Functional selectivity revealed by N-methylation scanning of human urotensin II and related peptides
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) …
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 …
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 …
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 …
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
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 …
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 …
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 …
pathological conditions, is composed of one G protein-coupled receptor (UT) and two …
Urantide Conformation and Interaction with the Urotensin‐II Receptor
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] …
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 …
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 …
coupled receptor UT, eg urotensin II (UII) and urotensin II-related peptide (URP), also exhibit …