6iiv - Revision history

OCA at 09:43, 22 November 2023

OCA — Wed, 22 Nov 2023 09:43:22 GMT

←Older revision		Revision as of 09:43, 22 November 2023
Line 1:		Line 1:

	==Crystal structure of the human thromboxane A2 receptor bound to daltroban==		==Crystal structure of the human thromboxane A2 receptor bound to daltroban==
-	<StructureSection load='6iiv' size='340' side='right' caption='[[6iiv]], [[Resolution\|resolution]] 3.00Å' scene=''>	+	<StructureSection load='6iiv' size='340' side='right'caption='[[6iiv]], [[Resolution\|resolution]] 3.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6iiv]] is a 1 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~"bacillus_coli"_migula_1895 "bacillus~~ coli~~" migula 1895~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6IIV OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6IIV FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6iiv]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Clostridium_pasteurianum Clostridium pasteurianum], [https://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6IIV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6IIV FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=A90:2-[4-[2-[(4-chlorophenyl)sulfonylamino]ethyl]phenyl]ethanoic+acid'>A90</scene>, <scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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]] 3Å</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">TBXA2R ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=562 "Bacillus coli" Migula 1895])</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=A90:2-[4-[2-[(4-chlorophenyl)sulfonylamino]ethyl]phenyl]ethanoic+acid'>A90</scene>, <scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
-	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6iiv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6iiv OCA], [~~http~~://pdbe.org/6iiv PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=6iiv RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/6iiv PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=6iiv 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=6iiv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6iiv OCA], [https://pdbe.org/6iiv PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6iiv RCSB], [https://www.ebi.ac.uk/pdbsum/6iiv PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6iiv ProSAT]</span></td></tr>
	</table>		</table>
		+	== Disease ==
		+	[https://www.uniprot.org/uniprot/TA2R_HUMAN TA2R_HUMAN] Bleeding diathesis due to thromboxane synthesis deficiency. Disease susceptibility is associated with variants affecting the gene represented in this entry.
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX]] Electron-transport protein of unknown function.	+	[https://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX] Electron-transport protein of unknown function.[https://www.uniprot.org/uniprot/TA2R_HUMAN TA2R_HUMAN] Receptor for thromboxane A2 (TXA2), a potent stimulator of platelet aggregation. The activity of this receptor is mediated by a G-protein that activates a phosphatidylinositol-calcium second messenger system. In the kidney, the binding of TXA2 to glomerular TP receptors causes intense vasoconstriction. Activates phospholipase C.<ref>PMID:8613548</ref> Activates adenylyl cyclase.<ref>PMID:8613548</ref> Inhibits adenylyl cyclase.<ref>PMID:8613548</ref> [https://www.uniprot.org/uniprot/RUBR_CLOPA RUBR_CLOPA] Rubredoxin is a small nonheme, iron protein lacking acid-labile sulfide. Its single Fe, chelated to 4 Cys, functions as an electron acceptor and may also stabilize the conformation of the molecule.
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 23:		Line 25:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Bacillus coli migula 1895~~]]	+	[[Category: Clostridium pasteurianum]]
-	[[Category: ~~Fan, H~~]]	+	[[Category: Escherichia coli]]
-	[[Category: ~~Wu, B~~]]	+	[[Category: Homo sapiens]]
-	[[Category: ~~Zhao, Q~~]]	+	[[Category: Large Structures]]
-	[[Category: ~~Antagonist~~]]	+	[[Category: Fan H]]
-	[[Category: ~~Complex~~]]	+	[[Category: Wu B]]
-	[[Category: ~~Gpcr]]~~	+	[[Category: Zhao Q]]
-	~~[[Category: Signaling protein~~]]	+

OCA at 08:45, 26 December 2018

OCA — Wed, 26 Dec 2018 08:45:50 GMT

←Older revision

Revision as of 08:45, 26 December 2018

OCA at 08:32, 19 December 2018

OCA — Wed, 19 Dec 2018 08:32:18 GMT

←Older revision		Revision as of 08:32, 19 December 2018
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 6iiv is ~~ON HOLD until Paper~~ Publication	+	==Crystal structure of the human thromboxane A2 receptor bound to daltroban==
		+	<StructureSection load='6iiv' size='340' side='right' caption='[[6iiv]], [[Resolution\|resolution]] 3.00Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[6iiv]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6IIV OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6IIV FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=A90:2-[4-[2-[(4-chlorophenyl)sulfonylamino]ethyl]phenyl]ethanoic+acid'>A90</scene>, <scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
		+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6iiv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6iiv OCA], [http://pdbe.org/6iiv PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6iiv RCSB], [http://www.ebi.ac.uk/pdbsum/6iiv PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6iiv ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/C562_ECOLX C562_ECOLX]] Electron-transport protein of unknown function.
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Stimulated by thromboxane A2, an endogenous arachidonic acid metabolite, the thromboxane A2 receptor (TP) plays a pivotal role in cardiovascular homeostasis, and thus is considered as an important drug target for cardiovascular disease. Here, we report crystal structures of the human TP bound to two nonprostanoid antagonists, ramatroban and daltroban, at 2.5 A and 3.0 A resolution, respectively. The TP structures reveal a ligand-binding pocket capped by two layers of extracellular loops that are stabilized by two disulfide bonds, limiting ligand access from the extracellular milieu. These structures provide details of interactions between the receptor and antagonists, which help to integrate previous mutagenesis and SAR data. Molecular docking of prostanoid-like ligands, combined with mutagenesis, ligand-binding and functional assays, suggests a prostanoid binding mode that may also be adopted by other prostanoid receptors. These insights into TP deepen our understanding about ligand recognition and selectivity mechanisms of this physiologically important receptor.

-	~~Authors~~:	+	Structural basis for ligand recognition of the human thromboxane A2 receptor.,Fan H, Chen S, Yuan X, Han S, Zhang H, Xia W, Xu Y, Zhao Q, Wu B Nat Chem Biol. 2019 Jan;15(1):27-33. doi: 10.1038/s41589-018-0170-9. Epub 2018, Dec 3. PMID:30510189<ref>PMID:30510189</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased Structures~~]]	+	</div>
		+	<div class="pdbe-citations 6iiv" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Fan, H]]
		+	[[Category: Wu, B]]
		+	[[Category: Zhao, Q]]
		+	[[Category: Antagonist]]
		+	[[Category: Complex]]
		+	[[Category: Gpcr]]
		+	[[Category: Signaling protein]]

OCA at 18:49, 2 December 2018

OCA — Sun, 02 Dec 2018 18:49:27 GMT

←Older revision		Revision as of 18:49, 2 December 2018
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

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

	Authors:		Authors:

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

OCA — Wed, 17 Oct 2018 06:25:14 GMT

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

←Older revision

Revision as of 06:25, 17 October 2018

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

OCA — Wed, 17 Oct 2018 06:25:12 GMT

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

New page

'''Unreleased structure'''

The entry 6iiv is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]