Isoform-selective HDAC inhibitors

Selective C4-modified SAHA analogs inhibit HDAC6 and HDAC8 enzymes for targeted therapeutic applications.

Technology Summary

Histone deacetylase (HDAC) proteins are key players in cancer progression and have emerged recently as targets for anti-cancer drugs. WSU researchers have synthesized a variety of small molecule HDAC inhibitors and evaluated their potencies. This technology involves the design, synthesis, and characterization of C4-modified suberoylanilide hydroxamic acid (SAHA) analogs that selectively inhibit histone deacetylase enzymes HDAC6 and HDAC8. These enzymes play key roles in the progression of diseases such as cancer, and selective inhibition allows for improved therapeutic efficacy with reduced side effects. 

Key Advantages

• High selectivity for HDAC6 and HDAC8 enzymes reduces off-target effects
• Detailed synthesis procedures for reproducible compound production
• Demonstrated efficacy in modulating biological activity related to cell viability
• Dual inhibitors targeting both HDAC6 and HDAC8

Market Opportunities

• Research tools for studying HDAC6/8 enzyme functions
• Pharmaceutical development of selective HDAC inhibitors
• Novel Inhibitor development and substrate identification for next generation Cancer therapeutics

Stage of Development

Pre-Clinical

Patent Status

Issued US patent 10,259,779

References & Publications

Negmeldin, et al.  2018, Europ J Med Chem, 143, 1790-1806

https://doi.org/10.1016/j.ejmech.2017.10.076