PMID:15498552
| Citation |
Wilmot, CM, Saysell, CG, Blessington, A, Conn, DA, Kurtis, CR, McPherson, MJ, Knowles, PF and Phillips, SE (2004) Medical implications from the crystal structure of a copper-containing amine oxidase complexed with the antidepressant drug tranylcypromine. FEBS Lett. 576:301-5 |
|---|---|
| Abstract |
The X-ray crystal structure of the copper-containing quinoprotein amine oxidase from E. coli has been determined in complex with the antidepressant drug tranylcypromine to 2.4 A resolution. The drug is a racemic mix of two enantiomers, but only one is seen bound to the enzyme. The other enantiomer is not acting as a substrate for the enzyme as no catalytic activity was detected when the enzyme was initially exposed to the drug. The inhibition of human copper amine oxidases could be a source of side-effects in its use as an antidepressant to inhibit the flavin-containing monoamine oxidases in the brain. |
| Links |
PubMed Online version:10.1016/j.febslet.2004.09.031 |
| Keywords |
Amine Oxidase (Copper-Containing)/chemistry; Amine Oxidase (Copper-Containing)/metabolism; Antidepressive Agents/chemistry; Antidepressive Agents/metabolism; Binding Sites; Crystallography, X-Ray/methods; Escherichia coli/enzymology; Models, Molecular; Tranylcypromine/chemistry; Tranylcypromine/metabolism |
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