2xp3: Difference between revisions
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==DISCOVERY OF CELL-ACTIVE PHENYL-IMIDAZOLE PIN1 INHIBITORS BY STRUCTURE-GUIDED FRAGMENT EVOLUTION== | ==DISCOVERY OF CELL-ACTIVE PHENYL-IMIDAZOLE PIN1 INHIBITORS BY STRUCTURE-GUIDED FRAGMENT EVOLUTION== | ||
<StructureSection load='2xp3' size='340' side='right' caption='[[2xp3]], [[Resolution|resolution]] 2.00Å' scene=''> | <StructureSection load='2xp3' size='340' side='right'caption='[[2xp3]], [[Resolution|resolution]] 2.00Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[2xp3]] is a 1 chain structure with sequence from [ | <table><tr><td colspan='2'>[[2xp3]] is a 1 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=2XP3 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2XP3 FirstGlance]. <br> | ||
</td></tr><tr id=' | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2Å</td></tr> | ||
<tr id=' | <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=B21:5-(2-METHOXYPHENYL)-2-FUROIC+ACID'>B21</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=2xp3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2xp3 OCA], [https://pdbe.org/2xp3 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2xp3 RCSB], [https://www.ebi.ac.uk/pdbsum/2xp3 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2xp3 ProSAT]</span></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | |||
</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 == | ||
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
</div> | </div> | ||
<div class="pdbe-citations 2xp3" style="background-color:#fffaf0;"></div> | |||
==See Also== | |||
*[[Peptidyl-prolyl cis-trans isomerase 3D structures|Peptidyl-prolyl cis-trans isomerase 3D structures]] | |||
== References == | == References == | ||
<references/> | <references/> | ||
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</StructureSection> | </StructureSection> | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: | [[Category: Large Structures]] | ||
[[Category: Baker | [[Category: Baker L]] | ||
[[Category: Bryant | [[Category: Bryant CJ]] | ||
[[Category: Davis | [[Category: Davis BE]] | ||
[[Category: Dokurno | [[Category: Dokurno P]] | ||
[[Category: Fromont | [[Category: Fromont C]] | ||
[[Category: Matossova | [[Category: Matossova N]] | ||
[[Category: Moore | [[Category: Moore JD]] | ||
[[Category: Murray | [[Category: Murray JB]] | ||
[[Category: Northfield | [[Category: Northfield CJ]] | ||
[[Category: Nunns | [[Category: Nunns C]] | ||
[[Category: Oldfield | [[Category: Oldfield V]] | ||
[[Category: Potter | [[Category: Potter A]] | ||
[[Category: Ray | [[Category: Ray S]] | ||
[[Category: Richardson | [[Category: Richardson CM]] | ||
[[Category: Robinson | [[Category: Robinson D]] | ||
[[Category: Scrace | [[Category: Scrace SF]] | ||
[[Category: Surgenor | [[Category: Surgenor AE]] | ||