A new review from the McCafferty lab focuses on KDM1 class lysine demethylases. These enzymes are integrally involved in many biological processes and diseases and are therefore promising therapeutic targets. The comprehensive review describes the unique structure and substrate specificity of these enzymes, as well as current efforts toward inhibitor development. It further explores the regulation of KDM1 function through the formation of multiprotein complexes. Read more here, in the special issue of Biopolymers Peptide Science.