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5o2b
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(New page: ==Crystal structure of WNK3 kinase domain in a diphosphorylated state and in a complex with the inhibitor PP-121== <StructureSection load='5o2b' size='340' side='right' caption='5o2b,...) |
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==Crystal structure of WNK3 kinase domain in a diphosphorylated state and in a complex with the inhibitor PP-121== | ==Crystal structure of WNK3 kinase domain in a diphosphorylated state and in a complex with the inhibitor PP-121== | ||
| - | <StructureSection load='5o2b' size='340' side='right' caption='[[5o2b]], [[Resolution|resolution]] 2.04Å' scene=''> | + | <StructureSection load='5o2b' size='340' side='right'caption='[[5o2b]], [[Resolution|resolution]] 2.04Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[5o2b]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5O2B OCA]. For a <b>guided tour on the structure components</b> use [ | + | <table><tr><td colspan='2'>[[5o2b]] is a 2 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=5O2B OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5O2B FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=KS1:1-CYCLOPENTYL-3-(1H-PYRROLO[2,3-B]PYRIDIN-5-YL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-AMINE'>KS1</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</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]] 2.038Å</td></tr> |
| - | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=KS1:1-CYCLOPENTYL-3-(1H-PYRROLO[2,3-B]PYRIDIN-5-YL)-1H-PYRAZOLO[3,4-D]PYRIMIDIN-4-AMINE'>KS1</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></td></tr> | |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5o2b FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5o2b OCA], [https://pdbe.org/5o2b PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5o2b RCSB], [https://www.ebi.ac.uk/pdbsum/5o2b PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5o2b ProSAT]</span></td></tr> |
</table> | </table> | ||
== Function == | == Function == | ||
| - | [ | + | [https://www.uniprot.org/uniprot/WNK3_HUMAN WNK3_HUMAN] Serine/threonine kinase which plays an important role in the regulation of electrolyte homeostasis, cell signaling, survival and proliferation. Acts as an activator and inhibitor of sodium-coupled chloride cotransporters and potassium-coupled chloride cotransporters respectively (PubMed:16275913, PubMed:16275911, PubMed:16357011). Phosphorylates WNK4. Regulates the phosphorylation of SLC12A1 and SLC12A2. Increases Ca(2+) influx mediated by TRPV5 and TRPV6 by enhancing their membrane expression level via a kinase-dependent pathway (PubMed:18768590). Inhibits the activity of KCNJ1 by decreasing its expression at the cell membrane in a non-catalytic manner.<ref>PMID:16275911</ref> <ref>PMID:16275913</ref> <ref>PMID:16357011</ref> <ref>PMID:16501604</ref> <ref>PMID:17975670</ref> <ref>PMID:18768590</ref> <ref>PMID:20525693</ref> Isoform 1, isoform 2, isoform 3 and isoform 4 stimulate the activity of SLC12A1, SLC12A2 and SLC12A3 and inhibit the activity of SLC12A4, SLC12A5, SLC12A6 and SLC12A7. According to PubMed:19470686, isoform 1 inhibits the activity of SLC12A3.<ref>PMID:19470686</ref> <ref>PMID:21613606</ref> |
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| + | ==See Also== | ||
| + | *[[Serine/threonine protein kinase 3D structures|Serine/threonine protein kinase 3D structures]] | ||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: | + | [[Category: Homo sapiens]] |
| - | [[Category: Arrowsmith | + | [[Category: Large Structures]] |
| - | [[Category: Borkowska | + | [[Category: Arrowsmith CH]] |
| - | [[Category: Bountra | + | [[Category: Borkowska O]] |
| - | [[Category: Bufton | + | [[Category: Bountra C]] |
| - | [[Category: Bullock | + | [[Category: Bufton JC]] |
| - | [[Category: Burgess-Brown | + | [[Category: Bullock A]] |
| - | [[Category: Chalk | + | [[Category: Burgess-Brown NA]] |
| - | + | [[Category: Chalk R]] | |
| - | [[Category: Edwards | + | [[Category: Edwards AM]] |
| - | [[Category: Newman | + | [[Category: Newman JA]] |
| - | [[Category: Pinkas | + | [[Category: Pinkas DM]] |
| - | [[Category: | + | [[Category: Von Delft F]] |
| - | + | ||
| - | + | ||
Current revision
Crystal structure of WNK3 kinase domain in a diphosphorylated state and in a complex with the inhibitor PP-121
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Categories: Homo sapiens | Large Structures | Arrowsmith CH | Borkowska O | Bountra C | Bufton JC | Bullock A | Burgess-Brown NA | Chalk R | Edwards AM | Newman JA | Pinkas DM | Von Delft F
