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| | <StructureSection load='3acl' size='340' side='right'caption='[[3acl]], [[Resolution|resolution]] 2.35Å' scene=''> | | <StructureSection load='3acl' size='340' side='right'caption='[[3acl]], [[Resolution|resolution]] 2.35Å' scene=''> |
| | == Structural highlights == | | == Structural highlights == |
| - | <table><tr><td colspan='2'>[[3acl]] 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=3ACL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3ACL FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[3acl]] 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=3ACL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3ACL FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3F1:N-{[4-(BENZYLOXY)PHENYL](METHYL)-LAMBDA~4~-SULFANYLIDENE}-4-METHYLBENZENESULFONAMIDE'>3F1</scene>, <scene name='pdbligand=FE2:FE+(II)+ION'>FE2</scene></td></tr> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.35Å</td></tr> |
| - | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1j1l|1j1l]]</div></td></tr> | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3F1:N-{[4-(BENZYLOXY)PHENYL](METHYL)-LAMBDA~4~-SULFANYLIDENE}-4-METHYLBENZENESULFONAMIDE'>3F1</scene>, <scene name='pdbligand=FE2:FE+(II)+ION'>FE2</scene></td></tr> |
| - | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PIR ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=3acl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3acl OCA], [https://pdbe.org/3acl PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3acl RCSB], [https://www.ebi.ac.uk/pdbsum/3acl PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3acl 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=3acl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3acl OCA], [https://pdbe.org/3acl PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3acl RCSB], [https://www.ebi.ac.uk/pdbsum/3acl PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3acl ProSAT]</span></td></tr> |
| | </table> | | </table> |
| | == Function == | | == Function == |
| - | [[https://www.uniprot.org/uniprot/PIR_HUMAN PIR_HUMAN]] Possible transcriptional coregulator. May contribute to the regulation of cellular processes via its interaction with BCL3. May be required for efficient terminal myeloid maturation of hematopoietic cells. May play a role in the regulation of cell migration. May promote apoptosis when overexpressed. Has quercetin 2,3-dioxygenase activity (in vitro).<ref>PMID:9079676</ref> <ref>PMID:17288615</ref> <ref>PMID:20010624</ref> <ref>PMID:20711196</ref>
| + | [https://www.uniprot.org/uniprot/PIR_HUMAN PIR_HUMAN] Possible transcriptional coregulator. May contribute to the regulation of cellular processes via its interaction with BCL3. May be required for efficient terminal myeloid maturation of hematopoietic cells. May play a role in the regulation of cell migration. May promote apoptosis when overexpressed. Has quercetin 2,3-dioxygenase activity (in vitro).<ref>PMID:9079676</ref> <ref>PMID:17288615</ref> <ref>PMID:20010624</ref> <ref>PMID:20711196</ref> |
| | == Evolutionary Conservation == | | == Evolutionary Conservation == |
| | [[Image:Consurf_key_small.gif|200px|right]] | | [[Image:Consurf_key_small.gif|200px|right]] |
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| | </div> | | </div> |
| | <div class="pdbe-citations 3acl" style="background-color:#fffaf0;"></div> | | <div class="pdbe-citations 3acl" style="background-color:#fffaf0;"></div> |
| | + | |
| | + | ==See Also== |
| | + | *[[Dioxygenase 3D structures|Dioxygenase 3D structures]] |
| | == References == | | == References == |
| | <references/> | | <references/> |
| | __TOC__ | | __TOC__ |
| | </StructureSection> | | </StructureSection> |
| - | [[Category: Human]] | + | [[Category: Homo sapiens]] |
| | [[Category: Large Structures]] | | [[Category: Large Structures]] |
| - | [[Category: Miyazaki, I]] | + | [[Category: Miyazaki I]] |
| - | [[Category: Okumura, H]] | + | [[Category: Okumura H]] |
| - | [[Category: Osada, H]] | + | [[Category: Osada H]] |
| - | [[Category: Simizu, S]] | + | [[Category: Simizu S]] |
| - | [[Category: Complex]]
| + | |
| - | [[Category: Cupin]]
| + | |
| - | [[Category: Inhibitor]]
| + | |
| - | [[Category: Iron]]
| + | |
| - | [[Category: Metal binding protein]]
| + | |
| Structural highlights
Function
PIR_HUMAN Possible transcriptional coregulator. May contribute to the regulation of cellular processes via its interaction with BCL3. May be required for efficient terminal myeloid maturation of hematopoietic cells. May play a role in the regulation of cell migration. May promote apoptosis when overexpressed. Has quercetin 2,3-dioxygenase activity (in vitro).[1] [2] [3] [4]
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
The discovery of small molecules that bind to a specific target and disrupt the function of proteins is an important step in chemical biology, especially for poorly characterized proteins. Human pirin is a nuclear protein of unknown function that is widely expressed in punctate subnuclear structures in human tissues. Here, we report the discovery of a small molecule that binds to pirin. We determined how the small molecule bound to pirin by solving the cocrystal structure. Either knockdown of pirin or treatment with the small molecule inhibited melanoma cell migration. Thus, inhibition of pirin by the small molecule has led to a greater understanding of the function of pirin and represents a new method of studying pirin-mediated signaling pathways.
A small-molecule inhibitor shows that pirin regulates migration of melanoma cells.,Miyazaki I, Simizu S, Okumura H, Takagi S, Osada H Nat Chem Biol. 2010 Sep;6(9):667-73. Epub 2010 Aug 15. PMID:20711196[5]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Wendler WM, Kremmer E, Forster R, Winnacker EL. Identification of pirin, a novel highly conserved nuclear protein. J Biol Chem. 1997 Mar 28;272(13):8482-9. PMID:9079676
- ↑ Gelbman BD, Heguy A, O'Connor TP, Zabner J, Crystal RG. Upregulation of pirin expression by chronic cigarette smoking is associated with bronchial epithelial cell apoptosis. Respir Res. 2007 Feb 8;8:10. PMID:17288615 doi:http://dx.doi.org/10.1186/1465-9921-8-10
- ↑ Licciulli S, Cambiaghi V, Scafetta G, Gruszka AM, Alcalay M. Pirin downregulation is a feature of AML and leads to impairment of terminal myeloid differentiation. Leukemia. 2010 Feb;24(2):429-37. doi: 10.1038/leu.2009.247. Epub 2009 Dec 10. PMID:20010624 doi:http://dx.doi.org/10.1038/leu.2009.247
- ↑ Miyazaki I, Simizu S, Okumura H, Takagi S, Osada H. A small-molecule inhibitor shows that pirin regulates migration of melanoma cells. Nat Chem Biol. 2010 Sep;6(9):667-73. Epub 2010 Aug 15. PMID:20711196 doi:10.1038/nchembio.423
- ↑ Miyazaki I, Simizu S, Okumura H, Takagi S, Osada H. A small-molecule inhibitor shows that pirin regulates migration of melanoma cells. Nat Chem Biol. 2010 Sep;6(9):667-73. Epub 2010 Aug 15. PMID:20711196 doi:10.1038/nchembio.423
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