2adu: Difference between revisions

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[[Image:2adu.gif|left|200px]]<br /><applet load="2adu" size="350" color="white" frame="true" align="right" spinBox="true"
[[Image:2adu.gif|left|200px]]
caption="2adu, resolution 1.90&Aring;" />
 
'''Human Methionine Aminopeptidase Complex with 4-Aryl-1,2,3-triazole Inhibitor'''<br />
{{Structure
|PDB= 2adu |SIZE=350|CAPTION= <scene name='initialview01'>2adu</scene>, resolution 1.90&Aring;
|SITE=
|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>
|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]
|GENE= METAP2, MNPEP, P67EIF2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
}}
 
'''Human Methionine Aminopeptidase Complex with 4-Aryl-1,2,3-triazole Inhibitor'''
 


==Overview==
==Overview==
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==About this Structure==
==About this Structure==
2ADU 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> and <scene name='pdbligand=R20:'>R20</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=2ADU OCA].  
2ADU 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=2ADU OCA].  


==Reference==
==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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=16134930 16134930]
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:[http://www.ncbi.nlm.nih.gov/pubmed/16134930 16134930]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Methionyl aminopeptidase]]
[[Category: Methionyl aminopeptidase]]
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[[Category: protease]]
[[Category: protease]]


''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:26:22 2008''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 15:48:24 2008''

Revision as of 16:48, 20 March 2008

File:2adu.gif


PDB ID 2adu

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



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


OverviewOverview

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 StructureAbout this Structure

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

ReferenceReference

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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