2adu: Difference between revisions

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New page: left|200px<br /> <applet load="2adu" size="450" color="white" frame="true" align="right" spinBox="true" caption="2adu, resolution 1.90Å" /> '''Human Methionine Am...
 
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[[Image:2adu.gif|left|200px]]<br />
[[Image:2adu.gif|left|200px]]<br /><applet load="2adu" size="350" color="white" frame="true" align="right" spinBox="true"  
<applet load="2adu" size="450" color="white" frame="true" align="right" spinBox="true"  
caption="2adu, resolution 1.90&Aring;" />
caption="2adu, resolution 1.90&Aring;" />
'''Human Methionine Aminopeptidase Complex with 4-Aryl-1,2,3-triazole Inhibitor'''<br />
'''Human Methionine Aminopeptidase Complex with 4-Aryl-1,2,3-triazole Inhibitor'''<br />


==Overview==
==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.
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==
==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 CO and R20 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://ispc.weizmann.ac.il/oca-bin/ocashort?id=2ADU OCA].  
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].  


==Reference==
==Reference==
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Chen, W.]]
[[Category: Chen, W.]]
[[Category: Fisher, P.W.]]
[[Category: Fisher, P W.]]
[[Category: Hansbury, M.J.]]
[[Category: Hansbury, M J.]]
[[Category: Ho, T.F.]]
[[Category: Ho, T F.]]
[[Category: Hofmann, G.A.]]
[[Category: Hofmann, G A.]]
[[Category: Janson, C.A.]]
[[Category: Janson, C A.]]
[[Category: Johanson, K.O.]]
[[Category: Johanson, K O.]]
[[Category: Johnson, R.K.]]
[[Category: Johnson, R K.]]
[[Category: Kallander, L.S.]]
[[Category: Kallander, L S.]]
[[Category: Kirkpatrick, R.B.]]
[[Category: Kirkpatrick, R B.]]
[[Category: Lu, Q.]]
[[Category: Lu, Q.]]
[[Category: Mattern, M.R.]]
[[Category: Mattern, M R.]]
[[Category: Meek, T.D.]]
[[Category: Meek, T D.]]
[[Category: Ryan, M.D.]]
[[Category: Ryan, M D.]]
[[Category: Schulz-Pritchard, C.K.]]
[[Category: Schulz-Pritchard, C K.]]
[[Category: Smith, W.W.]]
[[Category: Smith, W W.]]
[[Category: Tew, D.]]
[[Category: Tew, D.]]
[[Category: Thompson, S.K.]]
[[Category: Thompson, S K.]]
[[Category: Tomaszek, T.]]
[[Category: Tomaszek, T.]]
[[Category: Veber, D.F.]]
[[Category: Veber, D F.]]
[[Category: Ward, K.W.]]
[[Category: Ward, K W.]]
[[Category: Winkler, J.D.]]
[[Category: Winkler, J D.]]
[[Category: Yang, G.]]
[[Category: Yang, G.]]
[[Category: Zhang, G.F.]]
[[Category: Zhang, G F.]]
[[Category: CO]]
[[Category: CO]]
[[Category: R20]]
[[Category: R20]]
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[[Category: protease]]
[[Category: protease]]


''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 20:49:33 2007''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:26:22 2008''