Current Medicinal Chemistry

Atta-ur-Rahman, FRS
Honorary Life Fellow
Kings College
University of Cambridge


Serotonin N-acetyltransferase: Mechanism and Inhibition

Author(s): Weiping Zheng and Philip A. Cole

Affiliation: Department of Pharmacology and Molecular Sciences, the Johns Hopkins UniversitySchool of Medicine, 725 North Wolfe Street, Baltimore, MD 21205, USA


Serotonin N-acetyltransferase (arylalkylamine N-acetyltransferase, AANAT) catalyzes the rate-limiting step in the biosynthesis of the circadian hormone melatonin from serotonin. Although melatonin was identified 40 years ago, relatively little is known about its (patho)physiological roles, and a solid scientific foundation is still lacking for most therapeutic applications currently claimed for melatonin. The development of potent, specific, and cell permeable inhibitors for AANAT should constitute an important strategy to address these issues. These inhibitors are also potential therapeutics for various sleep / mood disorders. This review will focus on the efforts toward developing in vitro and in vivo AANAT inhibitors, including basic mechanistic studies on AANAT, which have played an important role in design.

Keywords: aanat, serotonin n-acefyltransferase, sleep disorder, mood disorder, aanat inhibitor

Order Reprints Order Eprints Rights & PermissionsPrintExport

Article Details

Page: [1187 - 1199]
Pages: 13
DOI: 10.2174/0929867023370013