tailieunhanh - Báo cáo khoa học: Interactions of imidazoline ligands with the active site of purified monoamine oxidase A

The two forms of monoamine oxidase, monoamine oxidase A and mono-amine oxidase B, have been associated with imidazoline-binding sites (type 2). Imidazoline ligands saturate the imidazoline-binding sites at nanomolar concentrations, but inhibit monoamine oxidase activity only at micromolar concentrations, suggesting two different binding sites [Ozaita A, Olmos G, Boronat MA, Lizcano JM, Unzeta M & Garcı´a-Sevilla JA (1997) Br J Pharmacol121,901–912]. | ỊFEBS Journal Interactions of imidazoline ligands with the active site of purified monoamine oxidase A Tadeusz Z. E. Jones1 Laura Giurato2 Salvatore Guccione2 and Rona R. Ramsay1 1 Centre for Biomolecular Sciences University of St Andrews North Haugh St Andrews UK 2 Dipartimento di Scienze Farmaceutiche Facolta di Farmacia University degli Studi di Catania Ed. 2 Cittềá Universitaria Catania Italy Keywords docking I2 binding sites imidazoline kinetics monoamine oxidase Correspondence R. R. Ramsay Centre for Biomolecular Sciences University of St Andrews North Haugh St Andrews Fife KY16 9ST UK Fax 44 1334 463400 Tel 44 1334 463411 E-mail rrr@ Received 26 September 2006 revised 15 January 2007 accepted 17 January 2007 doi The two forms of monoamine oxidase monoamine oxidase A and monoamine oxidase B have been associated with imidazoline-binding sites type 2 . Imidazoline ligands saturate the imidazoline-binding sites at nanomolar concentrations but inhibit monoamine oxidase activity only at micromolar concentrations suggesting two different binding sites Ozaita A Olmos G Boronat MA Lizcano JM Unzeta M Garcia-Sevilla JA 1997 Br J Pharmacol 121 901-912 . When purified human monoamine oxidase A was used to examine the interaction with the active site inhibition by guana-benz 2- 2-benzofuranyl -2-imidazoline and idazoxan was competitive with kynuramine as substrate giving Ki values of 3 pM 26 pM and 125 pM respectively. Titration of monoamine oxidase A with imidazoline ligands induced spectral changes that were used to measure the binding affinities for guanabenz pM and 2- 2-benzofuranyl -2-imidazoline 49 8 pM . Only one type of binding site was detected. Agmatine a putative endogenous ligand for some imidazoline sites reduced monoamine oxidase A under anaerobic conditions indicating that it binds close to the flavin in the active site. Flexible docking studies revealed multiple orientations within the large active .

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