2v5z
From Proteopedia
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| - | [[Image:2v5z.gif|left|200px]] | + | [[Image:2v5z.gif|left|200px]] | 
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| - | '''STRUCTURE OF HUMAN MAO B IN COMPLEX WITH THE SELECTIVE INHIBITOR SAFINAMIDE''' | + |  {{Structure | 
| + | |PDB= 2v5z |SIZE=350|CAPTION= <scene name='initialview01'>2v5z</scene>, resolution 1.60Å | ||
| + | |SITE= <scene name='pdbsite=AC1:Fad+Binding+Site+For+Chain+A'>AC1</scene>, <scene name='pdbsite=AC2:Sag+Binding+Site+For+Chain+A'>AC2</scene>, <scene name='pdbsite=AC3:Fad+Binding+Site+For+Chain+B'>AC3</scene> and <scene name='pdbsite=AC4:Sag+Binding+Site+For+Chain+B'>AC4</scene> | ||
| + | |LIGAND= <scene name='pdbligand=FAD:FLAVIN-ADENINE+DINUCLEOTIDE'>FAD</scene> and <scene name='pdbligand=SAG:(S)-(+)-2-[4-(FLUOROBENZYLOXY-BENZYLAMINO)PROPIONAMIDE]'>SAG</scene> | ||
| + | |ACTIVITY= [http://en.wikipedia.org/wiki/Amine_oxidase_(flavin-containing) Amine oxidase (flavin-containing)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.4.3.4 1.4.3.4]  | ||
| + | |GENE=  | ||
| + | }} | ||
| + | |||
| + | '''STRUCTURE OF HUMAN MAO B IN COMPLEX WITH THE SELECTIVE INHIBITOR SAFINAMIDE''' | ||
| + | |||
| ==Overview== | ==Overview== | ||
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| ==About this Structure== | ==About this Structure== | ||
| - | 2V5Z is a [ | + | 2V5Z is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2V5Z OCA].  | 
| ==Reference== | ==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:[http:// | + | 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://www.ncbi.nlm.nih.gov/pubmed/17915852 17915852] | 
| [[Category: Amine oxidase (flavin-containing)]] | [[Category: Amine oxidase (flavin-containing)]] | ||
| [[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
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| [[Category: transmembrane]] | [[Category: transmembrane]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu  | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 18:43:23 2008'' | 
Revision as of 16:43, 20 March 2008
 
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 | |||||||
| , resolution 1.60Å | |||||||
|---|---|---|---|---|---|---|---|
| Sites: | , , and | ||||||
| Ligands: | and | ||||||
| Activity: | Amine oxidase (flavin-containing), with EC number 1.4.3.4 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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. 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 Mar 20 18:43:23 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
