4m7i

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==Crystal Structure of GSK6157 Bound to PERK (R587-R1092, delete A660-T867) at 2.34A Resolution==
==Crystal Structure of GSK6157 Bound to PERK (R587-R1092, delete A660-T867) at 2.34A Resolution==
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<StructureSection load='4m7i' size='340' side='right' caption='[[4m7i]], [[Resolution|resolution]] 2.34&Aring;' scene=''>
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<StructureSection load='4m7i' size='340' side='right'caption='[[4m7i]], [[Resolution|resolution]] 2.34&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4m7i]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4M7I OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4M7I FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4m7i]] 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=4M7I OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4M7I FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=27D:1-[5-(4-AMINO-7-METHYL-7H-PYRROLO[2,3-D]PYRIMIDIN-5-YL)-4-FLUORO-1H-INDOL-1-YL]-2-(6-METHYLPYRIDIN-2-YL)ETHANONE'>27D</scene></td></tr>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=27D:1-[5-(4-AMINO-7-METHYL-7H-PYRROLO[2,3-D]PYRIMIDIN-5-YL)-4-FLUORO-1H-INDOL-1-YL]-2-(6-METHYLPYRIDIN-2-YL)ETHANONE'>27D</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4g34|4g34]], [[4g31|4g31]], [[3qd2|3qd2]]</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=4m7i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4m7i OCA], [https://pdbe.org/4m7i PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4m7i RCSB], [https://www.ebi.ac.uk/pdbsum/4m7i PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4m7i ProSAT]</span></td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">EIF2AK3, PEK, PERK ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span></td></tr>
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<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=4m7i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4m7i OCA], [http://pdbe.org/4m7i PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4m7i RCSB], [http://www.ebi.ac.uk/pdbsum/4m7i PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4m7i ProSAT]</span></td></tr>
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</table>
</table>
== Disease ==
== Disease ==
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[[http://www.uniprot.org/uniprot/E2AK3_HUMAN E2AK3_HUMAN]] Wolcott-Rallison syndrome. The disease is caused by mutations affecting the gene represented in this entry.<ref>PMID:10932183</ref>
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[https://www.uniprot.org/uniprot/E2AK3_HUMAN E2AK3_HUMAN] Wolcott-Rallison syndrome. The disease is caused by mutations affecting the gene represented in this entry.<ref>PMID:10932183</ref>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/E2AK3_HUMAN E2AK3_HUMAN]] Phosphorylates the alpha subunit of eukaryotic translation-initiation factor 2 (EIF2), leading to its inactivation and thus to a rapid reduction of translational initiation and repression of global protein synthesis. Serves as a critical effector of unfolded protein response (UPR)-induced G1 growth arrest due to the loss of cyclin-D1 (CCND1) (By similarity).
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[https://www.uniprot.org/uniprot/E2AK3_HUMAN E2AK3_HUMAN] Phosphorylates the alpha subunit of eukaryotic translation-initiation factor 2 (EIF2), leading to its inactivation and thus to a rapid reduction of translational initiation and repression of global protein synthesis. Serves as a critical effector of unfolded protein response (UPR)-induced G1 growth arrest due to the loss of cyclin-D1 (CCND1) (By similarity).
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
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[[Category: Homo sapiens]]
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[[Category: Non-specific serine/threonine protein kinase]]
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[[Category: Large Structures]]
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[[Category: Axten, J M]]
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[[Category: Axten JM]]
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[[Category: Gampe, R T]]
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[[Category: Gampe RT]]
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[[Category: Catalytic domain]]
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[[Category: Deletion mutant]]
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[[Category: Transferase-transferase inhibitor complex]]
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Revision as of 11:01, 21 December 2022

Crystal Structure of GSK6157 Bound to PERK (R587-R1092, delete A660-T867) at 2.34A Resolution

PDB ID 4m7i

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