Coming Down the Pike: HDAC inhibitors - Pharmaceutical Technology

Latest Issue

Latest Issue
PharmTech Europe

Coming Down the Pike: HDAC inhibitors

Pharmaceutical Technology
Volume 3, Issue 32

Finally, after years of focusing almost exclusively on kinases as targets for anticancer therapies, a new class of compound makes the jump from research laboratory to clinical development. The new kid on the block: Histone deactelyase inhibitors (HDAC inhibitors). These compounds prevent the expression of cancer-inducing genes by maintaining them in a suppressed state. Essentially, these new potential anticancer therapies take advantage of an epigenetic mechanism of controlling gene expression. That is, certain chemical modifications can suppress the expression of genes without altering the intrinsic sequence of nucleotides in the DNA code—hence the notion of epigenetic modification. Instead, these modifications—chiefly methylation or acetylation—somehow alter the structure of the chromatin in which the gene lies in such a way that a particular stretch of chromatin is tightly coiled and resistant to unwinding by transcription factors that might otherwise stimulate gene expression. If the suppressed gene contributes to carcinogenesis, then inhibiting its expression should inhibit its ability to cause cancer. HDAC inhibitors function by preventing the removal of suppressive acetyl groups from histone proteins on the chromatin. Several large pharma and biotech companies are developing HDAC inhibitors as anticancer therapies, some of which are in clinical trials.

Source: M. Paris et. al., "Histone Deacetylase Inhibitors: From Bench to Clinic," J. Med. Chem., ASAP Article, 10.1021/jm7011408, (Feb. 5, 2008), available at, accessed Feb. 14, 2008.


blog comments powered by Disqus
LCGC E-mail Newsletters

Subscribe: Click to learn more about the newsletter
| Weekly
| Monthly
| Weekly

FDASIA was signed into law two years ago. Where has the most progress been made in implementation?
Reducing drug shortages
Breakthrough designations
Protecting the supply chain
Expedited reviews of drug submissions
More stakeholder involvement
Reducing drug shortages
Breakthrough designations
Protecting the supply chain
Expedited reviews of drug submissions
More stakeholder involvement
View Results
Eric Langerr Outsourcing Outlook Eric LangerRelationship-building at Top of Mind for Clients
Cynthia Challener, PhD Ingredients Insider Cynthia ChallenerRisk Reduction Top Driver for Biopharmaceutical Raw Material Development
Jill Wechsler Regulatory Watch Jill Wechsler Changes and Challenges for Generic Drugs
Faiz Kermaini Industry Insider Faiz KermainiNo Signs of a Slowdown in Mergers
Ebola Outbreak Raises Ethical Issues
Better Comms Means a Fitter Future for Pharma, Part 2: Realizing the Benefits of Unified Communications
Better Comms Means a Fitter Future for Pharma, Part 1: Challenges and Changes
Sandoz Wins Biosimilar Filing Race
NIH Translational Research Partnership Yields Promising Therapy
Source: Pharmaceutical Technology,
Click here