Design,Synthesis,and Biological Evaluation of a Small-Molecule Inhibitor of the Histone Acetyltransferase Gcn5

摘要

Histone proteins are basic components of the eukaryotic chromatin.'1' They contain a DNA-interacting globular domain and a more flexible N-terminal region,~[2] which is a target for several posttranslational modifications.These include the acetylation of lysine residues and the methylation of lysine and arginine residues as well as the phosphorylation of serine hydroxyl functions and the attachment of an ubiquitin group.~[3]