1r5h

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[[Image:1r5h.jpg|left|200px]]
[[Image:1r5h.jpg|left|200px]]
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{{Structure
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|PDB= 1r5h |SIZE=350|CAPTION= <scene name='initialview01'>1r5h</scene>, resolution 2.40&Aring;
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The line below this paragraph, containing "STRUCTURE_1r5h", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=AO2:N&#39;-(2S,3R)-3-AMINO-4-CYCLOHEXYL-2-HYDROXY-BUTANO-N-(4-METHYLPHENYL)HYDRAZIDE'>AO2</scene>, <scene name='pdbligand=MN:MANGANESE+(II)+ION'>MN</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|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>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_1r5h| PDB=1r5h | SCENE= }}
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|RELATEDENTRY=[[1r58|1R58]], [[1r5g|1R5G]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1r5h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1r5h OCA], [http://www.ebi.ac.uk/pdbsum/1r5h PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1r5h RCSB]</span>
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}}
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'''Crystal Structure of MetAP2 complexed with A320282'''
'''Crystal Structure of MetAP2 complexed with A320282'''
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[[Category: Wang, J.]]
[[Category: Wang, J.]]
[[Category: Yang, F.]]
[[Category: Yang, F.]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 07:06:17 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:23:32 2008''
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Revision as of 04:06, 3 May 2008

Image:1r5h.jpg

Template:STRUCTURE 1r5h

Crystal Structure of MetAP2 complexed with A320282


Overview

Substituted 3-amino-2-hydroxyamides and related hydroxyamides and acylhydrazines were identified as inhibitors of human methionine aminopeptidase-2 (MetAP2). Examination of substituents through parallel synthesis and iterative structure-based design allowed the identification of potent inhibitors with good selectivity against MetAP1. Diacylhydrazine 3t (A-357300) was identified as an analogue displaying inhibition of methionine processing and cellular proliferation in human microvascular endothelial cells (HMVEC).

About this Structure

1R5H is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2., Sheppard GS, Wang J, Kawai M, BaMaung NY, Craig RA, Erickson SA, Lynch L, Patel J, Yang F, Searle XB, Lou P, Park C, Kim KH, Henkin J, Lesniewski R, Bioorg Med Chem Lett. 2004 Feb 23;14(4):865-8. PMID:15012983 Page seeded by OCA on Sat May 3 07:06:17 2008

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