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| | <StructureSection load='5awx' size='340' side='right'caption='[[5awx]], [[Resolution|resolution]] 1.86Å' scene=''> | | <StructureSection load='5awx' size='340' side='right'caption='[[5awx]], [[Resolution|resolution]] 1.86Å' scene=''> |
| | == Structural highlights == | | == Structural highlights == |
| - | <table><tr><td colspan='2'>[[5awx]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5AWX OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5AWX FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[5awx]] 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=5AWX OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5AWX FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=BR:BROMIDE+ION'>BR</scene></td></tr> | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=BR:BROMIDE+ION'>BR</scene></td></tr> |
| - | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">PTPRZ1, HTPZP2, PTPRZ, PTPRZ2, PTPZ ([http://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=5awx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5awx OCA], [https://pdbe.org/5awx PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5awx RCSB], [https://www.ebi.ac.uk/pdbsum/5awx PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5awx ProSAT]</span></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'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5awx FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5awx OCA], [http://pdbe.org/5awx PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5awx RCSB], [http://www.ebi.ac.uk/pdbsum/5awx PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5awx 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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| | | | |
| | ==See Also== | | ==See Also== |
| - | *[[Tyrosine phosphatase|Tyrosine phosphatase]] | + | *[[Tyrosine phosphatase 3D structures|Tyrosine phosphatase 3D structures]] |
| | == References == | | == References == |
| | <references/> | | <references/> |
| | __TOC__ | | __TOC__ |
| | </StructureSection> | | </StructureSection> |
| - | [[Category: Human]] | + | [[Category: Homo sapiens]] |
| | [[Category: Large Structures]] | | [[Category: Large Structures]] |
| - | [[Category: Protein-tyrosine-phosphatase]]
| + | [[Category: Sugawara H]] |
| - | [[Category: Sugawara, H]] | + | |
| - | [[Category: Hydrolase]]
| + | |
| - | [[Category: Protein tyrosine phosphatase]]
| + | |
| Structural highlights
Function
PTPRZ_HUMAN May be involved in the regulation of specific developmental processes in the CNS.
Publication Abstract from PubMed
Protein tyrosine phosphatase receptor-type Z (PTPRZ) is aberrantly over-expressed in glioblastoma and a causative factor for its malignancy. However, small molecules that selectively inhibit the catalytic activity of PTPRZ have not been discovered. We herein performed an in vitro screening of a chemical library, and identified SCB4380 as the first potent inhibitor for PTPRZ. The stoichiometric binding of SCB4380 to the catalytic pocket was demonstrated by biochemical and mass spectrometric analyses. We determined the crystal structure of the catalytic domain of PTPRZ, and the structural basis of the binding of SCB4380 elucidated by a molecular docking method was validated by site-directed mutagenesis studies. The intracellular delivery of SCB4380 by liposome carriers inhibited PTPRZ activity in C6 glioblastoma cells, and thereby suppressed their migration and proliferation in vitro and tumor growth in a rat allograft model. Therefore, selective inhibition of PTPRZ represents a promising approach for glioma therapy.
Small-molecule inhibition of PTPRZ reduces tumor growth in a rat model of glioblastoma.,Fujikawa A, Nagahira A, Sugawara H, Ishii K, Imajo S, Matsumoto M, Kuboyama K, Suzuki R, Tanga N, Noda M, Uchiyama S, Tomoo T, Ogata A, Masumura M, Noda M Sci Rep. 2016 Feb 9;6:20473. doi: 10.1038/srep20473. PMID:26857455[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Fujikawa A, Nagahira A, Sugawara H, Ishii K, Imajo S, Matsumoto M, Kuboyama K, Suzuki R, Tanga N, Noda M, Uchiyama S, Tomoo T, Ogata A, Masumura M, Noda M. Small-molecule inhibition of PTPRZ reduces tumor growth in a rat model of glioblastoma. Sci Rep. 2016 Feb 9;6:20473. doi: 10.1038/srep20473. PMID:26857455 doi:http://dx.doi.org/10.1038/srep20473
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