3odk: Difference between revisions
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== | ==Discovery of cell-active phenyl-imidazole Pin1 inhibitors by structure-guided fragment evolution== | ||
[[http://www.uniprot.org/uniprot/PIN1_HUMAN PIN1_HUMAN | <StructureSection load='3odk' size='340' side='right'caption='[[3odk]], [[Resolution|resolution]] 2.30Å' scene=''> | ||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[3odk]] 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=3ODK OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3ODK 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]] 2.3Å</td></tr> | |||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ODK:3-PYRIDIN-2-YL-1H-PYRAZOLE-5-CARBOXYLIC+ACID'>ODK</scene>, <scene name='pdbligand=PE4:2-{2-[2-(2-{2-[2-(2-ETHOXY-ETHOXY)-ETHOXY]-ETHOXY}-ETHOXY)-ETHOXY]-ETHOXY}-ETHANOL'>PE4</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=3odk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3odk OCA], [https://pdbe.org/3odk PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3odk RCSB], [https://www.ebi.ac.uk/pdbsum/3odk PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3odk ProSAT]</span></td></tr> | |||
</table> | |||
== 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> | |||
== | ==See Also== | ||
[[ | *[[Peptidyl-prolyl cis-trans isomerase 3D structures|Peptidyl-prolyl cis-trans isomerase 3D structures]] | ||
== References == | |||
== | <references/> | ||
__TOC__ | |||
</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]] | ||
Latest revision as of 10:34, 21 February 2024
Discovery of cell-active phenyl-imidazole Pin1 inhibitors by structure-guided fragment evolution
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