1r5h

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(New page: 200px<br /> <applet load="1r5h" size="450" color="white" frame="true" align="right" spinBox="true" caption="1r5h, resolution 2.40&Aring;" /> '''Crystal Structure o...)
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[[Image:1r5h.gif|left|200px]]<br />
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[[Image:1r5h.jpg|left|200px]]<br /><applet load="1r5h" size="350" color="white" frame="true" align="right" spinBox="true"
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<applet load="1r5h" size="450" color="white" frame="true" align="right" spinBox="true"
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caption="1r5h, resolution 2.40&Aring;" />
caption="1r5h, resolution 2.40&Aring;" />
'''Crystal Structure of MetAP2 complexed with A320282'''<br />
'''Crystal Structure of MetAP2 complexed with A320282'''<br />
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==About this Structure==
==About this Structure==
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1R5H 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 AO2 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=1R5H OCA].
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1R5H 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=AO2:'>AO2</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=1R5H OCA].
==Reference==
==Reference==
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[[Category: hydrolase]]
[[Category: hydrolase]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 19:00:23 2007''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 16:47:06 2008''

Revision as of 14:47, 15 February 2008


1r5h, resolution 2.40Å

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Crystal Structure of MetAP2 complexed with A320282

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

1R5H 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

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