6nos
From Proteopedia
(Difference between revisions)
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| - | '''Unreleased structure''' | ||
| - | + | ==PD-L1 IgV domain V76T with fragment== | |
| + | <StructureSection load='6nos' size='340' side='right' caption='[[6nos]], [[Resolution|resolution]] 2.70Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[6nos]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6NOS OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6NOS FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=KWA:1-[5-(3,5-dichlorophenyl)furan-2-yl]-N-methylmethanamine'>KWA</scene></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=6nos FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6nos OCA], [http://pdbe.org/6nos PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6nos RCSB], [http://www.ebi.ac.uk/pdbsum/6nos PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6nos ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [[http://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> | |
| - | + | </div> | |
| - | + | <div class="pdbe-citations 6nos" style="background-color:#fffaf0;"></div> | |
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
[[Category: Perry, E]] | [[Category: Perry, E]] | ||
| + | [[Category: Zhao, B]] | ||
| + | [[Category: Cancer drug discovery]] | ||
| + | [[Category: Fragment-based screening]] | ||
| + | [[Category: Immune system]] | ||
| + | [[Category: Immunotherapy]] | ||
| + | [[Category: Pd-l1 inhibitor]] | ||
| + | [[Category: Structure-based design]] | ||
Revision as of 06:56, 21 February 2019
PD-L1 IgV domain V76T with fragment
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