1b6a: Difference between revisions

Revision as of 11:07, 2 May 2008

HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH TNP-470

OverviewOverview

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 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 Page seeded by OCA on Fri May 2 11:07:32 2008

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OCA

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 [[Image:1b6a.gif|left|200px]]
- {{Structure
+<!--
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+The line below this paragraph, containing "STRUCTURE_1b6a", creates the "Structure Box" on the page.
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+You may change the PDB parameter (which sets the PDB file loaded into the applet)
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+or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-|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>
+or leave the SCENE parameter empty for the default display.
-|GENE=
+-->
-|DOMAIN=
+{{STRUCTURE_1b6a|  PDB=1b6a  |  SCENE=  }}
-|RELATEDENTRY=
-|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1b6a FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1b6a OCA], [http://www.ebi.ac.uk/pdbsum/1b6a PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1b6a RCSB]</span>
-}}
 '''HUMAN METHIONINE AMINOPEPTIDASE 2 COMPLEXED WITH TNP-470'''
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 [[Category: Clardy, J C.]]
 [[Category: Liu, S.]]
-[[Category: aminopeptidase]]
+[[Category: Aminopeptidase]]
-[[Category: angiogenesis inhibitor]]
+[[Category: Angiogenesis inhibitor]]
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May  2 11:07:32 2008''
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 18:54:27 2008''