1b6a: Difference between revisions

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{{STRUCTURE_1b6a|  PDB=1b6a  |  SCENE=  }}  
{{STRUCTURE_1b6a|  PDB=1b6a  |  SCENE=  }}  


'''HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH TNP-470'''
===HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH TNP-470===




==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.
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==About this Structure==
==About this Structure==
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[[Category: Aminopeptidase]]
[[Category: Aminopeptidase]]
[[Category: Angiogenesis inhibitor]]
[[Category: Angiogenesis inhibitor]]
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Revision as of 18:21, 30 June 2008

File:1b6a.png

Template:STRUCTURE 1b6a

HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH TNP-470HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH TNP-470

Template:ABSTRACT PUBMED 9812898

About this StructureAbout this Structure

1B6A is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

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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