- 1
References
SHOWING 1-10 OF 205 REFERENCES
Selective class IIa HDAC inhibitors: myth or reality
- Medicine, Biology
- Cellular and Molecular Life Sciences
- 2014
- 27
Histone deacetylase inhibitors in the treatment of cancer: overview and perspectives.
- Biology, Medicine
- Future medicinal chemistry
- 2012
- 130
Emerging approaches for histone deacetylase inhibitor drug discovery
- Biology, Medicine
- Expert opinion on drug discovery
- 2015
- 53
Development of the pan-DAC inhibitor panobinostat (LBH589): successes and challenges.
- Medicine
- Cancer letters
- 2009
- 304
Design of novel histone deacetylase inhibitors.
- Chemistry, Medicine
- Bioorganic & medicinal chemistry letters
- 2007
- 41
Histone Deacetylase Inhibitors in Clinical Studies as Templates for New Anticancer Agents
- Biology, Medicine
- Molecules
- 2015
- 433
- PDF
Inside HDACs with more selective HDAC inhibitors.
- Chemistry, Medicine
- European journal of medicinal chemistry
- 2016
- 118
Selective inhibitors of zinc-dependent histone deacetylases. Therapeutic targets relevant to cancer.
- Biology, Medicine
- Current pharmaceutical design
- 2015
- 7
Anticancer activities of histone deacetylase inhibitors
- Biology, Medicine
- Nature Reviews Drug Discovery
- 2006
- 2,544
- PDF
Histone deacetylase inhibitors: a review on class-I specific inhibition.
- Medicine
- Mini reviews in medicinal chemistry
- 2015
- 15