View source for 6hvb


==NMR structure of Urotensin Peptide Asp-c[Cys-Phe-(N-Me)Trp-Lys-Tyr-Cys]-Val in SDS solution==
<StructureSection load='6hvb' size='340' side='right'caption='[[6hvb]]' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[6hvb]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6HVB OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6HVB FirstGlance]. <br>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR, 10 models</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=E9M:(2S)-3-(1H-indol-3-yl)-2-(methylamino)propanoic+acid'>E9M</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=6hvb FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6hvb OCA], [https://pdbe.org/6hvb PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6hvb RCSB], [https://www.ebi.ac.uk/pdbsum/6hvb PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6hvb ProSAT]</span></td></tr>
</table>
== Function ==
[https://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.

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>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 6hvb" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Abate L]]
[[Category: Bellavita R]]
[[Category: Billard E]]
[[Category: Brancaccio D]]
[[Category: Carotenuto A]]
[[Category: Chatenet D]]
[[Category: D'Emmanuele di Villa Bianca R]]
[[Category: Di Maro S]]
[[Category: Grieco P]]
[[Category: Hebert TE]]
[[Category: Lubell WD]]
[[Category: Marinelli L]]
[[Category: Merlino F]]
[[Category: Novellino E]]
[[Category: Santicioli P]]
[[Category: Yousif AM]]