Inhibition of the function of class IIa HDACs by blocking their interaction with MEF2.

ABSTRACT: Enzymes that modify the epigenetic status of cells provide attractive targets for therapy in various diseases. The therapeutic development of epigenetic modulators, however, has been largely limited to direct targeting of catalytic active site conserved across multiple members of an enzyme family, which complicates mechanistic studies and drug development. Class IIa histone deacetylases (HDACs) are a group of epigenetic enzymes that depends on interaction with Myocyte Enhancer Factor-2 (MEF2) for their recruitment to specific genomic loci. Targeting this interaction presents an alternative approach to inhibiting this class of HDACs. We have used structural and functional approaches to identify and characterize a group of small molecules that indirectly target class IIa HDACs by blocking th

SUBMITTER: Jayathilaka N 

PROVIDER: S-EPMC3384312 | biostudies-literature | 2012 Jul

REPOSITORIES: biostudies-literature