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6k1q

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'''Unreleased structure'''
 
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The entry 6k1q is ON HOLD until Paper Publication
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==Human endothelin receptor type-B in complex with inverse agonist IRL2500==
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<StructureSection load='6k1q' size='340' side='right'caption='[[6k1q]], [[Resolution|resolution]] 2.70&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[6k1q]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6K1Q OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6K1Q FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=D2U:(2~{S})-2-[[(2~{R})-2-[(3,5-dimethylphenyl)carbonyl-methyl-amino]-3-(4-phenylphenyl)propanoyl]amino]-3-(1~{H}-indol-3-yl)propanoic+acid'>D2U</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene></td></tr>
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<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>
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<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=6k1q FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6k1q OCA], [http://pdbe.org/6k1q PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6k1q RCSB], [http://www.ebi.ac.uk/pdbsum/6k1q PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6k1q ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[[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>
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== Function ==
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[[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>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Endothelin receptors (ETA and ETB) are G-protein-coupled receptors activated by endothelin-1 and are involved in blood pressure regulation. IRL2500 is a peptide-mimetic of the C-terminal tripeptide of endothelin-1, and has been characterized as a potent ETB-selective antagonist, which has preventive effects against brain edema. Here, we report the crystal structure of the human ETB receptor in complex with IRL2500 at 2.7 A-resolution. The structure revealed the different binding modes between IRL2500 and endothelin-1, and provides structural insights into its ETB-selectivity. Notably, the biphenyl group of IRL2500 penetrates into the transmembrane core proximal to D(2.50), thus stabilizing the inactive conformation. Using the newly-established constitutively active mutant, we clearly demonstrate that IRL2500 functions as an inverse agonist for the ETB receptor. The current findings will expand the chemical space of ETR antagonists and facilitate the design of inverse agonists for other class A GPCRs.
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Authors: Nagiri, C., Shihoya, W., Nureki, O.
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Crystal structure of human endothelin ETB receptor in complex with peptide inverse agonist IRL2500.,Nagiri C, Shihoya W, Inoue A, Kadji FMN, Aoki J, Nureki O Commun Biol. 2019 Jun 21;2:236. doi: 10.1038/s42003-019-0482-7. eCollection 2019. PMID:31263780<ref>PMID:31263780</ref>
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Description: Human endothelin receptor type-B in complex with inverse agonist IRL2500
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[Category: Unreleased Structures]]
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</div>
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[[Category: Nureki, O]]
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<div class="pdbe-citations 6k1q" style="background-color:#fffaf0;"></div>
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Large Structures]]
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[[Category: Lysozyme]]
[[Category: Nagiri, C]]
[[Category: Nagiri, C]]
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[[Category: Nureki, O]]
[[Category: Shihoya, W]]
[[Category: Shihoya, W]]
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[[Category: Alpha helical]]
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[[Category: Signaling protein]]

Revision as of 10:43, 17 July 2019

Human endothelin receptor type-B in complex with inverse agonist IRL2500

PDB ID 6k1q

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