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Aralkylamine N-acetyltransferase (AANAT) is a key enzyme in vertebrate melatonin synthesis, catalyzing the acetylation of serotonin to N-acetylserotonin, which is subsequently converted to melatonin in the pineal gland. AANAT expression is highly regulated by the circadian clock and light exposure. It is considered the penultimate and rate-limiting enzyme in the melatonin biosynthetic pathway, thereby controlling the timing and amplitude of melatonin secretion and, consequently, circadian and seasonal physiological rhythms. Genetic regulation, protein stability (through phosphorylation and 14-3-3 protein interaction), and substrate specificity are critical to its function. AANAT is under investigation as a therapeutic target for drugs aimed at modulating sleep, mood, and circadian rhythm disorders[1][2][4].
Drugs or compounds targeting AANAT would act by inhibiting or enhancing its enzyme activity, thereby decreasing or increasing melatonin synthesis from serotonin, respectively[1].
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