1r58

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[[Image:1r58.png|left|200px]]
 
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{{STRUCTURE_1r58| PDB=1r58 | SCENE= }}
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==Crystal Structure of MetAP2 complexed with A357300==
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<StructureSection load='1r58' size='340' side='right'caption='[[1r58]], [[Resolution|resolution]] 1.90&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[1r58]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1R58 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1R58 FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.9&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=AO5:N-((2S,3R)-3-AMINO-2-HYDROXY-5-(ISOPROPYLSULFANYL)PENTANOYL)-N-3-CHLOROBENZOYL+HYDRAZIDE'>AO5</scene>, <scene name='pdbligand=MN:MANGANESE+(II)+ION'>MN</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1r58 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1r58 OCA], [https://pdbe.org/1r58 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1r58 RCSB], [https://www.ebi.ac.uk/pdbsum/1r58 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1r58 ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/MAP2_HUMAN MAP2_HUMAN] Cotranslationally removes the N-terminal methionine from nascent proteins. The N-terminal methionine is often cleaved when the second residue in the primary sequence is small and uncharged (Met-Ala-, Cys, Gly, Pro, Ser, Thr, or Val). The catalytic activity of human METAP2 toward Met-Val peptides is consistently two orders of magnitude higher than that of METAP1, suggesting that it is responsible for processing proteins containing N-terminal Met-Val and Met-Thr sequences in vivo. Protects eukaryotic initiation factor EIF2S1 from translation-inhibiting phosphorylation by inhibitory kinases such as EIF2AK2/PKR and EIF2AK1/HCR. Plays a critical role in the regulation of protein synthesis.
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/r5/1r58_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1r58 ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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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).
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===Crystal Structure of MetAP2 complexed with A357300===
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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<ref>PMID:15012983</ref>
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{{ABSTRACT_PUBMED_15012983}}
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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==About this Structure==
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<div class="pdbe-citations 1r58" style="background-color:#fffaf0;"></div>
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[[1r58]] is a 1 chain structure of [[Aminopeptidase]] with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1R58 OCA].
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==See Also==
==See Also==
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*[[Aminopeptidase|Aminopeptidase]]
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*[[Aminopeptidase 3D structures|Aminopeptidase 3D structures]]
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== References ==
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==Reference==
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<references/>
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<ref group="xtra">PMID:015012983</ref><references group="xtra"/>
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__TOC__
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Methionyl aminopeptidase]]
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[[Category: Large Structures]]
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[[Category: BaMaung, N Y.]]
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[[Category: BaMaung NY]]
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[[Category: Craig, R A.]]
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[[Category: Craig RA]]
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[[Category: Ericken, S A.]]
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[[Category: Ericken SA]]
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[[Category: Henkin, J.]]
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[[Category: Henkin J]]
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[[Category: Kawai, M.]]
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[[Category: Kawai M]]
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[[Category: Kim, K H.]]
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[[Category: Kim KH]]
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[[Category: Lesniewski, R.]]
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[[Category: Lesniewski R]]
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[[Category: Lou, P.]]
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[[Category: Lou P]]
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[[Category: Lynch, L.]]
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[[Category: Lynch L]]
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[[Category: Park, C.]]
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[[Category: Park C]]
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[[Category: Patel, J.]]
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[[Category: Patel J]]
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[[Category: Searle, X B.]]
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[[Category: Searle XB]]
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[[Category: Sheppard, G S.]]
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[[Category: Sheppard GS]]
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[[Category: Wang, J.]]
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[[Category: Wang J]]
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[[Category: Yang, F.]]
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[[Category: Yang F]]
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[[Category: Hydrolase]]
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Current revision

Crystal Structure of MetAP2 complexed with A357300

PDB ID 1r58

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