7u3h - Revision history

OCA at 17:11, 18 October 2023

OCA — Wed, 18 Oct 2023 17:11:01 GMT

←Older revision		Revision as of 17:11, 18 October 2023
Line 4:		Line 4:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[7u3h]] 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=7U3H OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7U3H FirstGlance]. <br>		<table><tr><td colspan='2'>[[7u3h]] 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=7U3H OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7U3H FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=L6O:(5R)-N-(4-fluorophenyl)-5-methyl-4,5-dihydro-1,3-thiazol-2-amine'>L6O</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]] 1.798Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=L6O:(5R)-N-(4-fluorophenyl)-5-methyl-4,5-dihydro-1,3-thiazol-2-amine'>L6O</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=7u3h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7u3h OCA], [https://pdbe.org/7u3h PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7u3h RCSB], [https://www.ebi.ac.uk/pdbsum/7u3h PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7u3h 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=7u3h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7u3h OCA], [https://pdbe.org/7u3h PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7u3h RCSB], [https://www.ebi.ac.uk/pdbsum/7u3h PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7u3h ProSAT]</span></td></tr>
	</table>		</table>

OCA at 06:25, 26 October 2022

OCA — Wed, 26 Oct 2022 06:25:59 GMT

←Older revision		Revision as of 06:25, 26 October 2022
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 7u3h is ~~ON HOLD until Paper~~ Publication	+	==GID4 in complex with compound 7==
		+	<StructureSection load='7u3h' size='340' side='right'caption='[[7u3h]], [[Resolution\|resolution]] 1.80Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[7u3h]] 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=7U3H OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7U3H FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=L6O:(5R)-N-(4-fluorophenyl)-5-methyl-4,5-dihydro-1,3-thiazol-2-amine'>L6O</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=7u3h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7u3h OCA], [https://pdbe.org/7u3h PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7u3h RCSB], [https://www.ebi.ac.uk/pdbsum/7u3h PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7u3h ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[https://www.uniprot.org/uniprot/GID4_HUMAN GID4_HUMAN]
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Targeted protein degradation (TPD) strategies exploit bivalent small molecules to bridge substrate proteins to an E3 ubiquitin ligase to induce substrate degradation. Few E3s have been explored as degradation effectors due to a dearth of E3-binding small molecules. We show that genetically induced recruitment to the GID4 subunit of the CTLH E3 complex induces protein degradation. An NMR-based fragment screen followed by structure-guided analog elaboration identified two binders of GID4, 16 and 67, with Kd values of 110 and 17 muM in vitro. A parallel DNA-encoded library (DEL) screen identified five binders of GID4, the best of which, 88, had a Kd of 5.6 muM in vitro and an EC50 of 558 nM in cells with strong selectivity for GID4. X-ray co-structure determination revealed the basis for GID4-small molecule interactions. These results position GID4-CTLH as an E3 for TPD and provide candidate scaffolds for high-affinity moieties that bind GID4.

-	~~Authors~~:	+	Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4.,Chana CK, Maisonneuve P, Posternak G, Grinberg NGA, Poirson J, Ona SM, Ceccarelli DF, Mader P, St-Cyr DJ, Pau V, Kurinov I, Tang X, Deng D, Cui W, Su W, Kuai L, Soll R, Tyers M, Rost HL, Batey RA, Taipale M, Gingras AC, Sicheri F J Med Chem. 2022 Sep 18. doi: 10.1021/acs.jmedchem.2c00509. PMID:36117290<ref>PMID:36117290</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased~~ Structures]]	+	</div>
		+	<div class="pdbe-citations 7u3h" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Homo sapiens]]
		+	[[Category: Large Structures]]
		+	[[Category: Chana CK]]
		+	[[Category: Sicheri F]]

OCA: Protected "7u3h" [edit=sysop:move=sysop]

OCA — Wed, 09 Mar 2022 04:55:35 GMT

Protected "7u3h" [edit=sysop:move=sysop]

←Older revision

Revision as of 04:55, 9 March 2022

OCA: New page: '''Unreleased structure''' The entry 7u3h is ON HOLD until Paper Publication Authors: Description: Category: Unreleased Structures

OCA — Wed, 09 Mar 2022 04:55:34 GMT

New page: '''Unreleased structure''' The entry 7u3h is ON HOLD until Paper Publication Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 7u3h is ON HOLD until Paper Publication

Authors:

Description:
[[Category: Unreleased Structures]]