2p98

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[[Image:2p98.jpg|left|200px]]
[[Image:2p98.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2p98 |SIZE=350|CAPTION= <scene name='initialview01'>2p98</scene>, resolution 1.700&Aring;
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The line below this paragraph, containing "STRUCTURE_2p98", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=MN:MANGANESE+(II)+ION'>MN</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=YE7:IMIDAZO[2,1-A]ISOQUINOLINE-2-CARBOHYDRAZIDE'>YE7</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[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] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= map ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=562 Escherichia coli])
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-->
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|DOMAIN=
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{{STRUCTURE_2p98| PDB=2p98 | SCENE= }}
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|RELATEDENTRY=[[2gtx|2GTX]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2p98 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2p98 OCA], [http://www.ebi.ac.uk/pdbsum/2p98 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2p98 RCSB]</span>
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}}
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'''E. coli methionine aminopeptidase monometalated with inhibitor YE7'''
'''E. coli methionine aminopeptidase monometalated with inhibitor YE7'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Ye, Q.]]
[[Category: Ye, Q.]]
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[[Category: enzyme-inhibitor complex]]
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[[Category: Enzyme-inhibitor complex]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: metalloenzyme]]
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[[Category: Metalloenzyme]]
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[[Category: mn(ii)-form]]
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[[Category: Monometalated]]
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[[Category: monometalated]]
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[[Category: Mononuclear]]
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[[Category: mononuclear]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 12:39:08 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:32:44 2008''
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Revision as of 09:39, 4 May 2008

Image:2p98.jpg

Template:STRUCTURE 2p98

E. coli methionine aminopeptidase monometalated with inhibitor YE7


Overview

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 Structure

2P98 is a Single protein structure of sequence from Escherichia coli. Full crystallographic information is available from OCA.

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:17948983 Page seeded by OCA on Sun May 4 12:39:08 2008

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OCA

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