1r58: Difference between revisions
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New page: left|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'' | ||
