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| | ==Human PTPRZ D1 domain complexed with NAZ2329== | | ==Human PTPRZ D1 domain complexed with NAZ2329== |
| - | <StructureSection load='5h08' size='340' side='right' caption='[[5h08]], [[Resolution|resolution]] 2.53Å' scene=''> | + | <StructureSection load='5h08' size='340' side='right'caption='[[5h08]], [[Resolution|resolution]] 2.53Å' scene=''> |
| | == Structural highlights == | | == Structural highlights == |
| - | <table><tr><td colspan='2'>[[5h08]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5H08 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5H08 FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[5h08]] 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=5H08 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5H08 FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=7WL:3-{[2-Ethoxy-5-(trifluoromethyl)benzyl]sulfanyl}-N-(phenylsulfonyl)thiophene-2-carboxamide'>7WL</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]] 2.53Å</td></tr> |
| - | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5awx|5awx]]</td></tr> | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=7WL:3-{[2-Ethoxy-5-(trifluoromethyl)benzyl]sulfanyl}-N-(phenylsulfonyl)thiophene-2-carboxamide'>7WL</scene></td></tr> |
| - | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Protein-tyrosine-phosphatase Protein-tyrosine-phosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.48 3.1.3.48] </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=5h08 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5h08 OCA], [https://pdbe.org/5h08 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5h08 RCSB], [https://www.ebi.ac.uk/pdbsum/5h08 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5h08 ProSAT]</span></td></tr> |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5h08 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5h08 OCA], [http://pdbe.org/5h08 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5h08 RCSB], [http://www.ebi.ac.uk/pdbsum/5h08 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5h08 ProSAT]</span></td></tr> | + | |
| | </table> | | </table> |
| | == Function == | | == Function == |
| - | [[http://www.uniprot.org/uniprot/PTPRZ_HUMAN PTPRZ_HUMAN]] May be involved in the regulation of specific developmental processes in the CNS. | + | [https://www.uniprot.org/uniprot/PTPRZ_HUMAN PTPRZ_HUMAN] May be involved in the regulation of specific developmental processes in the CNS. |
| | <div style="background-color:#fffaf0;"> | | <div style="background-color:#fffaf0;"> |
| | == Publication Abstract from PubMed == | | == Publication Abstract from PubMed == |
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| | </div> | | </div> |
| | <div class="pdbe-citations 5h08" style="background-color:#fffaf0;"></div> | | <div class="pdbe-citations 5h08" style="background-color:#fffaf0;"></div> |
| | + | |
| | + | ==See Also== |
| | + | *[[Tyrosine phosphatase 3D structures|Tyrosine phosphatase 3D structures]] |
| | == References == | | == References == |
| | <references/> | | <references/> |
| | __TOC__ | | __TOC__ |
| | </StructureSection> | | </StructureSection> |
| - | [[Category: Protein-tyrosine-phosphatase]] | + | [[Category: Homo sapiens]] |
| - | [[Category: Sugawara, H]] | + | [[Category: Large Structures]] |
| - | [[Category: Hydrolase]] | + | [[Category: Sugawara H]] |
| - | [[Category: Hydrolase-hydrolase inhibitor complex]]
| + | |
| - | [[Category: Protein tyrosine phosphatase]]
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| Structural highlights
Function
PTPRZ_HUMAN May be involved in the regulation of specific developmental processes in the CNS.
Publication Abstract from PubMed
The R5 subfamily of receptor-type protein tyrosine phosphatases (RPTPs) comprises PTPRZ and PTPRG. A recent study on primary human glioblastomas suggested a close association between PTPRZ1 (human PTPRZ) expression and cancer stemness. However, the functional roles of PTPRZ activity in glioma stem cells have remained unclear. In the present study, we found that sphere-forming cells from the rat C6 and human U251 glioblastoma cell lines showed high expression levels of PTPRZ-B, the short receptor isoform of PTPRZ. Stable PTPRZ knockdown altered the expression levels of stem cell transcription factors such as SOX2, OLIG2, and POU3F2 and decreased the sphere-forming abilities of these cells. Suppressive effects on the cancer stem-like properties of the cells were also observed following the knockdown of PTPRG. Here, we identified NAZ2329, a cell-permeable small molecule that allosterically inhibits both PTPRZ and PTPRG. NAZ2329 reduced the expression of SOX2 in C6 and U251 cells and abrogated the sphere-forming abilities of these cells. Tumor growth in the C6 xenograft mouse model was significantly slower with the co-treatment of NAZ2329 with temozolomide, an alkylating agent, than with the individual treatments. These results indicate that pharmacological inhibition of R5 RPTPs is a promising strategy for the treatment of malignant gliomas.
Targeting PTPRZ inhibits stem cell-like properties and tumorigenicity in glioblastoma cells.,Fujikawa A, Sugawara H, Tanaka T, Matsumoto M, Kuboyama K, Suzuki R, Tanga N, Ogata A, Masumura M, Noda M Sci Rep. 2017 Jul 17;7(1):5609. doi: 10.1038/s41598-017-05931-8. PMID:28717188[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Fujikawa A, Sugawara H, Tanaka T, Matsumoto M, Kuboyama K, Suzuki R, Tanga N, Ogata A, Masumura M, Noda M. Targeting PTPRZ inhibits stem cell-like properties and tumorigenicity in glioblastoma cells. Sci Rep. 2017 Jul 17;7(1):5609. doi: 10.1038/s41598-017-05931-8. PMID:28717188 doi:http://dx.doi.org/10.1038/s41598-017-05931-8
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