Chromatin modifications as targets for new anticancer drugs.
Chromatin proteins undergo diverse posttranslational modifications, esp. acetylation and methylation, that contribute to the control of transcriptional processes. The result of these modifications in its various states is called the histone code. This review presents an overview of those modifications of chromatin proteins that affect the side chains of lysines and arginines and define variations of the chromatin acetylome and methylome. The relevant enzymes are presented and the feasibility to influence their activity by inhibition or activation is discussed. The manipulation of these enzymes is an exciting strategy towards an increased understanding of their role in the functionality of a cell. Additionally, this may lead to new approaches for the treatment of diseases that are based on a dysregulation of transcription, especially cancer.
Schäfer
Stefan
S
Institute of Pharmaceutical Sciences, University of Freiburg, Freiburg, Germany.
Jung
Manfred
M
D000107:Acetylation; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002843:Chromatin / Q000235:genetics / Q000378:metabolism*; D006657:Histones / Q000378:metabolism*; D006801:Humans; D011499:Protein Processing, Post-Translational / Q000187:drug effects*
D000970:Antineoplastic Agents; D002843:Chromatin; D006657:Histones