Format

Send to

Choose Destination
See comment in PubMed Commons below
Curr Chem Genomics. 2011;5(Suppl 1):62-71. doi: 10.2174/1875397301005010062. Epub 2011 Aug 22.

Chemical biology of lysine demethylases.

Author information

1
Structural Genomics Consortium, Oxford University, Roosevelt Drive, Oxford OX3 7DQ, UK.

Abstract

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

KEYWORDS:

Epigenetic; chromatin; histone; inhibitor.; lysine demethylase

PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for PubMed Central
    Loading ...
    Support Center