7cek - Revision history

OCA at 16:06, 29 November 2023

2023-11-29T16:06:57Z

←Older revision		Revision as of 16:06, 29 November 2023
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	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[7cek]] is a 6 chain structure with sequence from [https://en.wikipedia.org/wiki/Gallus_gallus Gallus gallus], [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] and [https://en.wikipedia.org/wiki/Sus_scrofa Sus scrofa]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7CEK OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7CEK FirstGlance]. <br>		<table><tr><td colspan='2'>[[7cek]] is a 6 chain structure with sequence from [https://en.wikipedia.org/wiki/Gallus_gallus Gallus gallus], [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] and [https://en.wikipedia.org/wiki/Sus_scrofa Sus scrofa]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7CEK OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7CEK FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ACP:PHOSPHOMETHYLPHOSPHONIC+ACID+ADENYLATE+ESTER'>ACP</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=FW9:N4-(1,3-benzodioxol-5-ylmethyl)-6-(3-methoxyphenyl)pyrimidine-2,4-diamine'>FW9</scene>, <scene name='pdbligand=GDP:GUANOSINE-5-DIPHOSPHATE'>GDP</scene>, <scene name='pdbligand=GTP:GUANOSINE-5-TRIPHOSPHATE'>GTP</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</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]] 2.696Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ACP:PHOSPHOMETHYLPHOSPHONIC+ACID+ADENYLATE+ESTER'>ACP</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=FW9:N4-(1,3-benzodioxol-5-ylmethyl)-6-(3-methoxyphenyl)pyrimidine-2,4-diamine'>FW9</scene>, <scene name='pdbligand=GDP:GUANOSINE-5-DIPHOSPHATE'>GDP</scene>, <scene name='pdbligand=GTP:GUANOSINE-5-TRIPHOSPHATE'>GTP</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</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=7cek FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7cek OCA], [https://pdbe.org/7cek PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7cek RCSB], [https://www.ebi.ac.uk/pdbsum/7cek PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7cek 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=7cek FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7cek OCA], [https://pdbe.org/7cek PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7cek RCSB], [https://www.ebi.ac.uk/pdbsum/7cek PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7cek ProSAT]</span></td></tr>
	</table>		</table>

OCA at 20:19, 16 November 2022

2022-11-16T20:19:51Z

←Older revision		Revision as of 20:19, 16 November 2022
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-	====	+	==Crystal structure of T2R-TTL-BML-284 complex==
-	<StructureSection load='7cek' size='340' side='right'caption='[[7cek]]' scene=''>	+	<StructureSection load='7cek' size='340' side='right'caption='[[7cek]], [[Resolution\|resolution]] 2.70Å' 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'>[[7cek]] is a 6 chain structure with sequence from [https://en.wikipedia.org/wiki/Gallus_gallus Gallus gallus], [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] and [https://en.wikipedia.org/wiki/Sus_scrofa Sus scrofa]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7CEK OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7CEK 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=7cek FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7cek OCA], [https://pdbe.org/7cek PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7cek RCSB], [https://www.ebi.ac.uk/pdbsum/7cek PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7cek 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=ACP:PHOSPHOMETHYLPHOSPHONIC+ACID+ADENYLATE+ESTER'>ACP</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=FW9:N4-(1,3-benzodioxol-5-ylmethyl)-6-(3-methoxyphenyl)pyrimidine-2,4-diamine'>FW9</scene>, <scene name='pdbligand=GDP:GUANOSINE-5-DIPHOSPHATE'>GDP</scene>, <scene name='pdbligand=GTP:GUANOSINE-5-TRIPHOSPHATE'>GTP</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</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=7cek FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7cek OCA], [https://pdbe.org/7cek PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7cek RCSB], [https://www.ebi.ac.uk/pdbsum/7cek PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7cek ProSAT]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[https://www.uniprot.org/uniprot/TBA1B_PIG TBA1B_PIG] Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Here, we report a novel mechanism to selectively degrade target proteins. 3-(3-Phenoxybenzyl)amino-beta-carboline (PAC), a tubulin inhibitor, promotes selective degradation of alphabeta-tubulin heterodimers. Biochemical studies have revealed that PAC specifically denatures tubulin, making it prone to aggregation that predisposes it to ubiquitinylation and then degradation. The degradation is mediated by a single hydrogen bond formed between the pyridine nitrogen of PAC and betaGlu198, which is identified as a low-barrier hydrogen bond (LBHB). In contrast, another two tubulin inhibitors that only form normal hydrogen bonds with betaGlu198 exhibit no degradation effect. Thus, the LBHB accounts for the degradation. We then screened for compounds capable of forming an LBHB with betaGlu198 and demonstrated that BML284, a Wnt signaling activator, also promotes tubulin heterodimer degradation through the LBHB. Our study provided a unique example of LBHB function and identified a novel approach to obtain tubulin degraders.
		+
		+	Small Molecules Promote Selective Denaturation and Degradation of Tubulin Heterodimers through a Low-Barrier Hydrogen Bond.,Yang J, Li Y, Qiu Q, Wang R, Yan W, Yu Y, Niu L, Pei H, Wei H, Ouyang L, Ye H, Xu D, Wei Y, Chen Q, Chen L J Med Chem. 2022 Jul 14;65(13):9159-9173. doi: 10.1021/acs.jmedchem.2c00379. Epub, 2022 Jun 28. PMID:35762925<ref>PMID:35762925</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 7cek" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Tubulin 3D Structures\|Tubulin 3D Structures]]
		+	*[[Tubulin tyrosine ligase\|Tubulin tyrosine ligase]]
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Gallus gallus]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: ~~Z-disk~~]]	+	[[Category: Rattus norvegicus]]
		+	[[Category: Sus scrofa]]
		+	[[Category: Chen LJ]]
		+	[[Category: Chen Q]]
		+	[[Category: Yang JH]]
		+	[[Category: Yu Y]]

OCA at 07:29, 25 June 2021

2021-06-25T07:29:50Z

←Older revision		Revision as of 07:29, 25 June 2021
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-	'''Unreleased structure'''

-	~~The entry~~ 7cek ~~is ON HOLD until Paper Publication~~	+	====
-		+	<StructureSection load='7cek' size='340' side='right'caption='[[7cek]]' scene=''>
-	~~Authors~~: ~~Chen, L~~.J.~~, Chen, Q~~.~~, Yu, Y~~.~~, Yang, J~~.H.	+	== 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 T2R-TTL-BML-284 complex~~	+	</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=7cek FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7cek OCA], [https://pdbe.org/7cek PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7cek RCSB], [https://www.ebi.ac.uk/pdbsum/7cek PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7cek ProSAT]</span></td></tr>
-	[~~[Category~~: ~~Unreleased Structures~~]]	+	</table>
-	[~~[Category~~: ~~Yu, Y~~]]	+	__TOC__
-	[~~[Category~~: ~~Yang~~, J.H]]	+	</StructureSection>
-	[[Category: ~~Chen, Q~~]]	+	[[Category: Large Structures]]
-	[[Category: ~~Chen, L.J~~]]	+	[[Category: Z-disk]]

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

2020-07-08T11:28:08Z

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

←Older revision

Revision as of 11:28, 8 July 2020

OCA: New page: '''Unreleased structure''' The entry 7cek is ON HOLD until Paper Publication Authors: Chen, L.J., Chen, Q., Yu, Y., Yang, J.H. Description: Crystal structure of T2R-TTL-BML-284 complex...

2020-07-08T11:28:07Z

New page: '''Unreleased structure''' The entry 7cek is ON HOLD until Paper Publication Authors: Chen, L.J., Chen, Q., Yu, Y., Yang, J.H. Description: Crystal structure of T2R-TTL-BML-284 complex...

New page

'''Unreleased structure'''

The entry 7cek is ON HOLD until Paper Publication

Authors: Chen, L.J., Chen, Q., Yu, Y., Yang, J.H.

Description: Crystal structure of T2R-TTL-BML-284 complex
[[Category: Unreleased Structures]]
[[Category: Yu, Y]]
[[Category: Yang, J.H]]
[[Category: Chen, Q]]
[[Category: Chen, L.J]]