Available technologies
Modulators of Class IIa HDACs
Team
Life Science
Industry
Healthcare
Sector
Therapeutic Programs
Histone deacetylases (HDACs), also known as lysine deacetylases, are enzymes that mediate the removal of acetyl groups from numerous acetylated proteins (including histones). In contrast to the more ubiquitously expressed Class I HDACs, which have been explored as targets for anti-cancer therapies, Class IIa HDACs have more tissue-restricted expression, significantly weaker histone deacetylation activity in the nucleus, and appear to drive pro-inflammatory responses in macrophages.
The Fairlie Research Group at The University of Queensland (UQ) has exploited structural differences between Class I and IIa HDACs to develop two generations of new compounds that are potent and selective inhibitors of class IIa HDACs.
In vivo proof of concept data has been generated in a rat model of collagen induced arthritis, with potential application in many chronic inflammatory diseases.
Key features
- New potent and selective inhibitors of class IIa HDAC enzymes
- No induction of cellular histone H4 acetylation, unlike most inhibitors of HDACs
- Potential for modulating class IIa HDAC functions in vivo with fewer cytotoxic side effects than other HDAC inhibitors.
