Summary:

Researchers at The Ohio State University have a novel class of small molecule inhibitors of histone deactylase designed to trigger growth arrest, differentiation, and/or apoptosis in many types of tumor cells. Our researchers have discovered that the lack of potency of known histone deacetylase inhibitors is due to a structural motif that interferes with access to the molecular target site on histones. The OSU compounds incorporate the chemical structure necessary to inhibit histone acetylation and thus to treat prostate and possibly other tumors of epithelial origin. The acetylation status of histones plays a major role in regulating gene transcription through modulation of packaging of DNA. The OSU compounds work by reactivating transcription of certain genes in neoplastic cells. Given the transcriptional regulation that results from dosing cells with these inhibitors, they may also act as preventive agents of neoplastic or hyperplastic diseases such as psoriasis.

These compounds are undergoing preclinical testing under the NIH Rapid Access to Interventional Development (RAID) program with the goal of entering into Phase 1 clinical trials within two years.

Potential Applications:

• Treatment of cancers of epithelial origin such as prostate, breast, ovary, etc
• Potential treatment for psoriasis and other diseases hallmarked by aberrant cell growth.