1r5h
From Proteopedia
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| , resolution 2.40Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | and | ||||||
| Activity: | Methionyl aminopeptidase, with EC number 3.4.11.18 | ||||||
| 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 23 13:25:54 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. | AO2 | MN | Hydrolase
