Developing Selective HDAC Inhibitors

Milton Brown
Anatoly Dritschilo
Mira Jung

With the emerging roles of histone deacetylase (HDAC) isoforms in tumor biology, the development of isoform selective HDAC inhibitors could be of major importance. A number of compounds including natural and synthesized have been reported to inhibit HDAC activity and most belong to hydroxamic acid class based on suberoylanilide hydroxamic acid (SAHA). SAHA is a non-selective HDAC inhibitor that has recently entered the clinical. We are presently developing isoform selective HDAC inhibitors for advancement as new prostate cancer agents and radiation sensitizing agents.