3ptg
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Design and Synthesis of a Novel, Orally Efficacious Tri-substituted Thiophene Based JNK Inhibitor== | |
| + | <StructureSection load='3ptg' size='340' side='right'caption='[[3ptg]], [[Resolution|resolution]] 2.43Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <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> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.43Å</td></tr> | ||
| + | <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> | ||
| + | <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> | ||
| + | == 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 == | ||
| + | [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. | ||
| - | + | ==See Also== | |
| - | + | *[[Mitogen-activated protein kinase 3D structures|Mitogen-activated protein kinase 3D structures]] | |
| - | + | == References == | |
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Artis DR]] | ||
| + | [[Category: Bard F]] | ||
| + | [[Category: Bowers S]] | ||
| + | [[Category: Brigham EF]] | ||
| + | [[Category: Griswold-Prenner I]] | ||
| + | [[Category: Hom RK]] | ||
| + | [[Category: Konradi AW]] | ||
| + | [[Category: Neitz J]] | ||
| + | [[Category: Neitzel M]] | ||
| + | [[Category: Pan H]] | ||
| + | [[Category: Powell K]] | ||
| + | [[Category: Probst GD]] | ||
| + | [[Category: Quinn KP]] | ||
| + | [[Category: Ruslim L]] | ||
| + | [[Category: Sauer J]] | ||
| + | [[Category: Sham HL]] | ||
| + | [[Category: Toth G]] | ||
| + | [[Category: Truong AP]] | ||
| + | [[Category: Yao N]] | ||
| + | [[Category: Yednock TA]] | ||
Current revision
Design and Synthesis of a Novel, Orally Efficacious Tri-substituted Thiophene Based JNK Inhibitor
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Categories: Homo sapiens | Large Structures | Artis DR | Bard F | Bowers S | Brigham EF | Griswold-Prenner I | Hom RK | Konradi AW | Neitz J | Neitzel M | Pan H | Powell K | Probst GD | Quinn KP | Ruslim L | Sauer J | Sham HL | Toth G | Truong AP | Yao N | Yednock TA
