2adu

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|PDB= 2adu |SIZE=350|CAPTION= <scene name='initialview01'>2adu</scene>, resolution 1.90&Aring;
|PDB= 2adu |SIZE=350|CAPTION= <scene name='initialview01'>2adu</scene>, resolution 1.90&Aring;
|SITE=
|SITE=
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|LIGAND= <scene name='pdbligand=CO:COBALT+(II)+ION'>CO</scene> and <scene name='pdbligand=R20:4-(3-METHYLPHENYL)-1H-1,2,3-TRIAZOLE'>R20</scene>
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|LIGAND= <scene name='pdbligand=CO:COBALT+(II)+ION'>CO</scene>, <scene name='pdbligand=R20:4-(3-METHYLPHENYL)-1H-1,2,3-TRIAZOLE'>R20</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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|ACTIVITY= <span class='plainlinks'>[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] </span>
|GENE= METAP2, MNPEP, P67EIF2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
|GENE= METAP2, MNPEP, P67EIF2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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|DOMAIN=
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2adu FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2adu OCA], [http://www.ebi.ac.uk/pdbsum/2adu PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2adu RCSB]</span>
}}
}}
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[[Category: Yang, G.]]
[[Category: Yang, G.]]
[[Category: Zhang, G F.]]
[[Category: Zhang, G F.]]
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[[Category: CO]]
 
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[[Category: R20]]
 
[[Category: aminopeptidase]]
[[Category: aminopeptidase]]
[[Category: hydrolase]]
[[Category: hydrolase]]
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[[Category: protease]]
[[Category: protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 15:48:24 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:51:14 2008''

Revision as of 22:51, 30 March 2008

Image:2adu.gif


PDB ID 2adu

Drag the structure with the mouse to rotate
, resolution 1.90Å
Ligands: ,
Gene: METAP2, MNPEP, P67EIF2 (Homo sapiens)
Activity: Methionyl aminopeptidase, with EC number 3.4.11.18
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



Human Methionine Aminopeptidase Complex with 4-Aryl-1,2,3-triazole Inhibitor


Overview

Inhibitors of human methionine aminopeptidase type 2 (hMetAP2) are of interest as potential treatments for cancer. A new class of small molecule reversible inhibitors of hMetAP2 was discovered and optimized, the 4-aryl-1,2,3-triazoles. Compound 24, a potent inhibitor of cobalt-activated hMetAP2, also inhibits human and mouse endothelial cell growth. Using a mouse matrigel model, this reversible hMetAP2 inhibitor was also shown to inhibit angiogenesis in vivo.

About this Structure

2ADU is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo., Kallander LS, Lu Q, Chen W, Tomaszek T, Yang G, Tew D, Meek TD, Hofmann GA, Schulz-Pritchard CK, Smith WW, Janson CA, Ryan MD, Zhang GF, Johanson KO, Kirkpatrick RB, Ho TF, Fisher PW, Mattern MR, Johnson RK, Hansbury MJ, Winkler JD, Ward KW, Veber DF, Thompson SK, J Med Chem. 2005 Sep 8;48(18):5644-7. PMID:16134930

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