1r5h
From Proteopedia
(Difference between revisions)
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== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[1r5h]] 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=1R5H OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1R5H FirstGlance]. <br> | <table><tr><td colspan='2'>[[1r5h]] 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=1R5H OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1R5H FirstGlance]. <br> | ||
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=AO2:N-(2S,3R)-3-AMINO-4-CYCLOHEXYL-2-HYDROXY-BUTANO-N-(4-METHYLPHENYL)HYDRAZIDE'>AO2</scene>, <scene name='pdbligand=MN:MANGANESE+(II)+ION'>MN</scene | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.4Å</td></tr> |
| - | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=AO2:N-(2S,3R)-3-AMINO-4-CYCLOHEXYL-2-HYDROXY-BUTANO-N-(4-METHYLPHENYL)HYDRAZIDE'>AO2</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=1r5h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1r5h OCA], [https://pdbe.org/1r5h PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1r5h RCSB], [https://www.ebi.ac.uk/pdbsum/1r5h PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1r5h ProSAT]</span></td></tr> | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1r5h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1r5h OCA], [https://pdbe.org/1r5h PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1r5h RCSB], [https://www.ebi.ac.uk/pdbsum/1r5h PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1r5h ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
| - | + | [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. | |
== Evolutionary Conservation == | == Evolutionary Conservation == | ||
[[Image:Consurf_key_small.gif|200px|right]] | [[Image:Consurf_key_small.gif|200px|right]] | ||
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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=1r5h ConSurf]. | </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=1r5h ConSurf]. | ||
<div style="clear:both"></div> | <div style="clear:both"></div> | ||
| - | <div style="background-color:#fffaf0;"> | ||
| - | == Publication Abstract from PubMed == | ||
| - | 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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| - | 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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| - | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| - | </div> | ||
| - | <div class="pdbe-citations 1r5h" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
*[[Aminopeptidase 3D structures|Aminopeptidase 3D structures]] | *[[Aminopeptidase 3D structures|Aminopeptidase 3D structures]] | ||
| - | == References == | ||
| - | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | + | [[Category: BaMaung NY]] | |
| - | [[Category: BaMaung | + | [[Category: Craig RA]] |
| - | [[Category: Craig | + | [[Category: Erickson SA]] |
| - | [[Category: Erickson | + | [[Category: Henkin J]] |
| - | [[Category: Henkin | + | [[Category: Kawai M]] |
| - | [[Category: Kawai | + | [[Category: Kim KH]] |
| - | [[Category: Kim | + | [[Category: Lesniewski R]] |
| - | [[Category: Lesniewski | + | [[Category: Lou P]] |
| - | [[Category: Lou | + | [[Category: Lynch L]] |
| - | [[Category: Lynch | + | [[Category: Park C]] |
| - | [[Category: Park | + | [[Category: Patel J]] |
| - | [[Category: Patel | + | [[Category: Searle XB]] |
| - | [[Category: Searle | + | [[Category: Sheppard GS]] |
| - | [[Category: Sheppard | + | [[Category: Wang J]] |
| - | [[Category: Wang | + | [[Category: Yang F]] |
| - | [[Category: Yang | + | |
| - | + | ||
Revision as of 06:09, 17 April 2024
Crystal Structure of MetAP2 complexed with A320282
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Categories: Homo sapiens | Large Structures | BaMaung NY | Craig RA | Erickson SA | Henkin J | Kawai M | Kim KH | Lesniewski R | Lou P | Lynch L | Park C | Patel J | Searle XB | Sheppard GS | Wang J | Yang F
