8skl
From Proteopedia
(Difference between revisions)
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<table><tr><td colspan='2'>[[8skl]] 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=8SKL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8SKL FirstGlance]. <br> | <table><tr><td colspan='2'>[[8skl]] 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=8SKL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8SKL 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]] 1.55Å</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]] 1.55Å</td></tr> | ||
| - | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=V2O:5-[1- | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=V2O:5-[1-fluoranyl-7-(3-methyl-3-oxidanyl-butoxy)-3-oxidanyl-naphthalen-2-yl]-1,1-bis(oxidanylidene)-1,2,5-thiadiazolidin-3-one'>V2O</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=8skl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8skl OCA], [https://pdbe.org/8skl PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8skl RCSB], [https://www.ebi.ac.uk/pdbsum/8skl PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8skl 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=8skl FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8skl OCA], [https://pdbe.org/8skl PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8skl RCSB], [https://www.ebi.ac.uk/pdbsum/8skl PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8skl ProSAT]</span></td></tr> | ||
</table> | </table> | ||
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<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
| - | The inhibition of protein tyrosine phosphatases ( | + | The inhibition of protein tyrosine phosphatases 1B (PTP1B) and N2 (PTPN2) has emerged as an exciting approach for bolstering T cell anti-tumor immunity. ABBV-CLS-484 is a PTP1B/PTPN2 inhibitor in clinical trials for solid tumors. Here we have explored the therapeutic potential of a related small-molecule-inhibitor, Compound-182. We demonstrate that Compound-182 is a highly potent and selective active site competitive inhibitor of PTP1B and PTPN2 that enhances T cell recruitment and activation and represses the growth of tumors in mice, without promoting overt immune-related toxicities. The enhanced anti-tumor immunity in immunogenic tumors can be ascribed to the inhibition of PTP1B/PTPN2 in T cells, whereas in cold tumors, Compound-182 elicited direct effects on both tumor cells and T cells. Importantly, treatment with Compound-182 rendered otherwise resistant tumors sensitive to alpha-PD-1 therapy. Our findings establish the potential for small molecule inhibitors of PTP1B and PTPN2 to enhance anti-tumor immunity and combat cancer. |
| - | A small molecule inhibitor of PTP1B and PTPN2 enhances T cell anti-tumor immunity.,Liang S, Tran E, Du X, Dong J, Sudholz H, Chen H, Qu Z, Huntington | + | A small molecule inhibitor of PTP1B and PTPN2 enhances T cell anti-tumor immunity.,Liang S, Tran E, Du X, Dong J, Sudholz H, Chen H, Qu Z, Huntington ND, Babon JJ, Kershaw NJ, Zhang ZY, Baell JB, Wiede F, Tiganis T Nat Commun. 2023 Jul 27;14(1):4524. doi: 10.1038/s41467-023-40170-8. PMID:37500611<ref>PMID:37500611</ref> |
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 8skl" style="background-color:#fffaf0;"></div> | <div class="pdbe-citations 8skl" style="background-color:#fffaf0;"></div> | ||
| + | |||
| + | ==See Also== | ||
| + | *[[Tyrosine phosphatase 3D structures|Tyrosine phosphatase 3D structures]] | ||
== References == | == References == | ||
<references/> | <references/> | ||
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[[Category: Babon JJ]] | [[Category: Babon JJ]] | ||
[[Category: Chen H]] | [[Category: Chen H]] | ||
| + | [[Category: Kershaw NJ]] | ||
[[Category: Tiganis T]] | [[Category: Tiganis T]] | ||
Current revision
PTP1B in complex with 182
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