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

Which of the following business challenge poses the greatest threat to your company?
Building a sustainable pipeline of products
Attracting a skilled workforce
Obtaining/maintaining adequate financing
Regulatory compliance
Building a sustainable pipeline of products
Attracting a skilled workforce
Obtaining/maintaining adequate financing
Regulatory compliance
View Results
Eric Langer Outsourcing Outlook Eric LangerBiopharma Outsourcing Activities Update
Cynthia Challener, PhD Ingredients Insider Cynthia Challener, PhDAppropriate Process Design Critical for Commercial Manufacture of Highly Potent APIs
Jill Wechsler Regulatory Watch Jill Wechsler FDA and Manufacturers Seek a More Secure Drug Supply Chain
Sean Milmo European Regulatory WatchSean MilmoQuality by Design?Bridging the Gap between Concept and Implementation
Report: Pfizer Makes $101 Billion Offer to AstraZeneca
Medicare Payment Data Raises Questions About Drug Costs
FDA Wants You!
A New Strategy to Tackle Antibiotic Resistance
Drug-Diagnostic Development Stymied by Payer Concerns
Source: Pharmaceutical Technology,
Click here