6nm7
From Proteopedia
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- | '''Unreleased structure''' | ||
- | + | ==PD-L1 IgV domain bound to fragment== | |
+ | <StructureSection load='6nm7' size='340' side='right'caption='[[6nm7]], [[Resolution|resolution]] 2.43Å' scene=''> | ||
+ | == Structural highlights == | ||
+ | <table><tr><td colspan='2'>[[6nm7]] is a 2 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=6NM7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6NM7 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]] 2.426Å</td></tr> | ||
+ | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=22L:5-PHENYLTHIENO[2,3-D]PYRIMIDIN-4(3H)-ONE'>22L</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=6nm7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6nm7 OCA], [https://pdbe.org/6nm7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6nm7 RCSB], [https://www.ebi.ac.uk/pdbsum/6nm7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6nm7 ProSAT]</span></td></tr> | ||
+ | </table> | ||
+ | == Function == | ||
+ | [https://www.uniprot.org/uniprot/PD1L1_HUMAN PD1L1_HUMAN] Involved in the costimulatory signal, essential for T-cell proliferation and production of IL10 and IFNG, in an IL2-dependent and a PDCD1-independent manner. Interaction with PDCD1 inhibits T-cell proliferation and cytokine production.<ref>PMID:10581077</ref> <ref>PMID:11015443</ref> | ||
+ | <div style="background-color:#fffaf0;"> | ||
+ | == Publication Abstract from PubMed == | ||
+ | The PD-1 immune checkpoint pathway is a highly validated target for cancer immunotherapy. Despite the potential advantages of small molecule inhibitors over antibodies, the discovery of small molecule checkpoint inhibitors has lagged behind. To discover small molecule inhibitors of the PD-1 pathway, we have utilized a fragment-based approach. Small molecules were identified that bind to PD-L1 and crystal structures of these compounds bound to PD-L1 were obtained. | ||
- | + | Fragment-based screening of programmed death ligand 1 (PD-L1).,Perry E, Mills JJ, Zhao B, Wang F, Sun Q, Christov PP, Tarr JC, Rietz TA, Olejniczak ET, Lee T, Fesik S Bioorg Med Chem Lett. 2019 Mar 15;29(6):786-790. doi: 10.1016/j.bmcl.2019.01.028., Epub 2019 Jan 24. PMID:30728114<ref>PMID:30728114</ref> | |
- | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
- | [[Category: | + | </div> |
- | [[Category: | + | <div class="pdbe-citations 6nm7" style="background-color:#fffaf0;"></div> |
- | [[Category: Perry | + | == References == |
+ | <references/> | ||
+ | __TOC__ | ||
+ | </StructureSection> | ||
+ | [[Category: Homo sapiens]] | ||
+ | [[Category: Large Structures]] | ||
+ | [[Category: Perry E]] | ||
+ | [[Category: Zhao B]] |
Current revision
PD-L1 IgV domain bound to fragment
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