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2v5z
From Proteopedia
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==Overview== | ==Overview== | ||
| - | Structures of human monoamine oxidase B (MAO B) in complex with safinamide | + | Structures of human monoamine oxidase B (MAO B) in complex with safinamide and two coumarin derivatives, all sharing a common benzyloxy substituent, were determined by X-ray crystallography. These compounds competitively inhibit MAO B with Ki values in the 0.1-0.5 microM range that are 30-700-fold lower than those observed with MAO A. The inhibitors bind noncovalently to MAO B, occupying both the entrance and the substrate cavities and showing a similarly oriented benzyloxy substituent. |
==About this Structure== | ==About this Structure== | ||
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==Reference== | ==Reference== | ||
| - | Structures of | + | Structures of human monoamine oxidase B complexes with selective noncovalent inhibitors: safinamide and coumarin analogs., Binda C, Wang J, Pisani L, Caccia C, Carotti A, Salvati P, Edmondson DE, Mattevi A, J Med Chem. 2007 Nov 15;50(23):5848-52. Epub 2007 Oct 4. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17915852 17915852] |
[[Category: Amine oxidase (flavin-containing)]] | [[Category: Amine oxidase (flavin-containing)]] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
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[[Category: Caccia, C.]] | [[Category: Caccia, C.]] | ||
[[Category: Carotti, A.]] | [[Category: Carotti, A.]] | ||
| - | [[Category: Edmondson, D | + | [[Category: Edmondson, D E.]] |
[[Category: Mattevi, A.]] | [[Category: Mattevi, A.]] | ||
[[Category: Pisani, L.]] | [[Category: Pisani, L.]] | ||
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[[Category: transmembrane]] | [[Category: transmembrane]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:53:22 2008'' |
Revision as of 16:53, 21 February 2008
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STRUCTURE OF HUMAN MAO B IN COMPLEX WITH THE SELECTIVE INHIBITOR SAFINAMIDE
Overview
Structures of human monoamine oxidase B (MAO B) in complex with safinamide and two coumarin derivatives, all sharing a common benzyloxy substituent, were determined by X-ray crystallography. These compounds competitively inhibit MAO B with Ki values in the 0.1-0.5 microM range that are 30-700-fold lower than those observed with MAO A. The inhibitors bind noncovalently to MAO B, occupying both the entrance and the substrate cavities and showing a similarly oriented benzyloxy substituent.
About this Structure
2V5Z is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Amine oxidase (flavin-containing), with EC number 1.4.3.4 Known structural/functional Sites: , , and . Full crystallographic information is available from OCA.
Reference
Structures of human monoamine oxidase B complexes with selective noncovalent inhibitors: safinamide and coumarin analogs., Binda C, Wang J, Pisani L, Caccia C, Carotti A, Salvati P, Edmondson DE, Mattevi A, J Med Chem. 2007 Nov 15;50(23):5848-52. Epub 2007 Oct 4. PMID:17915852
Page seeded by OCA on Thu Feb 21 18:53:22 2008
Categories: Amine oxidase (flavin-containing) | Homo sapiens | Single protein | Binda, C. | Caccia, C. | Carotti, A. | Edmondson, D E. | Mattevi, A. | Pisani, L. | Salvati, P. | Wang, J. | FAD | SAG | Fad | Flavoprotein | Human mao b structure | Membrane | Mitochondrion | Neuroprotection | Oxidoreductase | Parkinson's disease | Reversible inhibitor binding | Safinamide | Transmembrane
