1r5h
From Proteopedia
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|PDB= 1r5h |SIZE=350|CAPTION= <scene name='initialview01'>1r5h</scene>, resolution 2.40Å | |PDB= 1r5h |SIZE=350|CAPTION= <scene name='initialview01'>1r5h</scene>, resolution 2.40Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= | + | |LIGAND= <scene name='pdbligand=AO2:N'-(2S,3R)-3-AMINO-4-CYCLOHEXYL-2-HYDROXY-BUTANO-N-(4-METHYLPHENYL)HYDRAZIDE'>AO2</scene>, <scene name='pdbligand=MN:MANGANESE+(II)+ION'>MN</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] | + | |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> |
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[1r58|1R58]], [[1r5g|1R5G]] | ||
| + | |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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[[Category: Wang, J.]] | [[Category: Wang, J.]] | ||
[[Category: Yang, F.]] | [[Category: Yang, F.]] | ||
| - | [[Category: AO2]] | ||
| - | [[Category: MN]] | ||
[[Category: hydrolase]] | [[Category: hydrolase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 23 | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:23:32 2008'' |
Revision as of 20:23, 30 March 2008
| |||||||
| , resolution 2.40Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , | ||||||
| Activity: | Methionyl aminopeptidase, with EC number 3.4.11.18 | ||||||
| Related: | 1R58, 1R5G
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
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 Sun Mar 30 23:23:32 2008
Categories: Homo sapiens | Methionyl aminopeptidase | Single protein | BaMaung, N Y. | Craig, R A. | Erickson, S A. | Henkin, J. | Kawai, M. | Kim, K H. | Lesniewski, R. | Lou, P. | Lynch, L. | Park, C. | Patel, J. | Searle, X B. | Sheppard, G S. | Wang, J. | Yang, F. | Hydrolase
