7dy7 - Revision history

OCA at 16:42, 29 November 2023

OCA — Wed, 29 Nov 2023 16:42:25 GMT

←Older revision		Revision as of 16:42, 29 November 2023
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	<StructureSection load='7dy7' size='340' side='right'caption='[[7dy7]], [[Resolution\|resolution]] 2.42Å' scene=''>		<StructureSection load='7dy7' size='340' side='right'caption='[[7dy7]], [[Resolution\|resolution]] 2.42Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[7dy7]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7DY7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7DY7 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[7dy7]] 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=7DY7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7DY7 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=HOU:2-[[3-[[5-(2-methyl-3-phenyl-phenyl)-1,3,4-oxadiazol-2-yl]amino]phenyl]methylamino]ethanol'>HOU</scene></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]] 2.42Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=HOU:2-[[3-[[5-(2-methyl-3-phenyl-phenyl)-1,3,4-oxadiazol-2-yl]amino]phenyl]methylamino]ethanol'>HOU</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=7dy7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7dy7 OCA], [https://pdbe.org/7dy7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7dy7 RCSB], [https://www.ebi.ac.uk/pdbsum/7dy7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7dy7 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=7dy7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7dy7 OCA], [https://pdbe.org/7dy7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7dy7 RCSB], [https://www.ebi.ac.uk/pdbsum/7dy7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7dy7 ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== 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>	+	[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;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 22:		Line 23:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Cheng, Y]]	+	[[Category: Cheng Y]]
-	[[Category: Jiang, S]]	+	[[Category: Jiang S]]
-	[[Category: Lu~~, M L~~]]	+	[[Category: Lu ML]]
-	[[Category: Wang~~, T Y~~]]	+	[[Category: Wang TY]]
-	[[Category: Xiao~~, Y B]]~~	+	[[Category: Xiao YB]]
-	~~[[Category: Complex]]~~	+
-	~~[[Category: Dimer]]~~	+
-	~~[[Category: Immune checkpoint]]~~	+
-	~~[[Category: Immunosuppressant]]~~	+
-	~~[[Category: Inhibitor~~]]	+

OCA at 11:47, 27 April 2022

OCA — Wed, 27 Apr 2022 11:47:38 GMT

←Older revision		Revision as of 11:47, 27 April 2022
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	==Discovery of Novel Small-molecule Inhibitors of PD-1/PD-L1 Axis that Promotes PD-L1 Internalization and Degradation==		==Discovery of Novel Small-molecule Inhibitors of PD-1/PD-L1 Axis that Promotes PD-L1 Internalization and Degradation==
-	<StructureSection load='7dy7' size='340' side='right'caption='[[7dy7]]' scene=''>	+	<StructureSection load='7dy7' size='340' side='right'caption='[[7dy7]], [[Resolution\|resolution]] 2.42Å' 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=7DY7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7DY7 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[7dy7]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7DY7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7DY7 FirstGlance]. <br>
-	</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=7dy7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7dy7 OCA], [https://pdbe.org/7dy7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7dy7 RCSB], [https://www.ebi.ac.uk/pdbsum/7dy7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7dy7 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=HOU:2-[[3-[[5-(2-methyl-3-phenyl-phenyl)-1,3,4-oxadiazol-2-yl]amino]phenyl]methylamino]ethanol'>HOU</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=7dy7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7dy7 OCA], [https://pdbe.org/7dy7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7dy7 RCSB], [https://www.ebi.ac.uk/pdbsum/7dy7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7dy7 ProSAT]</span></td></tr>
	</table>		</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 ==
		+	Several monoclonal antibodies targeting the programmed cell death-1/programmed cell death-ligand 1 (PD-1/PD-L1) pathway have been used successfully in anticancer immunotherapy. Inherent limitations of antibody-based therapies remain, however, and alternative small-molecule inhibitors that can block the PD-1/PD-L1 axis are urgent needed. Herein, we report the discovery of compound 17 as a bifunctional inhibitor of PD-1/PD-L1 interactions. 17 inhibits PD-1/PD-L1 interactions and promotes dimerization, internalization, and degradation of PD-L1. 17 promotes cell-surface PD-L1 internalized into the cytosol and induces the degradation of PD-L1 in tumor cells through a lysosome-dependent pathway. Furthermore, 17 suppresses tumor growth in vivo by activating antitumor immunity. These results demonstrate that 17 targets the PD-1/PD-L1 axis and induces PD-L1 degradation.
		+
		+	Discovery of Small-Molecule Inhibitors of the PD-1/PD-L1 Axis That Promote PD-L1 Internalization and Degradation.,Wang T, Cai S, Cheng Y, Zhang W, Wang M, Sun H, Guo B, Li Z, Xiao Y, Jiang S J Med Chem. 2022 Mar 10;65(5):3879-3893. doi: 10.1021/acs.jmedchem.1c01682. Epub , 2022 Feb 21. PMID:35188766<ref>PMID:35188766</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 7dy7" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Cheng Y]]	+	[[Category: Cheng, Y]]
-	[[Category: Jiang S]]	+	[[Category: Jiang, S]]
-	[[Category: Lu ML]]	+	[[Category: Lu, M L]]
-	[[Category: Wang TY]]	+	[[Category: Wang, T Y]]
-	[[Category: Xiao YB]]	+	[[Category: Xiao, Y B]]
		+	[[Category: Complex]]
		+	[[Category: Dimer]]
		+	[[Category: Immune checkpoint]]
		+	[[Category: Immunosuppressant]]
		+	[[Category: Inhibitor]]

OCA at 06:59, 27 January 2022

OCA — Thu, 27 Jan 2022 06:59:48 GMT

←Older revision		Revision as of 06:59, 27 January 2022
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 7dy7 is ~~ON HOLD until Paper Publication~~	+	==Discovery of Novel Small-molecule Inhibitors of PD-1/PD-L1 Axis that Promotes PD-L1 Internalization and Degradation==
-		+	<StructureSection load='7dy7' size='340' side='right'caption='[[7dy7]]' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7DY7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7DY7 FirstGlance]. <br>
-	~~Description~~:	+	</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=7dy7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7dy7 OCA], [https://pdbe.org/7dy7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7dy7 RCSB], [https://www.ebi.ac.uk/pdbsum/7dy7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7dy7 ProSAT]</span></td></tr>
-	[[Category: ~~Unreleased Structures~~]]	+	</table>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Cheng Y]]
		+	[[Category: Jiang S]]
		+	[[Category: Lu ML]]
		+	[[Category: Wang TY]]
		+	[[Category: Xiao YB]]

OCA at 09:08, 10 February 2021

OCA — Wed, 10 Feb 2021 09:08:01 GMT

←Older revision		Revision as of 09:08, 10 February 2021
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 7dy7 is ON HOLD	+	The entry 7dy7 is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "7dy7" [edit=sysop:move=sysop]

OCA — Wed, 27 Jan 2021 06:42:17 GMT

Protected "7dy7" [edit=sysop:move=sysop]

←Older revision

Revision as of 06:42, 27 January 2021

OCA: New page: '''Unreleased structure''' The entry 7dy7 is ON HOLD Authors: Description: Category: Unreleased Structures

OCA — Wed, 27 Jan 2021 06:42:16 GMT

New page: '''Unreleased structure''' The entry 7dy7 is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 7dy7 is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]