1boa

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[[Image:1boa.gif|left|200px]]
[[Image:1boa.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1boa |SIZE=350|CAPTION= <scene name='initialview01'>1boa</scene>, resolution 1.8&Aring;
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The line below this paragraph, containing "STRUCTURE_1boa", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=BND:Fumagillin+480+Forms+A+Covalent+Bond+w.+HIS+231'>BND</scene> and <scene name='pdbsite=CO2:Dicobalt+Active+Site'>CO2</scene>
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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=CO:COBALT+(II)+ION'>CO</scene>, <scene name='pdbligand=FUG:FUMAGILLIN'>FUG</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=
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-->
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|DOMAIN=
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{{STRUCTURE_1boa| PDB=1boa | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1boa FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1boa OCA], [http://www.ebi.ac.uk/pdbsum/1boa PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1boa RCSB]</span>
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}}
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'''HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH ANGIOGENESIS INHIBITOR FUMAGILLIN'''
'''HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH ANGIOGENESIS INHIBITOR FUMAGILLIN'''
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[[Category: Liu, S.]]
[[Category: Liu, S.]]
[[Category: Widom, J.]]
[[Category: Widom, J.]]
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[[Category: angiogenesis inhibitor]]
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[[Category: Angiogenesis inhibitor]]
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[[Category: fumagillin]]
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[[Category: Fumagillin]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: methionine aminopeptidase]]
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[[Category: Methionine aminopeptidase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 11:45:43 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 19:04:57 2008''
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Revision as of 08:45, 2 May 2008

Template:STRUCTURE 1boa

HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH ANGIOGENESIS INHIBITOR FUMAGILLIN


Overview

The fungal metabolite fumagillin suppresses the formation of new blood vessels, and a fumagillin analog is currently in clinical trials as an anticancer agent. The molecular target of fumagillin is methionine aminopeptidase-2 (MetAP-2). A 1.8 A resolution crystal structure of free and inhibited human MetAP-2 shows a covalent bond formed between a reactive epoxide of fumagillin and histidine-231 in the active site of MetAP-2. Extensive hydrophobic and water-mediated polar interactions with other parts of fumagillin provide additional affinity. Fumagillin-based drugs inhibit MetAP-2 but not MetAP-1, and the three-dimensional structure also indicates the likely determinants of this specificity. The structural basis for fumagillin's potency and specificity forms the starting point for structure-based drug design.

About this Structure

1BOA is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structure of human methionine aminopeptidase-2 complexed with fumagillin., Liu S, Widom J, Kemp CW, Crews CM, Clardy J, Science. 1998 Nov 13;282(5392):1324-7. PMID:9812898 Page seeded by OCA on Fri May 2 11:45:43 2008

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