1qxw

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PDB ID 1qxw

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, resolution 1.67Å
Ligands: , and
Activity: Methionyl aminopeptidase, with EC number 3.4.11.18
Coordinates: save as pdb, mmCIF, xml



Crystal structure of Staphyloccocus aureus in complex with an aminoketone inhibitor 54135.


Overview

High-resolution crystal structures of Staphylococcus aureus methionine aminopeptidase I in complex with various keto heterocycles and aminoketones were determined, and the intermolecular ligand interactions with the enzyme are reported. The compounds are effective inhibitors of the S. aureus enzyme because of the formation of an uncleavable tetrahedral intermediate upon binding. The electron densities unequivocally show the enzyme-catalyzed transition-state analogue mimicking that for amide bond hydrolysis of substrates.

About this Structure

1QXW is a Single protein structure of sequence from Staphylococcus aureus. Full crystallographic information is available from OCA.

Reference

Crystal structures of Staphylococcusaureus methionine aminopeptidase complexed with keto heterocycle and aminoketone inhibitors reveal the formation of a tetrahedral intermediate., Douangamath A, Dale GE, D'Arcy A, Almstetter M, Eckl R, Frutos-Hoener A, Henkel B, Illgen K, Nerdinger S, Schulz H, Mac Sweeney A, Thormann M, Treml A, Pierau S, Wadman S, Oefner C, J Med Chem. 2004 Mar 11;47(6):1325-8. PMID:14998322

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