1boa: Difference between revisions
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[[Image:1boa.gif|left|200px]] | [[Image:1boa.gif|left|200px]] | ||
'''HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH ANGIOGENESIS INHIBITOR FUMAGILLIN''' | {{Structure | ||
|PDB= 1boa |SIZE=350|CAPTION= <scene name='initialview01'>1boa</scene>, resolution 1.8Å | |||
|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> | |||
|LIGAND= <scene name='pdbligand=CO:COBALT+(II)+ION'>CO</scene> and <scene name='pdbligand=FUG:FUMAGILLIN'>FUG</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= | |||
}} | |||
'''HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH ANGIOGENESIS INHIBITOR FUMAGILLIN''' | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
1BOA is a [ | 1BOA is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1BOA OCA]. | ||
==Reference== | ==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:[http:// | 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:[http://www.ncbi.nlm.nih.gov/pubmed/9812898 9812898] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Methionyl aminopeptidase]] | [[Category: Methionyl aminopeptidase]] | ||
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[[Category: methionine aminopeptidase]] | [[Category: methionine aminopeptidase]] | ||
''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 10:13:48 2008'' | ||
Revision as of 08:13, 20 March 2008
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| 1boa, resolution 1.8Å | |||||||||||||
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| Sites: | BND and CO2 | ||||||||||||
| Ligands: | CO and FUG | ||||||||||||
| Activity: | Methionyl aminopeptidase, with EC number 3.4.11.18 | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
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
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