Aralkylamine N-acetyltransferase
In enzymology, an aralkylamine N-acetyltransferase (EC 2.3.1.87) is an enzyme that catalyzes the chemical reaction
- acetyl-CoA + a 2-arylethylamine CoA + an N-acetyl-2-arylethylamine
Thus, the two substrates of this enzyme are acetyl-CoA and 2-arylethylamine, whereas its two products are CoA and N-acetyl-2-arylethylamine.
This enzyme belongs to the family of transferases, to be specific, those acyltransferases transferring groups other than aminoacyl groups. This enzyme participates in tryptophan metabolism.
Nomenclature
The systematic name of this enzyme class is acetyl-CoA:2-arylethylamine N-acetyltransferase. Other names in common use include:
- Serotonin acetyltransferase
- Serotonin acetylase
- Arylalkylamine N-acetyltransferase
- Serotonin N-acetyltransferase
- AANAT
- Melatonin rhythm enzyme
Structural studies
As of late 2007, 6 structures have been solved for this class of enzymes, with PDB accession codes 1B6B, 1IB1, 1KUV, 1KUX, 1KUY, and 1L0C.
AANAT inhibitors
Synthetic inhibitors of the enzyme have been discovered.[1][2][3]
References
- ^ Szewczuk LM, Saldanha SA, Ganguly S, Bowers EM, Javoroncov M, Karanam B, Culhane JC, Holbert MA, Klein DC, Abagyan R, Cole PA (November 2007). "De novo Discovery of Serotonin N-acetyltransferase Inhibitors". J. Med. Chem. 50 (22): 5330–8. doi:10.1021/jm0706463. PMC 2531295. PMID 17924613. http://www.pubmedcentral.nih.gov/articlerender.fcgi?tool=pmcentrez&artid=2531295.
- ^ Ferry G, Ubeaud C, Mozo J, Péan C, Hennig P, Rodriguez M, Scoul C, Bonnaud A, Nosjean O, Galizzi JP, Delagrange P, Renard P, Volland JP, Yous S, Lesieur D, Boutin JA (January 2004). "New substrate analogues of human serotonin N-acetyltransferase produce in situ specific and potent inhibitors". Eur. J. Biochem. 271 (2): 418–28. doi:10.1046/j.1432-1033.2003.03942.x. PMID 14717709.
- ^ Zheng W, Cole PA (October 2003). "Novel bisubstrate analog inhibitors of serotonin N-acetyltransferase: the importance of being neutral". Bioorg. Chem. 31 (5): 398–411. doi:10.1016/S0045-2068(03)00081-6. PMID 12941292.
Further reading
- Voisin P, Namboodiri MA, Klein DC (1984). "Arylamine N-acetyltransferase and arylalkylamine N-acetyltransferase in the mammalian pineal gland". J. Biol. Chem. 259 (17): 10913–8. PMID 6469990.
- Fauchere JL, Boutin JA (2000). "Substrate specificity and inhibition studies of human serotonin N-acetyltransferase". J. Biol. Chem. 275 (12): 8794–805. doi:10.1074/jbc.275.12.8794. PMID 10722724.
- Khalil EM and Cole PA (1998). "A potent inhibitor of the melatonin rhythm enzyme". J. Am. Chem. Soc. 120 (24): 6195–6196. doi:10.1021/ja981365a.