2adu
From Proteopedia
(New page: 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=" | + | |
caption="2adu, resolution 1.90Å" /> | caption="2adu, resolution 1.90Å" /> | ||
'''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 | + | 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:// | + | 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 | + | [[Category: Fisher, P W.]] |
| - | [[Category: Hansbury, M | + | [[Category: Hansbury, M J.]] |
| - | [[Category: Ho, T | + | [[Category: Ho, T F.]] |
| - | [[Category: Hofmann, G | + | [[Category: Hofmann, G A.]] |
| - | [[Category: Janson, C | + | [[Category: Janson, C A.]] |
| - | [[Category: Johanson, K | + | [[Category: Johanson, K O.]] |
| - | [[Category: Johnson, R | + | [[Category: Johnson, R K.]] |
| - | [[Category: Kallander, L | + | [[Category: Kallander, L S.]] |
| - | [[Category: Kirkpatrick, R | + | [[Category: Kirkpatrick, R B.]] |
[[Category: Lu, Q.]] | [[Category: Lu, Q.]] | ||
| - | [[Category: Mattern, M | + | [[Category: Mattern, M R.]] |
| - | [[Category: Meek, T | + | [[Category: Meek, T D.]] |
| - | [[Category: Ryan, M | + | [[Category: Ryan, M D.]] |
| - | [[Category: Schulz-Pritchard, C | + | [[Category: Schulz-Pritchard, C K.]] |
| - | [[Category: Smith, W | + | [[Category: Smith, W W.]] |
[[Category: Tew, D.]] | [[Category: Tew, D.]] | ||
| - | [[Category: Thompson, S | + | [[Category: Thompson, S K.]] |
[[Category: Tomaszek, T.]] | [[Category: Tomaszek, T.]] | ||
| - | [[Category: Veber, D | + | [[Category: Veber, D F.]] |
| - | [[Category: Ward, K | + | [[Category: Ward, K W.]] |
| - | [[Category: Winkler, J | + | [[Category: Winkler, J D.]] |
[[Category: Yang, G.]] | [[Category: Yang, G.]] | ||
| - | [[Category: Zhang, G | + | [[Category: Zhang, G F.]] |
[[Category: CO]] | [[Category: CO]] | ||
[[Category: R20]] | [[Category: R20]] | ||
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[[Category: protease]] | [[Category: protease]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:26:22 2008'' |
Revision as of 14:26, 21 February 2008
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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 with and as ligands. Active as Methionyl aminopeptidase, with EC number 3.4.11.18 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
Page seeded by OCA on Thu Feb 21 16:26:22 2008
Categories: Homo sapiens | Methionyl aminopeptidase | Single protein | Chen, W. | Fisher, P W. | Hansbury, M J. | Ho, T F. | Hofmann, G A. | Janson, C A. | Johanson, K O. | Johnson, R K. | Kallander, L S. | Kirkpatrick, R B. | Lu, Q. | Mattern, M R. | Meek, T D. | Ryan, M D. | Schulz-Pritchard, C K. | Smith, W W. | Tew, D. | Thompson, S K. | Tomaszek, T. | Veber, D F. | Ward, K W. | Winkler, J D. | Yang, G. | Zhang, G F. | CO | R20 | Aminopeptidase | Hydrolase | Metal binding | Protease
