Drug targeting of acyltransferases in the Triacylglyceride and 1-O-AcylCeramide biosynthetic pathways

Abstract

Acyltransferase enzymes (EC 2.3.) are a large group of enzymes that transfer acyl groups to a large variety of substrates. This review focuses on fatty acyltransferases involved in the biosynthetic pathways of glycerolipids and sphingolipids and how these enzymes have been pharmacologically targeted in their biological context. Glycerolipids and sphingolipids, commonly treated independently in their regulation and biological functions, are put together to emphasize the parallelism in their metabolism and bioactive roles. Furthermore, a newly considered signaling molecule, 1-O-acylceramide, resulting from the acylation of ceramide by DGAT2 enzyme, is discussed. Finally, the implications of DGAT2 as a putative Ceramide AcylTransferase (CAT) enzyme, with a putative dual role in TAG and 1-O-acylceramide generation, are explored.