5x93 - Revision history

OCA at 10:16, 15 November 2017

OCA — Wed, 15 Nov 2017 10:16:57 GMT

←Older revision		Revision as of 10:16, 15 November 2017
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-	==~~Crystal Structure of a Receptor_2~~==	+	==Human endothelin receptor type-B in complex with antagonist K-8794==
	<StructureSection load='5x93' size='340' side='right' caption='[[5x93]], [[Resolution\|resolution]] 2.20Å' scene=''>		<StructureSection load='5x93' size='340' side='right' caption='[[5x93]], [[Resolution\|resolution]] 2.20Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5x93]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5X93 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5X93 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5x93]] is a 1 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=5X93 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5X93 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=K87:3-[6-[(4-tert-butylphenyl)sulfonylamino]-5-(2-methoxyphenoxy)-2-pyrimidin-2-yl-pyrimidin-4-yl]oxy-N-(2,6-dimethylphenyl)propanamide'>K87</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=K87:3-[6-[(4-tert-butylphenyl)sulfonylamino]-5-(2-methoxyphenoxy)-2-pyrimidin-2-yl-pyrimidin-4-yl]oxy-N-(2,6-dimethylphenyl)propanamide'>K87</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">EDNRB, ETRB ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Lysozyme Lysozyme], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.17 3.2.1.17] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Lysozyme Lysozyme], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.17 3.2.1.17] </span></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=5x93 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5x93 OCA], [http://pdbe.org/5x93 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5x93 RCSB], [http://www.ebi.ac.uk/pdbsum/5x93 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5x93 ProSAT]</span></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=5x93 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5x93 OCA], [http://pdbe.org/5x93 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5x93 RCSB], [http://www.ebi.ac.uk/pdbsum/5x93 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5x93 ProSAT]</span></td></tr>
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Lysozyme]]		[[Category: Lysozyme]]
	[[Category: Doi, T]]		[[Category: Doi, T]]

OCA at 04:24, 21 September 2017

OCA — Thu, 21 Sep 2017 04:24:43 GMT

←Older revision		Revision as of 04:24, 21 September 2017
Line 1:		Line 1:
-	'''Unreleased structure'''

-	The entry ~~5x93~~ is ~~ON HOLD~~	+	==Crystal Structure of a Receptor_2==
		+	<StructureSection load='5x93' size='340' side='right' caption='[[5x93]], [[Resolution\|resolution]] 2.20Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5x93]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5X93 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5X93 FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=K87:3-[6-[(4-tert-butylphenyl)sulfonylamino]-5-(2-methoxyphenoxy)-2-pyrimidin-2-yl-pyrimidin-4-yl]oxy-N-(2,6-dimethylphenyl)propanamide'>K87</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr>
		+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Lysozyme Lysozyme], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.2.1.17 3.2.1.17] </span></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=5x93 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5x93 OCA], [http://pdbe.org/5x93 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5x93 RCSB], [http://www.ebi.ac.uk/pdbsum/5x93 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5x93 ProSAT]</span></td></tr>
		+	</table>
		+	== Disease ==
		+	[[http://www.uniprot.org/uniprot/EDNRB_HUMAN EDNRB_HUMAN]] Hirschsprung disease;Waardenburg-Shah syndrome. The disease is caused by mutations affecting the gene represented in this entry. The disease is caused by mutations affecting the gene represented in this entry. The disease is caused by mutations affecting the gene represented in this entry. Defects in EDNRB are associated with Waardenburg syndrome 2, with ocular albinism, autosomal recessive: A disorder characterized by the association of features typical of Waardenburg syndrome type 2 with ocular albinism. Patients manifest reduced visual acuity, albinotic fundus, deafness, hypomelanosis.<ref>PMID:28236341</ref>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/EDNRB_HUMAN EDNRB_HUMAN]] Non-specific receptor for endothelin 1, 2, and 3. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.<ref>PMID:7536888</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Endothelin receptors (ETRs) have crucial roles in vascular control and are targets for drugs designed to treat circulatory-system diseases and cancer progression. The nonpeptide dual-ETR antagonist bosentan is the first oral drug approved to treat pulmonary arterial hypertension. Here we report crystal structures of human endothelin ETB receptor bound to bosentan and to the ETB-selective analog K-8794, at 3.6-A and 2.2-A resolution, respectively. The K-8794-bound structure reveals the detailed water-mediated hydrogen-bonding network at the transmembrane core, which could account for the weak negative allosteric modulation of ETB by Na+ ions. The bosentan-bound structure reveals detailed interactions with ETB, which are probably conserved in the ETA receptor. A comparison of the two structures shows unexpected similarity between antagonist and agonist binding. Despite this similarity, bosentan sterically prevents the inward movement of transmembrane helix 6 (TM6), and thus exerts its antagonistic activity. These structural insights will facilitate the rational design of new ETR-targeting drugs.

-	~~Authors:~~ Shihoya, W., Nishizawa, T., Yamashita, K., ~~Hirata~~, K., Okuta, A., Tani, K., Fujiyoshi, Y., Doi, T., Nureki, O.	+	X-ray structures of endothelin ETB receptor bound to clinical antagonist bosentan and its analog.,Shihoya W, Nishizawa T, Yamashita K, Inoue A, Hirata K, Kadji FMN, Okuta A, Tani K, Aoki J, Fujiyoshi Y, Doi T, Nureki O Nat Struct Mol Biol. 2017 Sep;24(9):758-764. doi: 10.1038/nsmb.3450. Epub 2017, Aug 14. PMID:28805809<ref>PMID:28805809</ref>

-	~~Description: Crystal Structure of~~ a ~~Receptor_2~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	~~[[Category~~: ~~Unreleased Structures]]~~	+	</div>
-	[[Category: ~~Nureki, O~~]]	+	<div class="pdbe-citations 5x93" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Lysozyme]]
	[[Category: Doi, T]]		[[Category: Doi, T]]
	[[Category: Fujiyoshi, Y]]		[[Category: Fujiyoshi, Y]]
		+	[[Category: Hirata, K]]
		+	[[Category: Nishizawa, T]]
		+	[[Category: Nureki, O]]
	[[Category: Okuta, A]]		[[Category: Okuta, A]]
		+	[[Category: Shihoya, W]]
	[[Category: Tani, K]]		[[Category: Tani, K]]
	[[Category: Yamashita, K]]		[[Category: Yamashita, K]]
-	[[Category: ~~Nishizawa, T~~]]	+	[[Category: Alpha helical]]
-	[[Category: ~~Hirata, K]]~~	+	[[Category: Signaling protein]]
-	~~[[Category: Shihoya, W~~]]	+

OCA: Protected "5x93" [edit=sysop:move=sysop]

OCA — Wed, 15 Mar 2017 20:19:35 GMT

Protected "5x93" [edit=sysop:move=sysop]

←Older revision

Revision as of 20:19, 15 March 2017

OCA: New page: '''Unreleased structure''' The entry 5x93 is ON HOLD Authors: Shihoya, W., Nishizawa, T., Yamashita, K., Hirata, K., Okuta, A., Tani, K., Fujiyoshi, Y., Doi, T., Nureki, O. Description...

OCA — Wed, 15 Mar 2017 20:19:33 GMT

New page: '''Unreleased structure''' The entry 5x93 is ON HOLD Authors: Shihoya, W., Nishizawa, T., Yamashita, K., Hirata, K., Okuta, A., Tani, K., Fujiyoshi, Y., Doi, T., Nureki, O. Description...

New page

'''Unreleased structure'''

The entry 5x93 is ON HOLD

Authors: Shihoya, W., Nishizawa, T., Yamashita, K., Hirata, K., Okuta, A., Tani, K., Fujiyoshi, Y., Doi, T., Nureki, O.

Description: Crystal Structure of a Receptor_2
[[Category: Unreleased Structures]]
[[Category: Nureki, O]]
[[Category: Doi, T]]
[[Category: Fujiyoshi, Y]]
[[Category: Okuta, A]]
[[Category: Tani, K]]
[[Category: Yamashita, K]]
[[Category: Nishizawa, T]]
[[Category: Hirata, K]]
[[Category: Shihoya, W]]