2xpb
From Proteopedia
(Difference between revisions)
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<StructureSection load='2xpb' size='340' side='right'caption='[[2xpb]], [[Resolution|resolution]] 2.00Å' scene=''> | <StructureSection load='2xpb' size='340' side='right'caption='[[2xpb]], [[Resolution|resolution]] 2.00Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
- | <table><tr><td colspan='2'>[[2xpb]] is a 1 chain structure with sequence from [ | + | <table><tr><td colspan='2'>[[2xpb]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2XPB OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2XPB FirstGlance]. <br> |
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=12P:DODECAETHYLENE+GLYCOL'>12P</scene>, <scene name='pdbligand=4GE:5-[BENZYL(METHYL)CARBAMOYL]-2-(3-CHLOROPHENYL)-1H-IMIDAZOLE-4-CARBOXYLIC+ACID'>4GE</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=12P:DODECAETHYLENE+GLYCOL'>12P</scene>, <scene name='pdbligand=4GE:5-[BENZYL(METHYL)CARBAMOYL]-2-(3-CHLOROPHENYL)-1H-IMIDAZOLE-4-CARBOXYLIC+ACID'>4GE</scene></td></tr> | ||
- | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1f8a|1f8a]], [[1i8g|1i8g]], [[1pin|1pin]], [[2xp3|2xp3]], [[2xp8|2xp8]], [[2xp5|2xp5]], [[1nmv|1nmv]], [[2xp9|2xp9]], [[1nmw|1nmw]], [[1zcn|1zcn]], [[2xp4|2xp4]], [[2xp7|2xp7]], [[2f21|2f21]], [[2xp6|2xp6]], [[1i8h|1i8h]], [[2xpa|2xpa]], [[1i6c|1i6c]]</td></tr> | + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1f8a|1f8a]], [[1i8g|1i8g]], [[1pin|1pin]], [[2xp3|2xp3]], [[2xp8|2xp8]], [[2xp5|2xp5]], [[1nmv|1nmv]], [[2xp9|2xp9]], [[1nmw|1nmw]], [[1zcn|1zcn]], [[2xp4|2xp4]], [[2xp7|2xp7]], [[2f21|2f21]], [[2xp6|2xp6]], [[1i8h|1i8h]], [[2xpa|2xpa]], [[1i6c|1i6c]]</div></td></tr> |
- | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Peptidylprolyl_isomerase Peptidylprolyl isomerase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=5.2.1.8 5.2.1.8] </span></td></tr> |
- | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2xpb FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xpb OCA], [https://pdbe.org/2xpb PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2xpb RCSB], [https://www.ebi.ac.uk/pdbsum/2xpb PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2xpb ProSAT]</span></td></tr> |
</table> | </table> | ||
== Function == | == Function == | ||
- | [[ | + | [[https://www.uniprot.org/uniprot/PIN1_HUMAN PIN1_HUMAN]] Essential PPIase that regulates mitosis presumably by interacting with NIMA and attenuating its mitosis-promoting activity. Displays a preference for an acidic residue N-terminal to the isomerized proline bond. Catalyzes pSer/Thr-Pro cis/trans isomerizations. Down-regulates kinase activity of BTK. Can transactivate multiple oncogenes and induce centrosome amplification, chromosome instability and cell transformation. Required for the efficient dephosphorylation and recycling of RAF1 after mitogen activation.<ref>PMID:15664191</ref> <ref>PMID:16644721</ref> <ref>PMID:21497122</ref> |
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == |
Revision as of 05:25, 10 August 2022
DISCOVERY OF CELL-ACTIVE PHENYL-IMIDAZOLE PIN1 INHIBITORS BY STRUCTURE-GUIDED FRAGMENT EVOLUTION
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Categories: Human | Large Structures | Peptidylprolyl isomerase | Baker, L | Bryant, C J | Davis, B E | Dokurno, P | Fromont, C | Matossova, N | Moore, J D | Murray, J B | Northfield, C J | Nunns, C | Oldfield, V | Potter, A | Ray, S | Richardson, C M | Robinson, D | Scrace, S F | Surgenor, A E | Cell cycle | Isomerase | Oncogenic transformation | Proline directed kinase