OCA at 12:45, 1 February 2024

OCA — Thu, 01 Feb 2024 12:45:00 GMT

←Older revision		Revision as of 12:45, 1 February 2024
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-	====	+	==14-3-3 sigma with RelA/p65 binding site pS45 and covalently bound TCF521-158==
-	<StructureSection load='7o5a' size='340' side='right'caption='[[7o5a]]' scene=''>	+	<StructureSection load='7o5a' size='340' side='right'caption='[[7o5a]], [[Resolution\|resolution]] 1.80Å' 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= OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol= FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[7o5a]] 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=7O5A OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7O5A 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=7o5a FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7o5a OCA], [https://pdbe.org/7o5a PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7o5a RCSB], [https://www.ebi.ac.uk/pdbsum/7o5a PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7o5a ProSAT]</span></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]] 1.8Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=CSO:S-HYDROXYCYSTEINE'>CSO</scene>, <scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=V2Q:4-(3-methoxyazetidin-1-yl)carbonylbenzaldehyde'>V2Q</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=7o5a FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7o5a OCA], [https://pdbe.org/7o5a PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7o5a RCSB], [https://www.ebi.ac.uk/pdbsum/7o5a PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7o5a ProSAT]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[https://www.uniprot.org/uniprot/1433S_HUMAN 1433S_HUMAN] Adapter protein implicated in the regulation of a large spectrum of both general and specialized signaling pathways. Binds to a large number of partners, usually by recognition of a phosphoserine or phosphothreonine motif. Binding generally results in the modulation of the activity of the binding partner. When bound to KRT17, regulates protein synthesis and epithelial cell growth by stimulating Akt/mTOR pathway (By similarity). p53-regulated inhibitor of G2/M progression.
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Protein-protein modulation has emerged as a proven approach to drug discovery. While significant progress has been gained in developing protein-protein interaction (PPI) inhibitors, the orthogonal approach of PPI stabilization lacks established methodologies for drug design. Here, we report the systematic ''bottom-up'' development of a reversible covalent PPI stabilizer. An imine bond was employed to anchor the stabilizer at the interface of the 14-3-3/p65 complex, leading to a molecular glue that elicited an 81-fold increase in complex stabilization. Utilizing protein crystallography and biophysical assays, we deconvoluted how chemical properties of a stabilizer translate to structural changes in the ternary 14-3-3/p65/molecular glue complex. Furthermore, we explore how this leads to high cooperativity and increased stability of the complex.
		+
		+	An Exploration of Chemical Properties Required for Cooperative Stabilization of the 14-3-3 Interaction with NF-kappaB-Utilizing a Reversible Covalent Tethering Approach.,Wolter M, Valenti D, Cossar PJ, Hristeva S, Levy LM, Genski T, Hoffmann T, Brunsveld L, Tzalis D, Ottmann C J Med Chem. 2021 Jun 24;64(12):8423-8436. doi: 10.1021/acs.jmedchem.1c00401. Epub , 2021 Jun 2. PMID:34076416<ref>PMID:34076416</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 7o5a" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[14-3-3 protein 3D structures\|14-3-3 protein 3D structures]]
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: ~~Z-disk~~]]	+	[[Category: Ottmann C]]
		+	[[Category: Wolter M]]

OCA at 12:15, 9 June 2021

OCA — Wed, 09 Jun 2021 12:15:23 GMT

←Older revision		Revision as of 12:15, 9 June 2021
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-	'''Unreleased structure'''

-	~~The entry~~ 7o5a ~~is ON HOLD until Paper Publication~~	+	====
-		+	<StructureSection load='7o5a' size='340' side='right'caption='[[7o5a]]' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id= OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol= 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=7o5a FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7o5a OCA], [https://pdbe.org/7o5a PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7o5a RCSB], [https://www.ebi.ac.uk/pdbsum/7o5a PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7o5a ProSAT]</span></td></tr>
-	[[Category: ~~Unreleased~~ Structures]]	+	</table>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Z-disk]]

OCA at 08:18, 12 May 2021

OCA — Wed, 12 May 2021 08:18:52 GMT

←Older revision		Revision as of 08:18, 12 May 2021
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 7o5a is ON HOLD	+	The entry 7o5a is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "7o5a" [edit=sysop:move=sysop]

OCA — Wed, 14 Apr 2021 05:51:23 GMT

Protected "7o5a" [edit=sysop:move=sysop]

←Older revision

Revision as of 05:51, 14 April 2021

OCA: New page: '''Unreleased structure''' The entry 7o5a is ON HOLD Authors: Description: Category: Unreleased Structures

OCA — Wed, 14 Apr 2021 05:51:22 GMT

New page: '''Unreleased structure''' The entry 7o5a is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 7o5a is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]

7o5a - Revision history

OCA at 12:45, 1 February 2024

OCA at 12:15, 9 June 2021

OCA at 08:18, 12 May 2021

OCA: Protected "7o5a" [edit=sysop:move=sysop]

OCA: New page: '''Unreleased structure''' The entry 7o5a is ON HOLD Authors: Description: Category: Unreleased Structures