BioCentury
ARTICLE | Cover Story

HDACs get complex

January 27, 2011 8:00 AM UTC

Cellzome AG has reported a chemical proteomic method for determining the selectivity of HDAC inhibitors. The approach makes it possible, for the first time, to determine the effects of an inhibitor on HDACs as components of naturally occurring protein complexes rather than as the less biologically relevant isolated enzymes.1 The company is already exploring the potential of the method to identify HDAC inhibitors that are more selective and less toxic than the array of molecules currently on the market or in the clinic.

Histone deacetylases (HDACs) are a family of enzymes that regulate gene expression by removing acetyl groups from histones. In addition, HDACs regulate a variety of other cellular processes through the deacetylation of nonhistone proteins...