3oy1

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'''Unreleased structure'''
 
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The entry 3oy1 is ON HOLD until Paper Publication
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==Highly Selective c-Jun N-Terminal Kinase (JNK) 2 and 3 Inhibitors with In Vitro CNS-like Pharmacokinetic Properties==
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<StructureSection load='3oy1' size='340' side='right'caption='[[3oy1]], [[Resolution|resolution]] 1.70&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3oy1]] 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=3OY1 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3OY1 FirstGlance]. <br>
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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]] 1.7&#8491;</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=589:5-[2-(CYCLOHEXYLAMINO)PYRIDIN-4-YL]-4-NAPHTHALEN-2-YL-2-(TETRAHYDRO-2H-PYRAN-4-YL)-2,4-DIHYDRO-3H-1,2,4-TRIAZOL-3-ONE'>589</scene></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=3oy1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3oy1 OCA], [https://pdbe.org/3oy1 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3oy1 RCSB], [https://www.ebi.ac.uk/pdbsum/3oy1 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3oy1 ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/MK10_HUMAN MK10_HUMAN] Defects in MAPK10 are a cause of epileptic encephalopathy Lennox-Gastaut type (EELG) [MIM:[https://omim.org/entry/606369 606369]. Epileptic encephalopathies of the Lennox-Gastaut group are childhood epileptic disorders characterized by severe psychomotor delay and seizures. Note=A chromosomal aberration involving MAPK10 has been found in a single patient. Translocation t(Y;4)(q11.2;q21) which causes MAPK10 truncation.
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== Function ==
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[https://www.uniprot.org/uniprot/MK10_HUMAN MK10_HUMAN] Serine/threonine-protein kinase involved in various processes such as neuronal proliferation, differentiation, migration and programmed cell death. Extracellular stimuli such as proinflammatory cytokines or physical stress stimulate the stress-activated protein kinase/c-Jun N-terminal kinase (SAP/JNK) signaling pathway. In this cascade, two dual specificity kinases MAP2K4/MKK4 and MAP2K7/MKK7 phosphorylate and activate MAPK10/JNK3. In turn, MAPK10/JNK3 phosphorylates a number of transcription factors, primarily components of AP-1 such as JUN and ATF2 and thus regulates AP-1 transcriptional activity. Plays regulatory roles in the signaling pathways during neuronal apoptosis. Phosphorylates the neuronal microtubule regulator STMN2. Acts in the regulation of the beta-amyloid precursor protein/APP signaling during neuronal differentiation by phosphorylating APP. Participates also in neurite growth in spiral ganglion neurons.<ref>PMID:11718727</ref>
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Authors: Probst, G.D., Bowers, S., Sealy, J.M., Truong, A., Neitz, J., Hom, R.K., Galemmo Jr., R.A., Konradi, A.W., Sham, H.L., Quincy, D., Pan, H., Yao, N.
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==See Also==
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*[[Mitogen-activated protein kinase 3D structures|Mitogen-activated protein kinase 3D structures]]
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Description: Highly Selective c-Jun N-Terminal Kinase (JNK) 2 and 3 Inhibitors with In Vitro CNS-like Pharmacokinetic Properties
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Bowers S]]
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[[Category: Galemmo Jr RA]]
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[[Category: Hom RK]]
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[[Category: Konradi AW]]
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[[Category: Neitz J]]
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[[Category: Pan H]]
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[[Category: Probst GD]]
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[[Category: Quincy D]]
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[[Category: Sealy JM]]
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[[Category: Sham HL]]
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[[Category: Truong A]]
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[[Category: Yao N]]

Current revision

Highly Selective c-Jun N-Terminal Kinase (JNK) 2 and 3 Inhibitors with In Vitro CNS-like Pharmacokinetic Properties

PDB ID 3oy1

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