7zjp
From Proteopedia
(Difference between revisions)
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<StructureSection load='7zjp' size='340' side='right'caption='[[7zjp]], [[Resolution|resolution]] 2.19Å' scene=''> | <StructureSection load='7zjp' size='340' side='right'caption='[[7zjp]], [[Resolution|resolution]] 2.19Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[7zjp]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7ZJP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7ZJP FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[7zjp]] 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=7ZJP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7ZJP FirstGlance]. <br> |
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=JJU:2-methyl-4-[4-(trifluoromethyl)phenyl]pyrazolo[3,4-b]indole-7-carboxylic+acid'>JJU</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=JJU:2-methyl-4-[4-(trifluoromethyl)phenyl]pyrazolo[3,4-b]indole-7-carboxylic+acid'>JJU</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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=7zjp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7zjp OCA], [https://pdbe.org/7zjp PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7zjp RCSB], [https://www.ebi.ac.uk/pdbsum/7zjp PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7zjp ProSAT]</span></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=7zjp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7zjp OCA], [https://pdbe.org/7zjp PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7zjp RCSB], [https://www.ebi.ac.uk/pdbsum/7zjp PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7zjp ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Disease == | == Disease == | ||
| - | [[https://www.uniprot.org/uniprot/TEAD1_HUMAN TEAD1_HUMAN]] Defects in TEAD1 are the cause of Sveinsson chorioretinal atrophy (SCRA) [MIM:[https://omim.org/entry/108985 108985]]; also known as atrophia areata (AA) or helicoidal peripapillary chorioretinal degeneration (HPCD). SCRA is characterized by symmetrical lesions radiating from the optic disk involving the retina and the choroid.<ref>PMID:18579750</ref> <ref>PMID:20123905</ref> <ref>PMID:15016762</ref> | + | [[https://www.uniprot.org/uniprot/TEAD1_HUMAN TEAD1_HUMAN]] Defects in TEAD1 are the cause of Sveinsson chorioretinal atrophy (SCRA) [MIM:[https://omim.org/entry/108985 108985]]; also known as atrophia areata (AA) or helicoidal peripapillary chorioretinal degeneration (HPCD). SCRA is characterized by symmetrical lesions radiating from the optic disk involving the retina and the choroid.<ref>PMID:18579750</ref> <ref>PMID:20123905</ref> <ref>PMID:15016762</ref> |
== Function == | == Function == | ||
| - | [[https://www.uniprot.org/uniprot/TEAD1_HUMAN TEAD1_HUMAN]] Transcription factor which plays a key role in the Hippo signaling pathway, a pathway involved in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein MST1/MST2, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1, which in turn phosphorylates and inactivates YAP1 oncoprotein and WWTR1/TAZ. Acts by mediating gene expression of YAP1 and WWTR1/TAZ, thereby regulating cell proliferation, migration and epithelial mesenchymal transition (EMT) induction. Binds specifically and cooperatively to the SPH and GT-IIC 'enhansons' (5'-GTGGAATGT-3') and activates transcription in vivo in a cell-specific manner. The activation function appears to be mediated by a limiting cell-specific transcriptional intermediary factor (TIF). Involved in cardiac development. Binds to the M-CAT motif.<ref>PMID:18579750</ref> <ref>PMID:19324877</ref> | + | [[https://www.uniprot.org/uniprot/TEAD1_HUMAN TEAD1_HUMAN]] Transcription factor which plays a key role in the Hippo signaling pathway, a pathway involved in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein MST1/MST2, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1, which in turn phosphorylates and inactivates YAP1 oncoprotein and WWTR1/TAZ. Acts by mediating gene expression of YAP1 and WWTR1/TAZ, thereby regulating cell proliferation, migration and epithelial mesenchymal transition (EMT) induction. Binds specifically and cooperatively to the SPH and GT-IIC 'enhansons' (5'-GTGGAATGT-3') and activates transcription in vivo in a cell-specific manner. The activation function appears to be mediated by a limiting cell-specific transcriptional intermediary factor (TIF). Involved in cardiac development. Binds to the M-CAT motif.<ref>PMID:18579750</ref> <ref>PMID:19324877</ref> |
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | [[Category: Balsiger | + | [[Category: Balsiger A]] |
| - | [[Category: Bandeiras | + | [[Category: Bandeiras TM]] |
| - | [[Category: Boepple | + | [[Category: Boepple P]] |
| - | [[Category: Broome | + | [[Category: Broome R]] |
| - | [[Category: Carswell | + | [[Category: Carswell E]] |
| - | [[Category: Crowden | + | [[Category: Crowden A]] |
| - | [[Category: Diehl | + | [[Category: Diehl P]] |
| - | [[Category: Dillon | + | [[Category: Dillon C]] |
| - | [[Category: Doerfel | + | [[Category: Doerfel B]] |
| - | [[Category: Freire | + | [[Category: Freire F]] |
| - | [[Category: Garg | + | [[Category: Garg S]] |
| - | [[Category: Gunera | + | [[Category: Gunera J]] |
| - | [[Category: Heinrich | + | [[Category: Heinrich T]] |
| - | [[Category: Hooker | + | [[Category: Hooker M]] |
| - | [[Category: Koetzner | + | [[Category: Koetzner L]] |
| - | [[Category: Lemos | + | [[Category: Lemos AR]] |
| - | [[Category: Musil | + | [[Category: Musil D]] |
| - | [[Category: Pearson | + | [[Category: Pearson N]] |
| - | [[Category: Petersson | + | [[Category: Petersson C]] |
| - | [[Category: Schilke | + | [[Category: Schilke H]] |
| - | [[Category: Schlesiger | + | [[Category: Schlesiger S]] |
| - | [[Category: Schneider | + | [[Category: Schneider R]] |
| - | [[Category: Schwarz | + | [[Category: Schwarz D]] |
| - | [[Category: Seshire | + | [[Category: Seshire A]] |
| - | [[Category: Sirohi | + | [[Category: Sirohi S]] |
| - | [[Category: Sousa | + | [[Category: Sousa PMF]] |
| - | [[Category: Trivier | + | [[Category: Trivier E]] |
| - | [[Category: Wienke | + | [[Category: Wienke D]] |
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Revision as of 04:49, 8 September 2022
Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106
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Categories: Homo sapiens | Large Structures | Balsiger A | Bandeiras TM | Boepple P | Broome R | Carswell E | Crowden A | Diehl P | Dillon C | Doerfel B | Freire F | Garg S | Gunera J | Heinrich T | Hooker M | Koetzner L | Lemos AR | Musil D | Pearson N | Petersson C | Schilke H | Schlesiger S | Schneider R | Schwarz D | Seshire A | Sirohi S | Sousa PMF | Trivier E | Wienke D
