2p99: Difference between revisions
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[[Image:2p99.jpg|left|200px]] | [[Image:2p99.jpg|left|200px]] | ||
'''E. coli methionine aminopeptidase monometalated with inhibitor YE6''' | {{Structure | ||
|PDB= 2p99 |SIZE=350|CAPTION= <scene name='initialview01'>2p99</scene>, resolution 1.800Å | |||
|SITE= | |||
|LIGAND= <scene name='pdbligand=MN:MANGANESE+(II)+ION'>MN</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene> and <scene name='pdbligand=YE6:[5-(2-CHLOROPHENYL)-2-FUROYL]DIAZENE'>YE6</scene> | |||
|ACTIVITY= [http://en.wikipedia.org/wiki/Methionyl_aminopeptidase Methionyl aminopeptidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.11.18 3.4.11.18] | |||
|GENE= map ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=562 Escherichia coli]) | |||
}} | |||
'''E. coli methionine aminopeptidase monometalated with inhibitor YE6''' | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
2P99 is a [ | 2P99 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2P99 OCA]. | ||
==Reference== | ==Reference== | ||
Inhibition of monometalated methionine aminopeptidase: inhibitor discovery and crystallographic analysis., Huang M, Xie SX, Ma ZQ, Huang QQ, Nan FJ, Ye QZ, J Med Chem. 2007 Nov 15;50(23):5735-42. Epub 2007 Oct 19. PMID:[http:// | Inhibition of monometalated methionine aminopeptidase: inhibitor discovery and crystallographic analysis., Huang M, Xie SX, Ma ZQ, Huang QQ, Nan FJ, Ye QZ, J Med Chem. 2007 Nov 15;50(23):5735-42. Epub 2007 Oct 19. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17948983 17948983] | ||
[[Category: Escherichia coli]] | [[Category: Escherichia coli]] | ||
[[Category: Methionyl aminopeptidase]] | [[Category: Methionyl aminopeptidase]] | ||
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[[Category: mononuclear]] | [[Category: mononuclear]] | ||
''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 18:10:24 2008'' | ||
Revision as of 19:10, 20 March 2008
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| , resolution 1.800Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , and | ||||||
| Gene: | map (Escherichia coli) | ||||||
| Activity: | Methionyl aminopeptidase, with EC number 3.4.11.18 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
E. coli methionine aminopeptidase monometalated with inhibitor YE6
OverviewOverview
Two divalent metal ions are commonly seen in the active-site cavity of methionine aminopeptidase, and at least one of the metal ions is directly involved in catalysis. Although ample structural and functional information is available for dimetalated enzyme, methionine aminopeptidase likely functions as a monometalated enzyme under physiological conditions. Information on structure, as well as catalysis and inhibition, of the monometalated enzyme is lacking. By improving conditions of high-throughput screening, we identified a unique inhibitor with specificity toward the monometalated enzyme. Kinetic characterization indicates a mutual exclusivity in binding between the inhibitor and the second metal ion at the active site. This is confirmed by X-ray structure, and this inhibitor coordinates with the first metal ion and occupies the space normally occupied by the second metal ion. Kinetic and structural analyses of the inhibition by this and other inhibitors provide insight in designing effective inhibitors of methionine aminopeptidase.
About this StructureAbout this Structure
2P99 is a Single protein structure of sequence from Escherichia coli. Full crystallographic information is available from OCA.
ReferenceReference
Inhibition of monometalated methionine aminopeptidase: inhibitor discovery and crystallographic analysis., Huang M, Xie SX, Ma ZQ, Huang QQ, Nan FJ, Ye QZ, J Med Chem. 2007 Nov 15;50(23):5735-42. Epub 2007 Oct 19. PMID:17948983
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