4xt2 - Revision history

OCA at 07:49, 27 September 2023

2023-09-27T07:49:02Z

← Older revision		Revision as of 07:49, 27 September 2023
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	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4xt2]] is a 4 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=4XT2 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4XT2 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4xt2]] is a 4 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=4XT2 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4XT2 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=43L:(5S,7R)-5,7-BIS(3-BROMOPHENYL)-4,5,6,7-TETRAHYDROTETRAZOLO[1,5-A]PYRIMIDINE'>43L</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]] 1.698Å</td></tr>
			<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=43L:(5S,7R)-5,7-BIS(3-BROMOPHENYL)-4,5,6,7-TETRAHYDROTETRAZOLO[1,5-A]PYRIMIDINE'>43L</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=4xt2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xt2 OCA], [https://pdbe.org/4xt2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4xt2 RCSB], [https://www.ebi.ac.uk/pdbsum/4xt2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4xt2 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=4xt2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xt2 OCA], [https://pdbe.org/4xt2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4xt2 RCSB], [https://www.ebi.ac.uk/pdbsum/4xt2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4xt2 ProSAT]</span></td></tr>
	</table>		</table>

OCA at 17:50, 26 April 2023

2023-04-26T17:50:56Z

← Older revision		Revision as of 17:50, 26 April 2023
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	<StructureSection load='4xt2' size='340' side='right'caption='[[4xt2]], [[Resolution\|resolution]] 1.70Å' scene=''>		<StructureSection load='4xt2' size='340' side='right'caption='[[4xt2]], [[Resolution\|resolution]] 1.70Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4xt2]] is a 4 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=4XT2 OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4XT2 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4xt2]] is a 4 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=4XT2 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4XT2 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=43L:(5S,7R)-5,7-BIS(3-BROMOPHENYL)-4,5,6,7-TETRAHYDROTETRAZOLO[1,5-A]PYRIMIDINE'>43L</scene>~~</td></tr>~~		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=43L:(5S,7R)-5,7-BIS(3-BROMOPHENYL)-4,5,6,7-TETRAHYDROTETRAZOLO[1,5-A]PYRIMIDINE'>43L</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3f1p\|3f1p]], [[3f1o\|3f1o]], [[3hw7\|3hw7]], [[3h82\|3h82]], [[4ghi\|4ghi]], [[4gs9\|4gs9]], [[4lpz\|4lpz]]</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=4xt2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xt2 OCA], [https://pdbe.org/4xt2 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4xt2 RCSB], [https://www.ebi.ac.uk/pdbsum/4xt2 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4xt2 ProSAT]</span></td></tr>
	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ARNT, BHLHE2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN]), EPAS1, BHLHE73, HIF2A, MOP2, PASD2 ([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~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4xt2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xt2 OCA], [~~http~~://pdbe.org/4xt2 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4xt2 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4xt2 PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4xt2 ProSAT]</span></td></tr>
	</table>		</table>
	~~== Disease ==~~
	[[http://www.uniprot.org/uniprot/EPAS1_HUMAN EPAS1_HUMAN]] Defects in EPAS1 are the cause of familial erythrocytosis type 4 (ECYT4) [MIM:[http://omim.org/entry/611783 611783]]. ECYT4 is an autosomal dominant disorder characterized by increased serum red blood cell mass, elevated hemoglobin concentration and hematocrit, and normal platelet and leukocyte counts.<ref>PMID:19208626</ref> <ref>PMID:18378852</ref> <ref>PMID:18184961</ref> <ref>PMID:22367913</ref>
	== Function ==		== Function ==
	[~~[http~~://www.uniprot.org/uniprot/ARNT_HUMAN ARNT_HUMAN]] Required for activity of the Ah (dioxin) receptor. This protein is required for the ligand-binding subunit to translocate from the cytosol to the nucleus after ligand binding. The complex then initiates transcription of genes involved in the activation of PAH procarcinogens. The heterodimer with HIF1A or EPAS1/HIF2A functions as a transcriptional regulator of the adaptive response to hypoxia. [[http://www.uniprot.org/uniprot/EPAS1_HUMAN EPAS1_HUMAN]] Transcription factor involved in the induction of oxygen regulated genes. Binds to core DNA sequence 5'-[AG]CGTG-3' within the hypoxia response element (HRE) of target gene promoters. Regulates the vascular endothelial growth factor (VEGF) expression and seems to be implicated in the development of blood vessels and the tubular system of lung. May also play a role in the formation of the endothelium that gives rise to the blood brain barrier. Potent activator of the Tie-2 tyrosine kinase expression. Activation seems to require recruitment of transcriptional coactivators such as CREBPB and probably EP300. Interaction with redox regulatory protein APEX seems to activate CTAD.		[https://www.uniprot.org/uniprot/ARNT_HUMAN ARNT_HUMAN] Required for activity of the Ah (dioxin) receptor. This protein is required for the ligand-binding subunit to translocate from the cytosol to the nucleus after ligand binding. The complex then initiates transcription of genes involved in the activation of PAH procarcinogens. The heterodimer with HIF1A or EPAS1/HIF2A functions as a transcriptional regulator of the adaptive response to hypoxia.
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: ~~Human~~]]		[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: Gardner~~, K H~~]]		[[Category: Gardner KH]]
	[[Category: Scheuermann~~, T H]]~~		[[Category: Scheuermann TH]]
	~~[[Category: Cancer]]~~
	~~[[Category: Hypoxia inducible factor]]~~
	~~[[Category: Inhibitor]]~~
	~~[[Category: Transcription]]~~
	~~[[Category: Transcription factor~~]]

OCA at 23:49, 5 June 2019

2019-06-05T23:49:49Z

← Older revision		Revision as of 23:49, 5 June 2019
Line 1:		Line 1:

	==Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with a tetrazole-containing antagonist==		==Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with a tetrazole-containing antagonist==
	<StructureSection load='4xt2' size='340' side='right' caption='[[4xt2]], [[Resolution\|resolution]] 1.70Å' scene=''>		<StructureSection load='4xt2' size='340' side='right'caption='[[4xt2]], [[Resolution\|resolution]] 1.70Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4xt2]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4XT2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4XT2 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4xt2]] is a 4 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=4XT2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4XT2 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=43L:(5S,7R)-5,7-BIS(3-BROMOPHENYL)-4,5,6,7-TETRAHYDROTETRAZOLO[1,5-A]PYRIMIDINE'>43L</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=43L:(5S,7R)-5,7-BIS(3-BROMOPHENYL)-4,5,6,7-TETRAHYDROTETRAZOLO[1,5-A]PYRIMIDINE'>43L</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3f1p\|3f1p]], [[3f1o\|3f1o]], [[3hw7\|3hw7]], [[3h82\|3h82]], [[4ghi\|4ghi]], [[4gs9\|4gs9]], [[4lpz\|4lpz]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3f1p\|3f1p]], [[3f1o\|3f1o]], [[3hw7\|3hw7]], [[3h82\|3h82]], [[4ghi\|4ghi]], [[4gs9\|4gs9]], [[4lpz\|4lpz]]</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=4xt2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xt2 OCA], [http://pdbe.org/4xt2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4xt2 RCSB], [http://www.ebi.ac.uk/pdbsum/4xt2 PDBsum]</span></td></tr>		<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ARNT, BHLHE2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN]), EPAS1, BHLHE73, HIF2A, MOP2, PASD2 ([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://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4xt2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xt2 OCA], [http://pdbe.org/4xt2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4xt2 RCSB], [http://www.ebi.ac.uk/pdbsum/4xt2 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4xt2 ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
			[[Category: Human]]
			[[Category: Large Structures]]
	[[Category: Gardner, K H]]		[[Category: Gardner, K H]]
	[[Category: Scheuermann, T H]]		[[Category: Scheuermann, T H]]

OCA at 06:19, 23 December 2015

2015-12-23T06:19:22Z

← Older revision		Revision as of 06:19, 23 December 2015
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	==Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with a tetrazole-containing antagonist==		==Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with a tetrazole-containing antagonist==
	<StructureSection load='4xt2' size='340' side='right' caption='[[4xt2]]' scene=''>		<StructureSection load='4xt2' size='340' side='right' caption='[[4xt2]], [[Resolution\|resolution]] 1.70Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4xt2]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4XT2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4XT2 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4xt2]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4XT2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4XT2 FirstGlance]. <br>

OCA at 13:41, 9 December 2015

2015-12-09T13:41:57Z

@@ Line 1: / Line 1: @@
-'''Unreleased structure'''
+==Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with a tetrazole-containing antagonist==
-The entry 4xt2 is ON HOLD  until Paper Publication
+Isoform-Selective and Stereoselective Inhibition of Hypoxia Inducible Factor-2.,Scheuermann TH, Stroud D, Sleet CE, Bayeh L, Shokri C, Wang H, Caldwell CG, Longgood J, MacMillan JB, Bruick RK, Gardner KH, Tambar UK J Med Chem. 2015 Aug 13;58(15):5930-41. doi: 10.1021/acs.jmedchem.5b00529. Epub, 2015 Jul 30. PMID:26226049<ref>PMID:26226049</ref>
-Authors: Scheuermann, T.H., Gardner, K.H.
+From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
+</div>
-Description: Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with a tetrazole-containing antagonist
+<div class="pdbe-citations 4xt2" style="background-color:#fffaf0;"></div>
-[[Category: Unreleased Structures]]
+== References ==
-[[Category: Scheuermann, T.H]]
+<references/>
-[[Category: Gardner, K.H]]
+__TOC__

OCA at 13:04, 27 May 2015

2015-05-27T13:04:21Z

← Older revision		Revision as of 13:04, 27 May 2015
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

	The entry 4xt2 is ON HOLD		The entry 4xt2 is ON HOLD until Paper Publication

	Authors: Scheuermann, T.H., Gardner, K.H.		Authors: Scheuermann, T.H., Gardner, K.H.

OCA at 14:47, 7 February 2015

2015-02-07T14:47:24Z

← Older revision		Revision as of 14:47, 7 February 2015
Line 3:		Line 3:
	The entry 4xt2 is ON HOLD		The entry 4xt2 is ON HOLD

	Authors: Scheuermann, TH, Gardner, KH		Authors: Scheuermann, T.H., Gardner, K.H.

	Description: Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with a tetrazole-containing antagonist		Description: Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with a tetrazole-containing antagonist
	[[Category: Unreleased Structures]]		[[Category: Unreleased Structures]]
	[[Category: Scheuermann, ~~Th,~~ Gardner, Kh]]		[[Category: Scheuermann, T.H]]
			[[Category: Gardner, K.H]]

OCA: Protected "4xt2" [edit=sysop:move=sysop]

2015-01-28T15:49:08Z

Protected "4xt2" [edit=sysop:move=sysop]

← Older revision	Revision as of 15:49, 28 January 2015
(No difference)

OCA: New page: '''Unreleased structure''' The entry 4xt2 is ON HOLD Authors: Scheuermann, TH, Gardner, KH Description: Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-term...

2015-01-28T15:49:07Z

New page: '''Unreleased structure''' The entry 4xt2 is ON HOLD Authors: Scheuermann, TH, Gardner, KH Description: Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-term...

New page

'''Unreleased structure'''

The entry 4xt2 is ON HOLD

Authors: Scheuermann, TH, Gardner, KH

Description: Crystal structure of the high affinity heterodimer of HIF2 alpha and ARNT C-terminal PAS domains in complex with a tetrazole-containing antagonist
[[Category: Unreleased Structures]]
[[Category: Scheuermann, Th, Gardner, Kh]]