1r5h

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1r5h, resolution 2.40Å

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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 with and as ligands. Active as Methionyl aminopeptidase, with EC number 3.4.11.18 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

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