6hvc: Difference between revisions

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-'''Unreleased structure'''
-The entry 6hvc is ON HOLD
+==NMR structure of Urotensin Peptide Asp-c[Cys-Phe-Trp-(N-Me)Lys-Tyr-Cys]-Val in SDS solution==
+<StructureSection load='6hvc' size='340' side='right' caption='[[6hvc]], [[NMR_Ensembles_of_Models | 10 NMR models]]' scene=''>
+== Structural highlights ==
+<table><tr><td colspan='2'>[[6hvc]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6HVC OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6HVC FirstGlance]. <br>
+</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=NMK:'>NMK</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=6hvc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6hvc OCA], [http://pdbe.org/6hvc PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6hvc RCSB], [http://www.ebi.ac.uk/pdbsum/6hvc PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6hvc ProSAT]</span></td></tr>
+</table>
+== Function ==
+[[http://www.uniprot.org/uniprot/UTS2_HUMAN UTS2_HUMAN]] Highly potent vasoconstrictor.
+<div style="background-color:#fffaf0;">
+== Publication Abstract from PubMed ==
+In accordance with their common but also divergent physiological actions, human urotensin II ( hU-II, 1) and urotensin II-related peptide (URP, 2) could stabilize specific urotensin II receptor (UTR) conformations, thereby activating different signalling pathways, a feature referred to as biased agonism or functional selectivity. Sequential N-methylation of the amides in the conserved core sequence of 1, 2 and fragment U-II4-11 (3) shed light on structural requirements involved in their functional selectivity. Thus, eighteen N-methylated UTR ligands were synthesized and their biological profiles evaluated using both in vitro competition binding assays, ex vivo rat aortic ring bioassays and BRET-based biosensor experiments. Biological activity diverged from that of the parent structures contingent on the location of amide methylation indicating relevant hydrogen-bond interactions for function of the endogenous peptides. Conformational analysis of selected N-methyl analogs indicated the importance of specific amide residues of 2 for the distinct pharmacology relative to 1 and 3.
-Authors: Brancaccio, D., Carotenuto, A., Merlino, F., Billard, E., Yousif, A.M., Di Maro, S., Abate, L., Bellavita, R., D'Emmanuele di Villa Bianca, R., Santicioli, P., Marinelli, L., Novellino, E., Hebert, T.E., Lubell, W.D., Chatenet, D., Grieco, P.
+Functional Selectivity Revealed by N-Methylation Scanning of Human Urotensin II and Related Peptides.,Merlino F, Billard E, Yousif AM, Di Maro S, Brancaccio D, Abate L, Carotenuto A, Bellavita R, d'Emmanuele di Villa Bianca R, Santicioli P, Marinelli L, Novellino E, Hebert T, Lubell WD, Chatenet D, Grieco P J Med Chem. 2019 Jan 7. doi: 10.1021/acs.jmedchem.8b01601. PMID:30615452<ref>PMID:30615452</ref>
-Description: NMR structure of Urotensin Peptide Asp-c[Cys-Phe-Trp-(N-Me)Lys-Tyr-Cys]-Val in SDS solution
+From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
-[[Category: Unreleased Structures]]
+</div>
-[[Category: Santicioli, P]]
+<div class="pdbe-citations 6hvc" style="background-color:#fffaf0;"></div>
-[[Category: Carotenuto, A]]
+== References ==
-[[Category: Hebert, T.E]]
+<references/>
+__TOC__
+</StructureSection>
 [[Category: Abate, L]]
+[[Category: Bellavita, R]]
+[[Category: Bianca, R D.Emmanuele di Villa]]
 [[Category: Billard, E]]
+[[Category: Brancaccio, D]]
+[[Category: Carotenuto, A]]
+[[Category: Chatenet, D]]
+[[Category: Grieco, P]]
+[[Category: Hebert, T E]]
+[[Category: Lubell, W D]]
+[[Category: Marinelli, L]]
+[[Category: Maro, S Di]]
 [[Category: Merlino, F]]
-[[Category: Lubell, W.D]]
 [[Category: Novellino, E]]
-[[Category: Grieco, P]]
+[[Category: Santicioli, P]]
-[[Category: D'Emmanuele Di Villa Bianca, R]]
+[[Category: Yousif, A M]]
-[[Category: Bellavita, R]]
+[[Category: G protein-coupled receptor]]
-[[Category: Yousif, A.M]]
+[[Category: N-methylation]]
-[[Category: Brancaccio, D]]
+[[Category: Nmr solution]]
-[[Category: Marinelli, L]]
+[[Category: Peptide binding protein]]
-[[Category: Di Maro, S]]
+[[Category: Sd]]
-[[Category: Chatenet, D]]
+[[Category: Urotensin ii receptor]]