3rtp: Difference between revisions
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== | ==Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration== | ||
[[http://www.uniprot.org/uniprot/MK10_HUMAN MK10_HUMAN | <StructureSection load='3rtp' size='340' side='right'caption='[[3rtp]], [[Resolution|resolution]] 2.40Å' scene=''> | ||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[3rtp]] 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=3RTP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3RTP FirstGlance]. <br> | |||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.4Å</td></tr> | |||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=34I:N-[4-CYANO-3-(1H-1,2,4-TRIAZOL-5-YL)THIOPHEN-2-YL]-2-(2-OXO-3,4-DIHYDROQUINOLIN-1(2H)-YL)ACETAMIDE'>34I</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=3rtp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rtp OCA], [https://pdbe.org/3rtp PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3rtp RCSB], [https://www.ebi.ac.uk/pdbsum/3rtp PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3rtp ProSAT]</span></td></tr> | |||
</table> | |||
== 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 == | |||
[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> | |||
== | ==See Also== | ||
[[ | *[[Mitogen-activated protein kinase 3D structures|Mitogen-activated protein kinase 3D structures]] | ||
== References == | |||
<references/> | |||
__TOC__ | |||
</StructureSection> | |||
== | |||
<references | |||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: | [[Category: Large Structures]] | ||
[[Category: Artis | [[Category: Artis DR]] | ||
[[Category: Bard | [[Category: Bard F]] | ||
[[Category: Bowers | [[Category: Bowers S]] | ||
[[Category: Chan | [[Category: Chan W]] | ||
[[Category: Chen | [[Category: Chen L]] | ||
[[Category: Dryer | [[Category: Dryer M]] | ||
[[Category: Galemmo | [[Category: Galemmo Jr RA]] | ||
[[Category: Goldbach | [[Category: Goldbach E]] | ||
[[Category: Griswold-Prenne | [[Category: Griswold-Prenne I]] | ||
[[Category: Hom | [[Category: Hom RK]] | ||
[[Category: Konradi | [[Category: Konradi AW]] | ||
[[Category: Lin | [[Category: Lin M]] | ||
[[Category: Lorentzen | [[Category: Lorentzen C]] | ||
[[Category: Neitz | [[Category: Neitz RJ]] | ||
[[Category: Pan | [[Category: Pan H]] | ||
[[Category: Peterson | [[Category: Peterson B]] | ||
[[Category: Powell | [[Category: Powell K]] | ||
[[Category: Probst | [[Category: Probst GD]] | ||
[[Category: Quincy | [[Category: Quincy Q]] | ||
[[Category: Quinn | [[Category: Quinn KP]] | ||
[[Category: Ren | [[Category: Ren Z]] | ||
[[Category: Ruslim | [[Category: Ruslim L]] | ||
[[Category: Samant | [[Category: Samant B]] | ||
[[Category: Sauer | [[Category: Sauer J]] | ||
[[Category: Sealy | [[Category: Sealy JM]] | ||
[[Category: Sham | [[Category: Sham HL]] | ||
[[Category: Tonn | [[Category: Tonn G]] | ||
[[Category: Truong | [[Category: Truong AP]] | ||
[[Category: Wong | [[Category: Wong K]] | ||
[[Category: Wright | [[Category: Wright S]] | ||
[[Category: Yao | [[Category: Yao N]] | ||
[[Category: Yednock | [[Category: Yednock TA]] | ||
[[Category: Zhang | [[Category: Zhang H]] | ||
[[Category: Zmolek | [[Category: Zmolek W]] | ||