8fec

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Current revision (14:05, 18 October 2023) (edit) (undo)
 
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'''Unreleased structure'''
 
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The entry 8fec is ON HOLD until Paper Publication
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==Structure of J-PKAc chimera complexed with Aplithianine derivative==
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<StructureSection load='8fec' size='340' side='right'caption='[[8fec]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
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Authors: Du, L., Wilson, B.A.P., Li, N., Martinez Fiesco, J.A., Dalilian, M., Wang, D., Smith, E.A., Wamiru, A., Goncharova, E.I., Zhang, P., O''Keefe, B.R.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[8fec]] 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=8FEC OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8FEC FirstGlance]. <br>
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Description: Structure of J-PKAc chimera complexed with Aplithianine derivative
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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]] 2.7&#8491;</td></tr>
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[[Category: Unreleased Structures]]
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene>, <scene name='pdbligand=XU0:6-[(6P)-6-(4-bromo-1-methyl-1H-imidazol-5-yl)-2,3-dihydro-4H-1,4-thiazin-4-yl]-7H-purine'>XU0</scene></td></tr>
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[[Category: Martinez Fiesco, J.A]]
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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=8fec FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8fec OCA], [https://pdbe.org/8fec PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8fec RCSB], [https://www.ebi.ac.uk/pdbsum/8fec PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8fec ProSAT]</span></td></tr>
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[[Category: Zhang, P]]
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</table>
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[[Category: Wang, D]]
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== Function ==
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[[Category: Dalilian, M]]
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[https://www.uniprot.org/uniprot/KAPCA_HUMAN KAPCA_HUMAN] Phosphorylates a large number of substrates in the cytoplasm and the nucleus. Regulates the abundance of compartmentalized pools of its regulatory subunits through phosphorylation of PJA2 which binds and ubiquitinates these subunits, leading to their subsequent proteolysis. Phosphorylates CDC25B, ABL1, NFKB1, CLDN3, PSMC5/RPT6, PJA2, RYR2, RORA, TRPC1 and VASP. RORA is activated by phosphorylation. Required for glucose-mediated adipogenic differentiation increase and osteogenic differentiation inhibition from osteoblasts. Involved in the regulation of platelets in response to thrombin and collagen; maintains circulating platelets in a resting state by phosphorylating proteins in numerous platelet inhibitory pathways when in complex with NF-kappa-B (NFKB1 and NFKB2) and I-kappa-B-alpha (NFKBIA), but thrombin and collagen disrupt these complexes and free active PRKACA stimulates platelets and leads to platelet aggregation by phosphorylating VASP. Prevents the antiproliferative and anti-invasive effects of alpha-difluoromethylornithine in breast cancer cells when activated. RYR2 channel activity is potentiated by phosphorylation in presence of luminal Ca(2+), leading to reduced amplitude and increased frequency of store overload-induced Ca(2+) release (SOICR) characterized by an increased rate of Ca(2+) release and propagation velocity of spontaneous Ca(2+) waves, despite reduced wave amplitude and resting cytosolic Ca(2+). TRPC1 activation by phosphorylation promotes Ca(2+) influx, essential for the increase in permeability induced by thrombin in confluent endothelial monolayers. PSMC5/RPT6 activation by phosphorylation stimulates proteasome. Regulates negatively tight junction (TJs) in ovarian cancer cells via CLDN3 phosphorylation. NFKB1 phosphorylation promotes NF-kappa-B p50-p50 DNA binding. Involved in embryonic development by down-regulating the Hedgehog (Hh) signaling pathway that determines embryo pattern formation and morphogenesis. Isoform 2 phosphorylates and activates ABL1 in sperm flagellum to promote spermatozoa capacitation. Prevents meiosis resumption in prophase-arrested oocytes via CDC25B inactivation by phosphorylation. May also regulate rapid eye movement (REM) sleep in the pedunculopontine tegmental (PPT). Phosphorylates APOBEC3G and AICDA.<ref>PMID:15016832</ref> <ref>PMID:15642694</ref> <ref>PMID:15905176</ref> <ref>PMID:17565987</ref> <ref>PMID:17693412</ref> <ref>PMID:17333334</ref> <ref>PMID:20356841</ref> <ref>PMID:19949837</ref> <ref>PMID:21514275</ref> <ref>PMID:21812984</ref> <ref>PMID:21423175</ref> [https://www.uniprot.org/uniprot/DNJB1_HUMAN DNJB1_HUMAN] Interacts with HSP70 and can stimulate its ATPase activity. Stimulates the association between HSC70 and HIP.
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[[Category: Goncharova, E.I]]
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== References ==
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[[Category: Wamiru, A]]
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<references/>
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[[Category: Wilson, B.A.P]]
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__TOC__
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[[Category: Du, L]]
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</StructureSection>
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[[Category: O''Keefe, B.R]]
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[[Category: Homo sapiens]]
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[[Category: Li, N]]
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[[Category: Large Structures]]
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[[Category: Smith, E.A]]
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[[Category: Dalilian M]]
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[[Category: Du L]]
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[[Category: Goncharova EI]]
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[[Category: Li N]]
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[[Category: Martinez Fiesco JA]]
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[[Category: O'Keefe BR]]
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[[Category: Smith EA]]
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[[Category: Wamiru A]]
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[[Category: Wang D]]
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[[Category: Wilson BAP]]
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[[Category: Zhang P]]

Current revision

Structure of J-PKAc chimera complexed with Aplithianine derivative

PDB ID 8fec

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