Molecular Classification
Enzyme, Transferase (EC 2.3), Acyltransferase family
Other Names
Acyl group transferase, Acyl-transfer enzyme, Acyl-CoA:acyltransferase, Transferase enzymes (acyl group-specific)
Disease Roles
Cancer (via dysregulated lipid metabolism)Cardiovascular disease (through cholesterol/ester metabolism)Metabolic diseases (e.g., diabetes, obesity)

Acyltransferase Overview

Acyltransferase is a general term for a class of enzymes that catalyze the transfer of acyl groups from acyl donors (commonly acyl-CoA) to acceptor molecules, such as alcohols, amines, or other biomolecules. This group encompasses diverse families essential for lipid biosynthesis (e.g., triglycerides, phospholipids, cholesterol esters), protein acylation, and the regulation of many metabolic and signaling pathways. Specific members include Glycerol-3-phosphate acyltransferases, acyl-CoA:cholesterol acyltransferases (ACAT/SOAT), and toxin-activating acyltransferases among others. Each individual acyltransferase has unique substrate specificities, tissue distributions, and disease implications.

Mechanism of Action

Inhibition of substrate acylation (for ACAT inhibitors); Disruption of lipid biosynthesis (for specific family members, e.g., GPAT/AGPAT inhibitors)

Biological Functions

Lipid metabolism
Biosynthesis of membrane lipids and other biomolecules
Signal molecule modification
Hormone synthesis
Protein modification

Disease Associations

Cancer (via dysregulated lipid metabolism)
Cardiovascular disease (through cholesterol/ester metabolism)
Metabolic diseases (e.g., diabetes, obesity)
Neurodegenerative disease (cholesterol processing)
Infection (pathogenicity, toxin activation)

Safety Considerations

  • Off-target effects due to the diversity and ubiquity of acyltransferases
  • Disruption of essential lipid metabolic processes, with consequences for cell viability and metabolic homeostasis

Interacting Drugs

Specific inhibitors for individual acyltransferase members (e.g., ACAT inhibitors)

Associated Biomarkers

Biomarker
Tissue cholesteryl ester levels (for ACAT)
No universal acyltransferase biomarker