1r58
From Proteopedia
(New page: 200px<br /> <applet load="1r58" size="450" color="white" frame="true" align="right" spinBox="true" caption="1r58, resolution 1.90Å" /> '''Crystal Structure o...) |
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| - | [[Image:1r58.gif|left|200px]]<br /> | + | [[Image:1r58.gif|left|200px]]<br /><applet load="1r58" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1r58" size=" | + | |
caption="1r58, resolution 1.90Å" /> | caption="1r58, resolution 1.90Å" /> | ||
'''Crystal Structure of MetAP2 complexed with A357300'''<br /> | '''Crystal Structure of MetAP2 complexed with A357300'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Substituted 3-amino-2-hydroxyamides and related hydroxyamides and | + | Substituted 3-amino-2-hydroxyamides and related hydroxyamides and acylhydrazines were identified as inhibitors of human methionine aminopeptidase-2 (MetAP2). Examination of substituents through parallel synthesis and iterative structure-based design allowed the identification of potent inhibitors with good selectivity against MetAP1. Diacylhydrazine 3t (A-357300) was identified as an analogue displaying inhibition of methionine processing and cellular proliferation in human microvascular endothelial cells (HMVEC). |
==About this Structure== | ==About this Structure== | ||
| - | 1R58 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 MN and AO5 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:// | + | 1R58 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=MN:'>MN</scene> and <scene name='pdbligand=AO5:'>AO5</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=1R58 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Methionyl aminopeptidase]] | [[Category: Methionyl aminopeptidase]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: BaMaung, N | + | [[Category: BaMaung, N Y.]] |
| - | [[Category: Craig, R | + | [[Category: Craig, R A.]] |
| - | [[Category: Ericken, S | + | [[Category: Ericken, S A.]] |
[[Category: Henkin, J.]] | [[Category: Henkin, J.]] | ||
[[Category: Kawai, M.]] | [[Category: Kawai, M.]] | ||
| - | [[Category: Kim, K | + | [[Category: Kim, K H.]] |
[[Category: Lesniewski, R.]] | [[Category: Lesniewski, R.]] | ||
[[Category: Lou, P.]] | [[Category: Lou, P.]] | ||
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[[Category: Park, C.]] | [[Category: Park, C.]] | ||
[[Category: Patel, J.]] | [[Category: Patel, J.]] | ||
| - | [[Category: Searle, X | + | [[Category: Searle, X B.]] |
| - | [[Category: Sheppard, G | + | [[Category: Sheppard, G S.]] |
[[Category: Wang, J.]] | [[Category: Wang, J.]] | ||
[[Category: Yang, F.]] | [[Category: Yang, F.]] | ||
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[[Category: hydrolase]] | [[Category: hydrolase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:47:15 2008'' |
Revision as of 12:47, 21 February 2008
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Crystal Structure of MetAP2 complexed with A357300
Overview
Substituted 3-amino-2-hydroxyamides and related hydroxyamides and acylhydrazines were identified as inhibitors of human methionine aminopeptidase-2 (MetAP2). Examination of substituents through parallel synthesis and iterative structure-based design allowed the identification of potent inhibitors with good selectivity against MetAP1. Diacylhydrazine 3t (A-357300) was identified as an analogue displaying inhibition of methionine processing and cellular proliferation in human microvascular endothelial cells (HMVEC).
About this Structure
1R58 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
3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2., Sheppard GS, Wang J, Kawai M, BaMaung NY, Craig RA, Erickson SA, Lynch L, Patel J, Yang F, Searle XB, Lou P, Park C, Kim KH, Henkin J, Lesniewski R, Bioorg Med Chem Lett. 2004 Feb 23;14(4):865-8. PMID:15012983
Page seeded by OCA on Thu Feb 21 14:47:15 2008
Categories: Homo sapiens | Methionyl aminopeptidase | Single protein | BaMaung, N Y. | Craig, R A. | Ericken, S A. | Henkin, J. | Kawai, M. | Kim, K H. | Lesniewski, R. | Lou, P. | Lynch, L. | Park, C. | Patel, J. | Searle, X B. | Sheppard, G S. | Wang, J. | Yang, F. | AO5 | MN | Hydrolase
