Related Experiment Video
Updated: Jun 24, 2026
Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
Published on: August 10, 2017
Biomarkers for predicting clinical responses to HDAC inhibitors
Lindsay Stimson1, Nicholas B La Thangue
1Dept of Clinical Pharmacology, Laboratory of Cancer Biology, Oxford, United Kingdom.
Abstract:
Post-translational modifications of histone and non-histone proteins by acetylation are known to play a key role in tumourigenesis. Pharmacological manipulation of acetylation has been possible with the identification of small molecule inhibitors of histone deacetylases (HDAC), the enzymes responsible for deacetylating lysine residues. An explosion of drug discovery efforts in recent years has led to the development of an extensive group of HDAC inhibitors, many of which have been shown pre-clinically to have potent anti-tumour activity. Clinical trials using these agents are now underway, with Vorinostat (suberoylanilide hydroxamic acid) having been approved by the FDA for treating cutaneous T-cell lymphoma (CTCL) in patients with progressive, persistent or recurrent disease. This review discusses how biomarkers are being identified and used to expand our knowledge of the mechanisms by which HDAC inhibitors exhibit their anti-cancer effects. In the longer term, biomarkers will provide a means towards achieving patient stratification in tumour types that will respond favourably to HDAC inhibitors.
Insights
Histone deacetylase (HDAC) inhibitors show potent anti-tumor activity and are being investigated in clinical trials. Biomarkers are crucial for understanding their mechanisms and stratifying patients for effective cancer treatment.
Area of Science:
- Oncology
- Biochemistry
- Pharmacology
Background:
- Acetylation of histone and non-histone proteins is critical in tumor development.
- Histone deacetylases (HDAC) regulate acetylation, making them targets for cancer therapy.
- Numerous HDAC inhibitors have demonstrated significant preclinical anti-cancer effects.
Purpose of the Study:
- To review the identification and application of biomarkers in understanding HDAC inhibitor mechanisms.
- To explore the role of biomarkers in patient stratification for HDAC inhibitor therapy.
Main Methods:
- Literature review of HDAC inhibitors and biomarker research.
- Analysis of preclinical and clinical data on HDAC inhibitor efficacy.
- Discussion of emerging biomarker strategies in oncology.
Main Results:
- Vorinostat (suberoylanilide hydroxamic acid) is FDA-approved for cutaneous T-cell lymphoma.
- HDAC inhibitors exhibit potent anti-tumor activity, supported by extensive drug discovery efforts.
- Biomarkers are actively being identified to elucidate anti-cancer mechanisms of HDAC inhibitors.
Conclusions:
- Biomarkers are essential for advancing the understanding of how HDAC inhibitors combat cancer.
- Future application of biomarkers will enable personalized treatment strategies, improving patient outcomes.
More Related Videos
09:11Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
11:06Genome-wide Analysis of HDAC Inhibitor-mediated Modulation of microRNAs and mRNAs in B Cells Induced to Undergo Class-switch DNA Recombination and Plasma Cell Differentiation
Published on: September 20, 2017
