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1gos
From Proteopedia
| 1gos, resolution 3.00Å () | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Sites: | , , and | ||||||||
| Ligands: | , | ||||||||
| Activity: | Amine oxidase (flavin-containing), with EC number 1.4.3.4 | ||||||||
| Domains: | COG1231, PRK07233 | ||||||||
| Related: | 1h8r | ||||||||
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| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||
HUMAN MONOAMINE OXIDASE B
Monoamine oxidase B (MAO B) is a mitochondrial outermembrane flavoenzyme that is a well-known target for antidepressant and neuroprotective drugs. We determined the structure of the human enzyme to 3 A resolution. The enzyme binds to the membrane through a C-terminal transmembrane helix and apolar loops located at various positions in the sequence. The electron density shows that pargyline, an analog of the clinically used MAO B inhibitor, deprenyl, binds covalently to the flavin N5 atom. The active site of MAO B consists of a 420 A(3)-hydrophobic substrate cavity interconnected to an entrance cavity of 290 A(3). The recognition site for the substrate amino group is an aromatic cage formed by Tyr 398 and Tyr 435. The structure provides a framework for probing the catalytic mechanism, understanding the differences between the B- and A-monoamine oxidase isoforms and designing specific inhibitors.
Structure of human monoamine oxidase B, a drug target for the treatment of neurological disorders., Binda C, Newton-Vinson P, Hubalek F, Edmondson DE, Mattevi A, Nat Struct Biol. 2002 Jan;9(1):22-6. PMID:11753429
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
1GOS is a 2 chains structure with sequences from Homo sapiens. Full crystallographic information is available from OCA.
Reference
- Binda C, Newton-Vinson P, Hubalek F, Edmondson DE, Mattevi A. Structure of human monoamine oxidase B, a drug target for the treatment of neurological disorders. Nat Struct Biol. 2002 Jan;9(1):22-6. PMID:11753429 doi:10.1038/nsb732
Page seeded by OCA on Mon Aug 16 05:30:05 2010
