L-arginine:glycine amidinotransferase (AGAT) is the first enzyme in creatine biosynthesis. The activity of this enzyme is tightly regulated in vivo to maintain normal creatine metabolism. Since the enzyme activity appears to be compromised in medical conditions, such as heart failure, chronic kidney disease, or stroke, it is a tempting target for upregulation in conditions with low creatine levels. Our new paper published few days ago in Current Topics In Nutraceutical Research provides an update on specific nutraceuticals that are reported to modulate AGAT activity and discusses possible implications of targeting this enzyme in experimental and clinical nutrition. Several promising nutritional agents (e.g. creatine, norvaline, cysteine) have been identified that modulate AGAT activity and the resultant cellular bioenergetics; read more about it this review paper which is freely available.