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==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> | ||
[[3ptg]] is a 2 chain structure | </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== | ==See Also== | ||
*[[Mitogen-activated protein kinase|Mitogen-activated protein kinase]] | *[[Mitogen-activated protein kinase 3D structures|Mitogen-activated protein kinase 3D structures]] | ||
== References == | |||
== | <references/> | ||
< | __TOC__ | ||
</StructureSection> | |||
[[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: Brigham | [[Category: Brigham EF]] | ||
[[Category: Griswold-Prenner | [[Category: Griswold-Prenner I]] | ||
[[Category: Hom | [[Category: Hom RK]] | ||
[[Category: Konradi | [[Category: Konradi AW]] | ||
[[Category: Neitz | [[Category: Neitz J]] | ||
[[Category: Neitzel | [[Category: Neitzel M]] | ||
[[Category: Pan | [[Category: Pan H]] | ||
[[Category: Powell | [[Category: Powell K]] | ||
[[Category: Probst | [[Category: Probst GD]] | ||
[[Category: Quinn | [[Category: Quinn KP]] | ||
[[Category: Ruslim | [[Category: Ruslim L]] | ||
[[Category: Sauer | [[Category: Sauer J]] | ||
[[Category: Sham | [[Category: Sham HL]] | ||
[[Category: Toth | [[Category: Toth G]] | ||
[[Category: Truong | [[Category: Truong AP]] | ||
[[Category: Yao | [[Category: Yao N]] | ||
[[Category: Yednock | [[Category: Yednock TA]] | ||
Latest revision as of 13:43, 21 February 2024
Design and Synthesis of a Novel, Orally Efficacious Tri-substituted Thiophene Based JNK InhibitorDesign and Synthesis of a Novel, Orally Efficacious Tri-substituted Thiophene Based JNK Inhibitor
Structural highlights
DiseaseJIP1_HUMAN Defects in MAPK8IP1 are a cause of non-insulin-dependent diabetes mellitus (NIDDM) [MIM:125853. NIDDM is characterized by an autosomal dominant mode of inheritance, onset during adulthood and insulin resistance.[1] FunctionJIP1_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 AlsoReferences
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