BioCentury
ARTICLE | Cover Story

Hitting histone demethylases

August 9, 2012 7:00 AM UTC

A team from GlaxoSmithKline plc and the Structural Genomics Consortium has identified the first selective and potent histone demethylase inhibitor and shown it dampens the macrophage inflammatory response.1 The pharma now is exploring the therapeutic applications of the inhibitor in autoimmune and inflammatory diseases.

Histone methyltransferases add methyl groups to histone lysine residues, which can then be removed by histone demethylases. These two enzyme classes work in concert to regulate gene transcription...