7o7j
From Proteopedia
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==Crystal structure of the human HIPK3 kinase domain bound to abemaciclib== | ==Crystal structure of the human HIPK3 kinase domain bound to abemaciclib== | ||
| - | <StructureSection load='7o7j' size='340' side='right'caption='[[7o7j]]' scene=''> | + | <StructureSection load='7o7j' size='340' side='right'caption='[[7o7j]], [[Resolution|resolution]] 2.81Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7O7J OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7O7J FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[7o7j]] 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=7O7J OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7O7J FirstGlance]. <br> |
| - | </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=7o7j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7o7j OCA], [https://pdbe.org/7o7j PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7o7j RCSB], [https://www.ebi.ac.uk/pdbsum/7o7j PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7o7j ProSAT]</span></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]] 2.81Å</td></tr> |
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6ZV:N-{5-[(4-ETHYLPIPERAZIN-1-YL)METHYL]PYRIDIN-2-YL}-5-FLUORO-4-[4-FLUORO-2-METHYL-1-(PROPAN-2-YL)-1H-BENZIMIDAZOL-6-YL]PYRIMIDIN-2-AMINE'>6ZV</scene>, <scene name='pdbligand=PTR:O-PHOSPHOTYROSINE'>PTR</scene></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=7o7j FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7o7j OCA], [https://pdbe.org/7o7j PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7o7j RCSB], [https://www.ebi.ac.uk/pdbsum/7o7j PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7o7j ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/HIPK3_HUMAN HIPK3_HUMAN] Serine/threonine-protein kinase involved in transcription regulation, apoptosis and steroidogenic gene expression. Phosphorylates JUN and RUNX2. Seems to negatively regulate apoptosis by promoting FADD phosphorylation. Enhances androgen receptor-mediated transcription. May act as a transcriptional corepressor for NK homeodomain transcription factors. The phosphorylation of NR5A1 activates SF1 leading to increased steroidogenic gene expression upon cAMP signaling pathway stimulation. In osteoblasts, supports transcription activation: phosphorylates RUNX2 that synergizes with SPEN/MINT to enhance FGFR2-mediated activation of the osteocalcin FGF-responsive element (OCFRE).<ref>PMID:14766760</ref> <ref>PMID:17210646</ref> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
[[Category: Anand K]] | [[Category: Anand K]] | ||
[[Category: Geyer M]] | [[Category: Geyer M]] | ||
[[Category: Kaltheuner IH]] | [[Category: Kaltheuner IH]] | ||
Current revision
Crystal structure of the human HIPK3 kinase domain bound to abemaciclib
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