1xnz

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[[Image:1xnz.jpg|left|200px]]<br /><applet load="1xnz" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1xnz.jpg|left|200px]]
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caption="1xnz, resolution 1.52&Aring;" />
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'''Crystal Structure of Mn(II) form of E. coli. Methionine Aminopeptidase in complex with 5-(2-chlorophenyl)furan-2-carboxylic acid'''<br />
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{{Structure
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|PDB= 1xnz |SIZE=350|CAPTION= <scene name='initialview01'>1xnz</scene>, resolution 1.52&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=MN:MANGANESE+(II)+ION'>MN</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene> and <scene name='pdbligand=FCD:5-(2-CHLOROPHENYL)FURAN-2-CARBOXYLIC ACID'>FCD</scene>
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|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]
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|GENE= map ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=562 Escherichia coli])
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}}
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'''Crystal Structure of Mn(II) form of E. coli. Methionine Aminopeptidase in complex with 5-(2-chlorophenyl)furan-2-carboxylic acid'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1XNZ is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli] with <scene name='pdbligand=MN:'>MN</scene>, <scene name='pdbligand=NA:'>NA</scene> and <scene name='pdbligand=FCD:'>FCD</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1XNZ OCA].
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1XNZ is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1XNZ OCA].
==Reference==
==Reference==
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Metalloform-selective inhibitors of escherichia coli methionine aminopeptidase and X-ray structure of a Mn(II)-form enzyme complexed with an inhibitor., Ye QZ, Xie SX, Huang M, Huang WJ, Lu JP, Ma ZQ, J Am Chem Soc. 2004 Nov 3;126(43):13940-1. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15506752 15506752]
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Metalloform-selective inhibitors of escherichia coli methionine aminopeptidase and X-ray structure of a Mn(II)-form enzyme complexed with an inhibitor., Ye QZ, Xie SX, Huang M, Huang WJ, Lu JP, Ma ZQ, J Am Chem Soc. 2004 Nov 3;126(43):13940-1. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/15506752 15506752]
[[Category: Escherichia coli]]
[[Category: Escherichia coli]]
[[Category: Methionyl aminopeptidase]]
[[Category: Methionyl aminopeptidase]]
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[[Category: structure]]
[[Category: structure]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:57:04 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 15:12:24 2008''

Revision as of 13:12, 20 March 2008

Image:1xnz.jpg


PDB ID 1xnz

Drag the structure with the mouse to rotate
, resolution 1.52Å
Ligands: , and
Gene: map (Escherichia coli)
Activity: Methionyl aminopeptidase, with EC number 3.4.11.18
Coordinates: save as pdb, mmCIF, xml



Crystal Structure of Mn(II) form of E. coli. Methionine Aminopeptidase in complex with 5-(2-chlorophenyl)furan-2-carboxylic acid


Overview

Methionine aminopeptidase (MetAP) enzymes require a divalent metal ion such as Mn(II), Fe(II), Co(II), Ni(II), or Zn(II) for its removal of the N-terminal methionine from newly synthesized proteins, but it is not certain which of these ions is most important in vivo. Metalloform-selective MetAP inhibitors could be valuable for defining which metals are physiologically relevant for MetAP activation and could serve as leads for development of new therapeutic agents. We have screened a library of 43 736 small drug-like molecules against Escherichia coli MetAP and identified two groups of potent and highly metalloform-selective inhibitors of the Co(II)-form, and of the Mn(II)-form, of this enzyme. Compound 1 is 790-fold more selective for the Co(II)-form, while compound 4 is over 640-fold more potent toward the Mn(II)-form. The X-ray structure of a di-Mn(II) form of E. coli MetAP complexed with the Mn(II)-form-selective compound 4 was obtained, and it shows that the inhibitor interacts with both Mn(II) ions through the two oxygen atoms of its free carboxylate group. The preferential coordination of the hard (oxygen) donors to Mn(II) may contribute to its superb selectivity toward the Mn(II)-form.

About this Structure

1XNZ is a Single protein structure of sequence from Escherichia coli. Full crystallographic information is available from OCA.

Reference

Metalloform-selective inhibitors of escherichia coli methionine aminopeptidase and X-ray structure of a Mn(II)-form enzyme complexed with an inhibitor., Ye QZ, Xie SX, Huang M, Huang WJ, Lu JP, Ma ZQ, J Am Chem Soc. 2004 Nov 3;126(43):13940-1. PMID:15506752

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