3rtp: Difference between revisions

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-'''Unreleased structure'''
-The entry 3rtp is ON HOLD  until sometime in the future
+==Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration==
+<StructureSection load='3rtp' size='340' side='right'caption='[[3rtp]], [[Resolution|resolution]] 2.40&Aring;' 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]] 2.4&#8491;</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>
-Authors: Bowers, S., Truong, A.P., Neitz, R.J., Hom, R.K., Sealy, J.M., Probst, G.D., Quincy, Q., Peterson, B., Chan, W., Galemmo Jr., R.A., Konradi, A.W., Sham, H.L., Pan, H., Lin, M., Yao, N., Artis, D.R., Zhang, H., Chen, L., Dryer, M., Samant, B., Zmolek, W., Wong, K., Lorentzen, C., Goldbach, E., Tonn, G., Quinn, K.P., Sauer, J., Wright, S., Powell, K., Ruslim, L., Ren, Z., Bard, F., Yednock, T.A., Griswold-Prenne, I.
+==See Also==
+*[[Mitogen-activated protein kinase 3D structures|Mitogen-activated protein kinase 3D structures]]
-Description: Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration
+== References ==
+<references/>
+__TOC__
+</StructureSection>
+[[Category: Homo sapiens]]
+[[Category: Large Structures]]
+[[Category: Artis DR]]
+[[Category: Bard F]]
+[[Category: Bowers S]]
+[[Category: Chan W]]
+[[Category: Chen L]]
+[[Category: Dryer M]]
+[[Category: Galemmo Jr RA]]
+[[Category: Goldbach E]]
+[[Category: Griswold-Prenne I]]
+[[Category: Hom RK]]
+[[Category: Konradi AW]]
+[[Category: Lin M]]
+[[Category: Lorentzen C]]
+[[Category: Neitz RJ]]
+[[Category: Pan H]]
+[[Category: Peterson B]]
+[[Category: Powell K]]
+[[Category: Probst GD]]
+[[Category: Quincy Q]]
+[[Category: Quinn KP]]
+[[Category: Ren Z]]
+[[Category: Ruslim L]]
+[[Category: Samant B]]
+[[Category: Sauer J]]
+[[Category: Sealy JM]]
+[[Category: Sham HL]]
+[[Category: Tonn G]]
+[[Category: Truong AP]]
+[[Category: Wong K]]
+[[Category: Wright S]]
+[[Category: Yao N]]
+[[Category: Yednock TA]]
+[[Category: Zhang H]]
+[[Category: Zmolek W]]