3ptg: Difference between revisions

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[[Image:3ptg.png|left|200px]]


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==Design and Synthesis of a Novel, Orally Efficacious Tri-substituted Thiophene Based JNK Inhibitor==
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<StructureSection load='3ptg' size='340' side='right'caption='[[3ptg]], [[Resolution|resolution]] 2.43&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3ptg]] is a 2 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=3PTG OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3PTG 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]] 2.43&#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=932:N-[4-METHYL-3-(1H-1,2,4-TRIAZOL-5-YL)THIOPHEN-2-YL]-2-(2-OXO-3,4-DIHYDROQUINOLIN-1(2H)-YL)ACETAMIDE'>932</scene></td></tr>
{{STRUCTURE_3ptg|  PDB=3ptg  |  SCENE=  }}
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3ptg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ptg OCA], [https://pdbe.org/3ptg PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3ptg RCSB], [https://www.ebi.ac.uk/pdbsum/3ptg PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3ptg ProSAT]</span></td></tr>
 
</table>
===Design and Synthesis of a Novel, Orally Efficacious Tri-substituted Thiophene Based JNK Inhibitor===
== Disease ==
 
[https://www.uniprot.org/uniprot/JIP1_HUMAN JIP1_HUMAN] Defects in MAPK8IP1 are a cause of non-insulin-dependent diabetes mellitus (NIDDM) [MIM:[https://omim.org/entry/125853 125853]. NIDDM is characterized by an autosomal dominant mode of inheritance, onset during adulthood and insulin resistance.<ref>PMID:10700186</ref>
 
== Function ==
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[https://www.uniprot.org/uniprot/JIP1_HUMAN JIP1_HUMAN] The JNK-interacting protein (JIP) group of scaffold proteins selectively mediates JNK signaling by aggregating specific components of the MAPK cascade to form a functional JNK signaling module. Required for JNK activation in response to excitotoxic stress. Cytoplasmic MAPK8IP1 causes inhibition of JNK-regulated activity by retaining JNK in the cytoplasm and inhibiting JNK phosphorylation of c-Jun. May also participate in ApoER2-specific reelin signaling. Directly, or indirectly, regulates GLUT2 gene expression and beta-cell function. Appears to have a role in cell signaling in mature and developing nerve terminals. May function as a regulator of vesicle transport, through interactions with the JNK-signaling components and motor proteins (By similarity). Functions as an anti-apoptotic protein and whose level seems to influence the beta-cell death or survival response.
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{{ABSTRACT_PUBMED_21316234}}
 
==About this Structure==
[[3ptg]] is a 2 chain structure of [[Mitogen-activated protein kinase]] with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PTG OCA].  


==See Also==
==See Also==
*[[Mitogen-activated protein kinase]]
*[[Mitogen-activated protein kinase 3D structures|Mitogen-activated protein kinase 3D structures]]
 
== References ==
==Reference==
<references/>
<ref group="xtra">PMID:21316234</ref><references group="xtra"/>
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</StructureSection>
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Mitogen-activated protein kinase]]
[[Category: Large Structures]]
[[Category: Artis, D R.]]
[[Category: Artis DR]]
[[Category: Bard, F.]]
[[Category: Bard F]]
[[Category: Bowers, S.]]
[[Category: Bowers S]]
[[Category: Brigham, E F.]]
[[Category: Brigham EF]]
[[Category: Griswold-Prenner, I.]]
[[Category: Griswold-Prenner I]]
[[Category: Hom, R K.]]
[[Category: Hom RK]]
[[Category: Konradi, A W.]]
[[Category: Konradi AW]]
[[Category: Neitz, J.]]
[[Category: Neitz J]]
[[Category: Neitzel, M.]]
[[Category: Neitzel M]]
[[Category: Pan, H.]]
[[Category: Pan H]]
[[Category: Powell, K.]]
[[Category: Powell K]]
[[Category: Probst, G D.]]
[[Category: Probst GD]]
[[Category: Quinn, K P.]]
[[Category: Quinn KP]]
[[Category: Ruslim, L.]]
[[Category: Ruslim L]]
[[Category: Sauer, J.]]
[[Category: Sauer J]]
[[Category: Sham, H L.]]
[[Category: Sham HL]]
[[Category: Toth, G.]]
[[Category: Toth G]]
[[Category: Truong, A P.]]
[[Category: Truong AP]]
[[Category: Yao, N.]]
[[Category: Yao N]]
[[Category: Yednock, T A.]]
[[Category: Yednock TA]]

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