Amino acid conjugation is a novel biotransformation pathway in man for a limited number of xenobiotic carboxylic acids. It involves two mitochondrial enzymatic processes: formation of a reactive xenobiotic‐CoA thioester intermediate, catalyzed by an ATP‐dependent acid:CoA synthetase (ACSM), and linkage of the activated acyl group via an acyl‐CoA:amino acid
N
‐acyltransferase (GLYAT) to the amino group of the acceptor amino acid. However, knowledge of amino acid conjugation in terms of enzyme multiplicity, protein structure, and xenobiotic substrate selectivity is not well advanced.