Acetylation is an important covalent molecular modification. Originally identified as the method by which certain bacteria were able to deactivate anti-microbial compounds, acetylation is now also known as an important partitioning and signaling modification.

Acetyltransferases are enzymes that covalently transfer an acetyl group from a donor molecule (Acetyl CoA) to an acceptor. Acetyl CoA serves as a universal donor while the acceptor varies with the acetyltransferase. Acceptors include histones, kinases, transcription factors, receptors, neurotransmitter precursors like choline and serotonin, and anti-microbial agents like chloramphenicol and fluoroquinones. Acetylation can signal an increase or decrease in activity based on the context of the message. Frequently located at critical junctions in metabolic pathways, Acetyltransferases and their regulation have become attractive therapeutic targets to treat everything from insomnia to cancer.