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==Potent, Reversible MetAP2 Inhibitors via Fragment Based Drug Discovery==
==Potent, Reversible MetAP2 Inhibitors via Fragment Based Drug Discovery==
<StructureSection load='5jfr' size='340' side='right' caption='[[5jfr]], [[Resolution|resolution]] 1.60&Aring;' scene=''>
<StructureSection load='5jfr' size='340' side='right'caption='[[5jfr]], [[Resolution|resolution]] 1.60&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[5jfr]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5JFR OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5JFR FirstGlance]. <br>
<table><tr><td colspan='2'>[[5jfr]] 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=5JFR OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5JFR FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6KP:7-FLUORO-4-(5-METHYL-3H-IMIDAZO[4,5-B]PYRIDIN-6-YL)-2,4-DIHYDROPYRAZOLO[4,3-B]INDOLE'>6KP</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=MN:MANGANESE+(II)+ION'>MN</scene></td></tr>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.6&#8491;</td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5jhu|5jhu]], [[5ji6|5ji6]]</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6KP:7-FLUORO-4-(5-METHYL-3H-IMIDAZO[4,5-B]PYRIDIN-6-YL)-2,4-DIHYDROPYRAZOLO[4,3-B]INDOLE'>6KP</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=MN:MANGANESE+(II)+ION'>MN</scene></td></tr>
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[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] </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=5jfr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5jfr OCA], [https://pdbe.org/5jfr PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5jfr RCSB], [https://www.ebi.ac.uk/pdbsum/5jfr PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5jfr ProSAT]</span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5jfr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5jfr OCA], [http://pdbe.org/5jfr PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5jfr RCSB], [http://www.ebi.ac.uk/pdbsum/5jfr PDBsum]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
[[http://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.  
[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.
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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</div>
</div>
<div class="pdbe-citations 5jfr" style="background-color:#fffaf0;"></div>
<div class="pdbe-citations 5jfr" style="background-color:#fffaf0;"></div>
==See Also==
*[[Aminopeptidase 3D structures|Aminopeptidase 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Methionyl aminopeptidase]]
[[Category: Homo sapiens]]
[[Category: Dougan, D R]]
[[Category: Large Structures]]
[[Category: Lawson, J D]]
[[Category: Dougan DR]]
[[Category: Hydrolase]]
[[Category: Lawson JD]]
[[Category: Hydrolase-hydrolase inhibitor complex]]
[[Category: Metal ion binding]]
[[Category: Peptidase]]
[[Category: Proteolysis]]
Retrieved from "https://proteopedia.org/5jfr"