7np2 - Revision history

OCA at 12:37, 1 February 2024

OCA — Thu, 01 Feb 2024 12:37:54 GMT

←Older revision		Revision as of 12:37, 1 February 2024
Line 1:		Line 1:

-	====	+	==Crystal structure of 14-3-3 sigma in complex with 20mer Amot-p130 peptide==
-	<StructureSection load='7np2' size='340' side='right'caption='[[7np2]]' scene=''>	+	<StructureSection load='7np2' size='340' side='right'caption='[[7np2]], [[Resolution\|resolution]] 1.27Å' 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'>[[7np2]] 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=7NP2 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7NP2 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=7np2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7np2 OCA], [https://pdbe.org/7np2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7np2 RCSB], [https://www.ebi.ac.uk/pdbsum/7np2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7np2 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]] 1.27Å</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=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</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=7np2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7np2 OCA], [https://pdbe.org/7np2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7np2 RCSB], [https://www.ebi.ac.uk/pdbsum/7np2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7np2 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 ==
		+	The modulation of protein-protein interactions (PPIs) has developed into a well-established field of drug discovery. Despite the advances achieved in the field, many PPIs are still deemed as 'undruggable' targets and the design of PPIs stabilizers remains a significant challenge. The application of fragment-based methods for the identification of drug leads and to evaluate the 'tractability' of the desired protein target has seen a remarkable development in recent years. In this study, we explore the molecular characteristics of the 14-3-3/Amot-p130 PPI and the conceptual possibility of targeting this interface using X-ray crystallography fragment-based screening. We report the first structural elucidation of the 14-3-3 binding motif of Amot-p130 and the characterization of the binding mode and affinities involved. We made use of fragments to probe the 'ligandability' of the 14-3-3/Amot-p130 composite binding pocket. Here we disclose initial hits with promising stabilizing activity and an early-stage selectivity toward the Amot-p130 motifs over other representatives 14-3-3 partners. Our findings highlight the potential of using fragments to characterize and explore proteins' surfaces and might provide a starting point toward the development of small molecules capable of acting as molecular glues.
		+
		+	Fragment-based exploration of the 14-3-3/Amot-p130 interface.,Centorrino F, Andlovic B, Cossar P, Brunsveld L, Ottmann C Curr Res Struct Biol. 2021 Dec 29;4:21-28. doi: 10.1016/j.crstbi.2021.12.003. , eCollection 2022. PMID:35036934<ref>PMID:35036934</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 7np2" 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: Centorrino F]]
		+	[[Category: Ottmann C]]

OCA at 09:57, 12 January 2022

OCA — Wed, 12 Jan 2022 09:57:43 GMT

←Older revision		Revision as of 09:57, 12 January 2022
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 7np2 ~~is ON HOLD until Paper Publication~~	+	====
-		+	<StructureSection load='7np2' size='340' side='right'caption='[[7np2]]' scene=''>
-	~~Authors~~: ~~Centorrino, F~~.~~, Ottmann, C~~.	+	== 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~~: ~~Crystal structure of 14~~-~~3-3 sigma in complex with 20mer Amot-p130 peptide~~	+	</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=7np2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7np2 OCA], [https://pdbe.org/7np2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7np2 RCSB], [https://www.ebi.ac.uk/pdbsum/7np2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7np2 ProSAT]</span></td></tr>
-	[[~~Category~~: ~~Unreleased Structures~~]]	+	</table>
-	[[Category: ~~Ottmann, C~~]]	+	__TOC__
-	[[Category: ~~Centorrino, F~~]]	+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Z-disk]]

OCA at 09:29, 31 March 2021

OCA — Wed, 31 Mar 2021 09:29:11 GMT

←Older revision		Revision as of 09:29, 31 March 2021
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 7np2 is ON HOLD	+	The entry 7np2 is ON HOLD until Paper Publication

	Authors: Centorrino, F., Ottmann, C.		Authors: Centorrino, F., Ottmann, C.

OCA: Protected "7np2" [edit=sysop:move=sysop]

OCA — Wed, 10 Mar 2021 15:00:16 GMT

Protected "7np2" [edit=sysop:move=sysop]

←Older revision

Revision as of 15:00, 10 March 2021

OCA: New page: '''Unreleased structure''' The entry 7np2 is ON HOLD Authors: Centorrino, F., Ottmann, C. Description: Crystal structure of 14-3-3 sigma in complex with 20mer Amot-p130 peptide [[Categ...

OCA — Wed, 10 Mar 2021 15:00:15 GMT

New page: '''Unreleased structure''' The entry 7np2 is ON HOLD Authors: Centorrino, F., Ottmann, C. Description: Crystal structure of 14-3-3 sigma in complex with 20mer Amot-p130 peptide [[Categ...

New page

'''Unreleased structure'''

The entry 7np2 is ON HOLD

Authors: Centorrino, F., Ottmann, C.

Description: Crystal structure of 14-3-3 sigma in complex with 20mer Amot-p130 peptide
[[Category: Unreleased Structures]]
[[Category: Ottmann, C]]
[[Category: Centorrino, F]]