Functional selectivity revealed by N-methylation scanning of human urotensin II and related peptides

F Merlino, É Billard, AM Yousif, S Di Maro… - Journal of medicinal …, 2019 - ACS Publications
In accordance with their common but also divergent physiological actions, human urotensin
II (1) and urotensin II-related peptide (2) could stabilize specific urotensin II receptor (UTR) …

New directions for urotensin II receptor ligands

É Billard, M Iddir, H Nassour, L Lee‐Gosselin… - Peptide …, 2019 - Wiley Online Library
The urotensinergic system, formed by a G protein‐coupled receptor (GPCR) termed UT and
two endogenous peptide ligands Urotensin II (UII, H‐Glu‐Thr‐Pro‐Asp‐[Cys‐Phe‐Trp‐Lys …

De Novo Conception of Small Molecule Modulators Based on Endogenous Peptide Ligands: Pyrrolodiazepin-2-one γ-Turn Mimics That Differentially Modulate Urotensin II …

J Dufour-Gallant, D Chatenet… - Journal of Medicinal …, 2015 - ACS Publications
A proof-of-concept library of pyrrolodiazepinone small molecules was designed based on
the Bip-Lys-Tyr motif found in a recently described modulator of the urotensinergic system …

Lead optimization of P5U and urantide: discovery of novel potent ligands at the urotensin-II receptor

A Carotenuto, L Auriemma, F Merlino… - Journal of Medicinal …, 2014 - ACS Publications
We have optimized 1 (P5U) and urantide, two important ligands at the h-UT receptor,
designing several analogues by the exchange of the Tyr9 residue with different unnatural …

An investigation into the origin of the biased agonism associated with the urotensin II receptor activation

D Brancaccio, F Merlino, A Limatola… - Journal of Peptide …, 2015 - Wiley Online Library
The urotensin II receptor (UTR) has long been studied mainly for its involvement in the
cardiovascular homeostasis both in health and disease state. Two endogenous ligands …

[HTML][HTML] Synthesis of constrained analogues of tryptophan

E Rossi, V Pirovano, M Negrato… - Beilstein Journal of …, 2015 - beilstein-journals.org
A Lewis acid-catalysed diastereoselective [4+ 2] cycloaddition of vinylindoles and methyl 2-
acetamidoacrylate, leading to methyl 3-acetamido-1, 2, 3, 4-tetrahydrocarbazole-3 …

Exploration of the urocontrin A scaffold yields new urotensinergic system allosteric modulator and competitive antagonists

E Billard, TE Hébert, D Chatenet - Biochemical Pharmacology, 2023 - Elsevier
The urotensinergic system, involved in the development and/or progression of numerous
pathological conditions, is composed of one G protein-coupled receptor (UT) and two …

Urantide Conformation and Interaction with the Urotensin‐II Receptor

D Brancaccio, A Limatola, P Campiglia… - Archiv der …, 2014 - Wiley Online Library
Urotensin II (U‐II) is a disulfide bridged peptide hormone identified as the ligand of a G
protein‐coupled receptor. Human U‐II (H‐Glu‐Thr‐Pro‐Asp‐c [Cys‐Phe‐Trp‐Lys‐Tyr‐Cys] …

Development and pharmacological characterization of conformationally constrained urotensin II-related peptide agonists

D Chatenet, B Folch, D Feytens… - Journal of Medicinal …, 2013 - ACS Publications
Urotensin II (UII) and its paralog peptide, urotensin II-related peptide (URP), exert not only
common but also divergent actions through the activation of UT, a specific membrane-bound …

Insight into the role of urotensin II-related peptide tyrosine residue in UT activation

E Billard, M Létourneau, TE Hébert… - Biochemical Pharmacology, 2017 - Elsevier
While sharing common biological activity, the two endogenous ligands of the G protein-
coupled receptor UT, eg urotensin II (UII) and urotensin II-related peptide (URP), also exhibit …