3da6
From Proteopedia
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<StructureSection load='3da6' size='340' side='right'caption='[[3da6]], [[Resolution|resolution]] 2.00Å' scene=''> | <StructureSection load='3da6' size='340' side='right'caption='[[3da6]], [[Resolution|resolution]] 2.00Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[3da6]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/ | + | <table><tr><td colspan='2'>[[3da6]] 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=3DA6 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3DA6 FirstGlance]. <br> |
| - | </td></tr><tr id=' | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2Å</td></tr> |
| - | <tr id=' | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=BZ9:N-[3-METHYL-4-({3-[2-(METHYLAMINO)PYRIMIDIN-4-YL]PYRIDIN-2-YL}OXY)NAPHTHALEN-1-YL]-1H-BENZIMIDAZOL-2-AMINE'>BZ9</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=3da6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3da6 OCA], [https://pdbe.org/3da6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3da6 RCSB], [https://www.ebi.ac.uk/pdbsum/3da6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3da6 ProSAT]</span></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=3da6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3da6 OCA], [https://pdbe.org/3da6 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3da6 RCSB], [https://www.ebi.ac.uk/pdbsum/3da6 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3da6 ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Disease == | == Disease == | ||
| - | + | [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. | |
== Function == | == Function == | ||
| - | + | [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> | |
== Evolutionary Conservation == | == Evolutionary Conservation == | ||
[[Image:Consurf_key_small.gif|200px|right]] | [[Image:Consurf_key_small.gif|200px|right]] | ||
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=3da6 ConSurf]. | </jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=3da6 ConSurf]. | ||
<div style="clear:both"></div> | <div style="clear:both"></div> | ||
| - | <div style="background-color:#fffaf0;"> | ||
| - | == Publication Abstract from PubMed == | ||
| - | Selective small molecule inhibitors of Tie-2 kinase are important tools for the validation of Tie-2 signaling in pathological angiogenesis. Reported herein is the optimization of a nonselective scaffold into a potent and highly selective inhibitor of Tie-2 kinase. | ||
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| - | Pyridyl-pyrimidine benzimidazole derivatives as potent, selective, and orally bioavailable inhibitors of Tie-2 kinase.,Cee VJ, Cheng AC, Romero K, Bellon S, Mohr C, Whittington DA, Bak A, Bready J, Caenepeel S, Coxon A, Deak HL, Fretland J, Gu Y, Hodous BL, Huang X, Kim JL, Lin J, Long AM, Nguyen H, Olivieri PR, Patel VF, Wang L, Zhou Y, Hughes P, Geuns-Meyer S Bioorg Med Chem Lett. 2009 Jan 15;19(2):424-7. Epub 2008 Nov 20. PMID:19062275<ref>PMID:19062275</ref> | ||
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| - | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| - | </div> | ||
| - | <div class="pdbe-citations 3da6" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
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__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: | + | [[Category: Homo sapiens]] |
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | + | [[Category: Bellon S]] | |
| - | [[Category: Bellon | + | [[Category: Bready J]] |
| - | [[Category: Bready | + | [[Category: Caenepeel S]] |
| - | [[Category: Caenepeel | + | [[Category: Cee VJ]] |
| - | [[Category: Cee | + | [[Category: Cheng AC]] |
| - | [[Category: Cheng | + | [[Category: Coxon A]] |
| - | [[Category: Coxon | + | [[Category: Deak HL]] |
| - | [[Category: Deak | + | [[Category: Geuns-Meyer S]] |
| - | [[Category: Geuns-Meyer | + | [[Category: Hodous BL]] |
| - | [[Category: Hodous | + | [[Category: Hughes P]] |
| - | [[Category: Hughes | + | [[Category: Kim JL]] |
| - | [[Category: Kim | + | [[Category: Lin J]] |
| - | [[Category: Lin | + | [[Category: Mohr C]] |
| - | [[Category: Mohr | + | [[Category: Nguyen H]] |
| - | [[Category: Nguyen | + | [[Category: Olivieri PR]] |
| - | [[Category: Olivieri | + | [[Category: Patel VF]] |
| - | [[Category: Patel | + | [[Category: Romero K]] |
| - | [[Category: Romero | + | [[Category: Wang L]] |
| - | [[Category: Wang | + | [[Category: Whittington DA]] |
| - | [[Category: Whittington | + | |
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Current revision
Crystal Structure of human JNK3 complexed with N-(3-methyl-4-(3-(2-(methylamino)pyrimidin-4-yl)pyridin-2-yloxy)naphthalen-1-yl)-1H-benzo[d]imidazol-2-amine
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Categories: Homo sapiens | Large Structures | Bellon S | Bready J | Caenepeel S | Cee VJ | Cheng AC | Coxon A | Deak HL | Geuns-Meyer S | Hodous BL | Hughes P | Kim JL | Lin J | Mohr C | Nguyen H | Olivieri PR | Patel VF | Romero K | Wang L | Whittington DA
