6xnp
From Proteopedia
(Difference between revisions)
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==Crystal Structure of Human STING CTD complex with SR-717== | ==Crystal Structure of Human STING CTD complex with SR-717== | ||
| - | <StructureSection load='6xnp' size='340' side='right'caption='[[6xnp]]' scene=''> | + | <StructureSection load='6xnp' size='340' side='right'caption='[[6xnp]], [[Resolution|resolution]] 1.77Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6XNP OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6XNP FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[6xnp]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6XNP OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6XNP FirstGlance]. <br> |
| - | </td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6xnp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6xnp OCA], [http://pdbe.org/6xnp PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6xnp RCSB], [http://www.ebi.ac.uk/pdbsum/6xnp PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6xnp ProSAT]</span></td></tr> | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=V67:4,5-difluoro-2-{[6-(1H-imidazol-1-yl)pyridazine-3-carbonyl]amino}benzoic+acid'>V67</scene></td></tr> |
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6xnp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6xnp OCA], [http://pdbe.org/6xnp PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6xnp RCSB], [http://www.ebi.ac.uk/pdbsum/6xnp PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6xnp ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Stimulator of interferon genes (STING) links innate immunity to biological processes ranging from antitumor immunity to microbiome homeostasis. Mechanistic understanding of the anticancer potential for STING receptor activation is currently limited by metabolic instability of the natural cyclic dinucleotide (CDN) ligands. From a pathway-targeted cell-based screen, we identified a non-nucleotide, small-molecule STING agonist, termed SR-717, that demonstrates broad interspecies and interallelic specificity. A 1.8-angstrom cocrystal structure revealed that SR-717 functions as a direct cyclic guanosine monophosphate-adenosine monophosphate (cGAMP) mimetic that induces the same "closed" conformation of STING. SR-717 displayed antitumor activity; promoted the activation of CD8(+) T, natural killer, and dendritic cells in relevant tissues; and facilitated antigen cross-priming. SR-717 also induced the expression of clinically relevant targets, including programmed cell death 1 ligand 1 (PD-L1), in a STING-dependent manner. | ||
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| + | Antitumor activity of a systemic STING-activating non-nucleotide cGAMP mimetic.,Chin EN, Yu C, Vartabedian VF, Jia Y, Kumar M, Gamo AM, Vernier W, Ali SH, Kissai M, Lazar DC, Nguyen N, Pereira LE, Benish B, Woods AK, Joseph SB, Chu A, Johnson KA, Sander PN, Martinez-Pena F, Hampton EN, Young TS, Wolan DW, Chatterjee AK, Schultz PG, Petrassi HM, Teijaro JR, Lairson LL Science. 2020 Aug 21;369(6506):993-999. doi: 10.1126/science.abb4255. PMID:32820126<ref>PMID:32820126</ref> | ||
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| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 6xnp" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | [[Category: Chin | + | [[Category: Chin, E N]] |
| - | [[Category: Lairson | + | [[Category: Lairson, L L]] |
| - | [[Category: Petrassi | + | [[Category: Petrassi, H M]] |
| - | [[Category: Wolan | + | [[Category: Wolan, D W]] |
| - | [[Category: Yu C]] | + | [[Category: Yu, C]] |
| + | [[Category: Agonist]] | ||
| + | [[Category: Closed conformation]] | ||
| + | [[Category: Complex]] | ||
| + | [[Category: Immune system]] | ||
| + | [[Category: Immunity]] | ||
Revision as of 07:11, 2 September 2020
Crystal Structure of Human STING CTD complex with SR-717
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