6r5l - Revision history

OCA at 12:15, 24 January 2024

2024-01-24T12:15:39Z

←Older revision		Revision as of 12:15, 24 January 2024
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	<StructureSection load='6r5l' size='340' side='right'caption='[[6r5l]], [[Resolution\|resolution]] 1.88Å' scene=''>		<StructureSection load='6r5l' size='340' side='right'caption='[[6r5l]], [[Resolution\|resolution]] 1.88Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6r5l]] is a 2 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~Human Human~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6R5L OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=6R5L FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6r5l]] 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=6R5L OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6R5L FirstGlance]. <br>
-	</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=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=JT2:4-[[(2~{S})-1-azanylpropan-2-yl]amino]-6-(sulfanylmethyl)-1-benzothiophene-2-carboximidamide'>JT2</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</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]] 1.884Å</td></tr>
-	~~<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat">~~<scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene>~~</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=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=JT2:4-[[(2~{S})-1-azanylpropan-2-yl]amino]-6-(sulfanylmethyl)-1-benzothiophene-2-carboximidamide'>JT2</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
-	~~<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">SFN, HME1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])~~</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=6r5l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6r5l OCA], [https://pdbe.org/6r5l PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6r5l RCSB], [https://www.ebi.ac.uk/pdbsum/6r5l PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6r5l ProSAT]</span></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=6r5l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6r5l OCA], [~~http~~://pdbe.org/6r5l PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=6r5l RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/6r5l PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=6r5l ProSAT]</span></td></tr>	+
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://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.	+	[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;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
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	</div>		</div>
	<div class="pdbe-citations 6r5l" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 6r5l" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[14-3-3 protein 3D structures\|14-3-3 protein 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Castaldi, P]]	+	[[Category: Castaldi P]]
-	[[Category: Genet, S]]	+	[[Category: Genet S]]
-	[[Category: Guillory, X]]	+	[[Category: Guillory X]]
-	[[Category: Leysen, S]]	+	[[Category: Leysen S]]
-	[[Category: Ottmann, C]]	+	[[Category: Ottmann C]]
-	[[Category: Somsen, B]]	+	[[Category: Somsen B]]
-	[[Category: Wolter, M]]	+	[[Category: Wolter M]]
-	~~[[Category: Fragment soaking]]~~	+
-	~~[[Category: Peptide binding protein]]~~	+
-	~~[[Category: Protein protein interaction]]~~	+
-	~~[[Category: Stabilization~~]]	+

OCA at 11:23, 22 July 2020

2020-07-22T11:23:44Z

←Older revision		Revision as of 11:23, 22 July 2020
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	==Fragment AZ-006 binding at the p53pT387/14-3-3 sigma interface==		==Fragment AZ-006 binding at the p53pT387/14-3-3 sigma interface==
-	<StructureSection load='6r5l' size='340' side='right'caption='[[6r5l]]' scene=''>	+	<StructureSection load='6r5l' size='340' side='right'caption='[[6r5l]], [[Resolution\|resolution]] 1.88Å' 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=6R5L OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6R5L FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6r5l]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6R5L OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6R5L 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=6r5l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6r5l OCA], [http://pdbe.org/6r5l PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6r5l RCSB], [http://www.ebi.ac.uk/pdbsum/6r5l PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6r5l 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=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=JT2:4-[[(2~{S})-1-azanylpropan-2-yl]amino]-6-(sulfanylmethyl)-1-benzothiophene-2-carboximidamide'>JT2</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
		+	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">SFN, HME1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=6r5l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6r5l OCA], [http://pdbe.org/6r5l PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6r5l RCSB], [http://www.ebi.ac.uk/pdbsum/6r5l PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6r5l ProSAT]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[[http://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 ==
		+	Stabilization of protein-protein interactions (PPIs) holds great potential for therapeutic agents, as illustrated by the successful drugs rapamycin and lenalidomide. However, how such interface-binding molecules can be created in a rational, bottom-up manner is a largely unanswered question. We report here how a fragment-based approach can be used to identify chemical starting points for the development of small-molecule stabilizers that differentiate between two different PPI interfaces of the adapter protein 14-3-3. The fragments discriminately bind to the interface of 14-3-3 with the recognition motif of either the tumor suppressor protein p53 or the oncogenic transcription factor TAZ. This x-ray crystallography driven study shows that the rim of the interface of individual 14-3-3 complexes can be targeted in a differential manner with fragments that represent promising starting points for the development of specific 14-3-3 PPI stabilizers.
		+
		+	Fragment-based Differential Targeting of PPI Stabilizer Interfaces.,Guillory X, Wolter M, Leysen S, Neves JF, Kuusk A, Genet S, Somsen B, Morrow J, Rivers E, van Beek L, Patel J, Goodnow R, Schoenherr H, Fuller N, Cao Q, Doveston RG, Brunsveld L, Arkin MR, Castaldi MP, Boyd H, Landrieu I, Chen H, Ottmann C J Med Chem. 2020 Jun 5. doi: 10.1021/acs.jmedchem.9b01942. PMID:32501690<ref>PMID:32501690</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 6r5l" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Castaldi P]]	+	[[Category: Castaldi, P]]
-	[[Category: Genet S]]	+	[[Category: Genet, S]]
-	[[Category: Guillory X]]	+	[[Category: Guillory, X]]
-	[[Category: Leysen S]]	+	[[Category: Leysen, S]]
-	[[Category: Ottmann C]]	+	[[Category: Ottmann, C]]
-	[[Category: Somsen B]]	+	[[Category: Somsen, B]]
-	[[Category: Wolter M]]	+	[[Category: Wolter, M]]
		+	[[Category: Fragment soaking]]
		+	[[Category: Peptide binding protein]]
		+	[[Category: Protein protein interaction]]
		+	[[Category: Stabilization]]

OCA at 10:10, 17 June 2020

2020-06-17T10:10:20Z

←Older revision		Revision as of 10:10, 17 June 2020
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 6r5l is ~~ON HOLD until Paper Publication~~	+	==Fragment AZ-006 binding at the p53pT387/14-3-3 sigma interface==
-		+	<StructureSection load='6r5l' size='340' side='right'caption='[[6r5l]]' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6R5L OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6R5L FirstGlance]. <br>
-	~~Description~~:	+	</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=6r5l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6r5l OCA], [http://pdbe.org/6r5l PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6r5l RCSB], [http://www.ebi.ac.uk/pdbsum/6r5l PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6r5l ProSAT]</span></td></tr>
-	[[Category: ~~Unreleased Structures~~]]	+	</table>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Castaldi P]]
		+	[[Category: Genet S]]
		+	[[Category: Guillory X]]
		+	[[Category: Leysen S]]
		+	[[Category: Ottmann C]]
		+	[[Category: Somsen B]]
		+	[[Category: Wolter M]]

OCA at 05:38, 10 April 2019

2019-04-10T05:38:32Z

←Older revision		Revision as of 05:38, 10 April 2019
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 6r5l is ON HOLD	+	The entry 6r5l is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "6r5l" [edit=sysop:move=sysop]

2019-04-03T04:59:21Z

Protected "6r5l" [edit=sysop:move=sysop]

←Older revision

Revision as of 04:59, 3 April 2019

OCA: New page: '''Unreleased structure''' The entry 6r5l is ON HOLD Authors: Description: Category: Unreleased Structures

2019-04-03T04:59:18Z

New page: '''Unreleased structure''' The entry 6r5l is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 6r5l is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]