Chemical biology of lysine demethylases.

摘要: Abnormal levels of DNA methylation and/or histone modifications are observed in patients with a wide variety chronic diseases. Methylation lysines within tails is key modification that contributes to increased gene expression or repression depending on the specific residue and degree methylation, which turn controlled by interplay lysine methyl transferases demethylases. Drugs target these other enzymes controlling chromatin can modulate clusters genes, potentially offering higher therapeutic efficacy than classical agents acting downstream biochemical pathways susceptible degeneracy. Lysine demethylases, first discovered 2004, subject increasing interest as targets. This review provides an overview recent findings implicating demethylases range areas including oncology, immunoinflammation, metabolic disorders, neuroscience, virology regenerative medicine, together summary advances structural biology small molecule inhibitor discovery, supporting tractability protein family for development selective druglike inhibitors.