1qzy

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[[Image:1qzy.jpg|left|200px]]<br /><applet load="1qzy" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1qzy.jpg|left|200px]]
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caption="1qzy, resolution 1.60&Aring;" />
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'''Human Methionine Aminopeptidase in complex with bengamide inhibitor LAF153 and cobalt'''<br />
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{{Structure
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|PDB= 1qzy |SIZE=350|CAPTION= <scene name='initialview01'>1qzy</scene>, resolution 1.60&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=CO:COBALT+(II)+ION'>CO</scene>, <scene name='pdbligand=TDE:(E)-(2R,3R,4S,5R)-3,4,5-TRIHYDROXY-2-METHOXY-8,8-DIMETHYL-NON-6-ENOIC+ACID+((3S,6R)-6-HYDROXY-2-OXO-AZEPAN-3-YL)-AMIDE'>TDE</scene> and <scene name='pdbligand=TBU:TERTIARY-BUTYL ALCOHOL'>TBU</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=
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}}
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'''Human Methionine Aminopeptidase in complex with bengamide inhibitor LAF153 and cobalt'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1QZY is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=CO:'>CO</scene>, <scene name='pdbligand=TDE:'>TDE</scene> and <scene name='pdbligand=TBU:'>TBU</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=1QZY OCA].
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1QZY is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1QZY OCA].
==Reference==
==Reference==
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Proteomics-based target identification: bengamides as a new class of methionine aminopeptidase inhibitors., Towbin H, Bair KW, DeCaprio JA, Eck MJ, Kim S, Kinder FR, Morollo A, Mueller DR, Schindler P, Song HK, van Oostrum J, Versace RW, Voshol H, Wood J, Zabludoff S, Phillips PE, J Biol Chem. 2003 Dec 26;278(52):52964-71. Epub 2003 Oct 8. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=14534293 14534293]
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Proteomics-based target identification: bengamides as a new class of methionine aminopeptidase inhibitors., Towbin H, Bair KW, DeCaprio JA, Eck MJ, Kim S, Kinder FR, Morollo A, Mueller DR, Schindler P, Song HK, van Oostrum J, Versace RW, Voshol H, Wood J, Zabludoff S, Phillips PE, J Biol Chem. 2003 Dec 26;278(52):52964-71. Epub 2003 Oct 8. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/14534293 14534293]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Methionyl aminopeptidase]]
[[Category: Methionyl aminopeptidase]]
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[[Category: hydrolase]]
[[Category: hydrolase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:45:36 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 13:44:59 2008''

Revision as of 11:45, 20 March 2008

Image:1qzy.jpg


PDB ID 1qzy

Drag the structure with the mouse to rotate
, resolution 1.60Å
Ligands: , and
Activity: Methionyl aminopeptidase, with EC number 3.4.11.18
Coordinates: save as pdb, mmCIF, xml



Human Methionine Aminopeptidase in complex with bengamide inhibitor LAF153 and cobalt


Overview

LAF389 is a synthetic analogue of bengamides, a class of marine natural products that produce inhibitory effects on tumor growth in vitro and in vivo. A proteomics-based approach has been used to identify signaling pathways affected by bengamides. LAF389 treatment of cells resulted in altered mobility of a subset of proteins on two-dimensional gel electrophoresis. Detailed analysis of one of the proteins, 14-3-3gamma, showed that bengamide treatment resulted in retention of the amino-terminal methionine, suggesting that bengamides directly or indirectly inhibited methionine aminopeptidases (MetAps). Both known MetAps are inhibited by LAF389. Short interfering RNA suppression of MetAp2 also altered amino-terminal processing of 14-3-3gamma. A high resolution structure of human MetAp2 co-crystallized with a bengamide shows that the compound binds in a manner that mimics peptide substrates. Additionally, the structure reveals that three key hydroxyl groups on the inhibitor coordinate the di-cobalt center in the enzyme active site.

About this Structure

1QZY is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Proteomics-based target identification: bengamides as a new class of methionine aminopeptidase inhibitors., Towbin H, Bair KW, DeCaprio JA, Eck MJ, Kim S, Kinder FR, Morollo A, Mueller DR, Schindler P, Song HK, van Oostrum J, Versace RW, Voshol H, Wood J, Zabludoff S, Phillips PE, J Biol Chem. 2003 Dec 26;278(52):52964-71. Epub 2003 Oct 8. PMID:14534293

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