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4wnp

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==Structure of ULK1 bound to a potent inhibitor==
==Structure of ULK1 bound to a potent inhibitor==
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<StructureSection load='4wnp' size='340' side='right' caption='[[4wnp]], [[Resolution|resolution]] 1.88&Aring;' scene=''>
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<StructureSection load='4wnp' size='340' side='right'caption='[[4wnp]], [[Resolution|resolution]] 1.88&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4wnp]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4WNP OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4WNP FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4wnp]] is a 4 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=4WNP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4WNP 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=3RJ:N~2~-(1H-BENZIMIDAZOL-6-YL)-N~4~-(5-CYCLOBUTYL-1H-PYRAZOL-3-YL)QUINAZOLINE-2,4-DIAMINE'>3RJ</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene></td></tr>
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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]] 1.88&#8491;</td></tr>
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<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></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=3RJ:N~2~-(1H-BENZIMIDAZOL-6-YL)-N~4~-(5-CYCLOBUTYL-1H-PYRAZOL-3-YL)QUINAZOLINE-2,4-DIAMINE'>3RJ</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4wno|4wno]]</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=4wnp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4wnp OCA], [https://pdbe.org/4wnp PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4wnp RCSB], [https://www.ebi.ac.uk/pdbsum/4wnp PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4wnp ProSAT]</span></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=4wnp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4wnp OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4wnp RCSB], [http://www.ebi.ac.uk/pdbsum/4wnp PDBsum]</span></td></tr>
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</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/ULK1_HUMAN ULK1_HUMAN]] Serine/threonine-protein kinase involved in autophagy in response to starvation. Acts upstream of phosphatidylinositol 3-kinase PIK3C3 to regulate the formation of autophagophores, the precursors of autophagosomes. Part of regulatory feedback loops in autophagy: acts both as a downstream effector and negative regulator of mammalian target of rapamycin complex 1 (mTORC1) via interaction with RPTOR. Activated via phosphorylation by AMPK and also acts as a regulator of AMPK by mediating phosphorylation of AMPK subunits PRKAA1, PRKAB2 and PRKAG1, leading to negatively regulate AMPK activity. May phosphorylate ATG13/KIAA0652 and RPTOR; however such data need additional evidences. Plays a role early in neuronal differentiation and is required for granule cell axon formation.<ref>PMID:18936157</ref> <ref>PMID:21460634</ref> <ref>PMID:21795849</ref>
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[https://www.uniprot.org/uniprot/ULK1_HUMAN ULK1_HUMAN] Serine/threonine-protein kinase involved in autophagy in response to starvation. Acts upstream of phosphatidylinositol 3-kinase PIK3C3 to regulate the formation of autophagophores, the precursors of autophagosomes. Part of regulatory feedback loops in autophagy: acts both as a downstream effector and negative regulator of mammalian target of rapamycin complex 1 (mTORC1) via interaction with RPTOR. Activated via phosphorylation by AMPK and also acts as a regulator of AMPK by mediating phosphorylation of AMPK subunits PRKAA1, PRKAB2 and PRKAG1, leading to negatively regulate AMPK activity. May phosphorylate ATG13/KIAA0652 and RPTOR; however such data need additional evidences. Plays a role early in neuronal differentiation and is required for granule cell axon formation.<ref>PMID:18936157</ref> <ref>PMID:21460634</ref> <ref>PMID:21795849</ref>
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
</div>
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<div class="pdbe-citations 4wnp" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Serine/threonine protein kinase 3D structures|Serine/threonine protein kinase 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Non-specific serine/threonine protein kinase]]
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[[Category: Homo sapiens]]
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[[Category: Lazarus, M B]]
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[[Category: Large Structures]]
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[[Category: Novotny, C J]]
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[[Category: Lazarus MB]]
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[[Category: Shokat, K M]]
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[[Category: Novotny CJ]]
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[[Category: Autophagy]]
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[[Category: Shokat KM]]
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[[Category: Inhibitor]]
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[[Category: Kinase]]
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Current revision

Structure of ULK1 bound to a potent inhibitor

PDB ID 4wnp

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