1boa
From Proteopedia
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| - | [[Image:1boa.gif|left|200px]]<br /><applet load="1boa" size=" | + | [[Image:1boa.gif|left|200px]]<br /><applet load="1boa" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1boa, resolution 1.8Å" /> | caption="1boa, resolution 1.8Å" /> | ||
'''HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH ANGIOGENESIS INHIBITOR FUMAGILLIN'''<br /> | '''HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH ANGIOGENESIS INHIBITOR FUMAGILLIN'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1BOA is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with CO and FUG as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Known structural/functional Sites: <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>. Full crystallographic information is available from [http:// | + | 1BOA is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=CO:'>CO</scene> and <scene name='pdbligand=FUG:'>FUG</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Known structural/functional Sites: <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>. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1BOA OCA]. |
==Reference== | ==Reference== | ||
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[[Category: methionine aminopeptidase]] | [[Category: methionine aminopeptidase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Feb 3 09:33:28 2008'' |
Revision as of 07:33, 3 February 2008
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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 with and as ligands. Active as Methionyl aminopeptidase, with EC number 3.4.11.18 Known structural/functional Sites: and . 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
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