1boa: Difference between revisions

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[[Image:1boa.gif|left|200px]]
{{Seed}}
[[Image:1boa.png|left|200px]]


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{{STRUCTURE_1boa|  PDB=1boa  |  SCENE=  }}  
{{STRUCTURE_1boa|  PDB=1boa  |  SCENE=  }}  


'''HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH ANGIOGENESIS INHIBITOR FUMAGILLIN'''
===HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH ANGIOGENESIS INHIBITOR FUMAGILLIN===




==Overview==
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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.
The line below this paragraph, {{ABSTRACT_PUBMED_9812898}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 9812898 is the PubMed ID number.
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{{ABSTRACT_PUBMED_9812898}}


==About this Structure==
==About this Structure==
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[[Category: Hydrolase]]
[[Category: Hydrolase]]
[[Category: Methionine aminopeptidase]]
[[Category: Methionine aminopeptidase]]
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