Novel insights into the role of urotensin II in cardiovascular disease

J Pereira-Castro, C Brás-Silva, AP Fontes-Sousa - Drug discovery today, 2019 - Elsevier
Highlights•Urotensin II is a cyclic undecapeptide involved in cardiovascular
regulation.•Pseudo-irreversible binding to UT receptor could explain urotensin II low …

Towards targeting the urotensinergic system: overview and challenges

H Nassour, M Iddir, D Chatenet - Trends in Pharmacological Sciences, 2019 - cell.com
The urotensinergic system, comprised of a G protein-coupled receptor (UT) and two
endogenous ligands named urotensin II (UII) and urotensin II-related peptide (URP), has …

Expanding Structure–Activity Relationships of Human Urotensin II Peptide Analogues: A Proposed Key Role of the N-Terminal Region for Novel Urotensin II Receptor …

F Merlino, A Secondo, E Mitidieri… - Journal of Medicinal …, 2024 - ACS Publications
While the urotensinergic system plays a role in influencing various pathologies, its potential
remains untapped because of the absence of therapeutically effective urotensin II receptor …

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) …

Urotensin II(4–11) Azasulfuryl Peptides: Synthesis and Biological Activity

F Merlino, AM Yousif, É Billard… - Journal of Medicinal …, 2016 - ACS Publications
Cyclic azasulfuryl (As) peptide analogs of the urotensin II (UII, 1, H-Glu-Thr-Pro-Asp-c [Cys-
Phe-Trp-Lys-Tyr-Cys]-Val-OH) fragment 4–11 were synthesized to explore the influences of …

Urotensin‐II‐Targeted Liposomes as a New Drug Delivery System towards Prostate and Colon Cancer Cells

S Zappavigna, M Abate, AM Cossu, S Lusa… - Journal of …, 2019 - Wiley Online Library
Urotensin‐II (UT‐II) and its receptor (UTR) are involved in the occurrence of different
epithelial cancers. In particular, UTR was found overexpressed on colon, bladder, and …

Urotensin II receptor deficiency ameliorates ligation-induced carotid intimal hyperplasia partially through the RhoA-YAP1 pathway

P Wei, K Tian, H Liu, K Li, N Alam, D Cheng… - … et Biophysica Acta (BBA …, 2024 - Elsevier
Intimal hyperplasia (IH) is a common pathological feature of vascular proliferative diseases,
such as atherosclerosis and restenosis after angioplasty. Urotensin II (UII) and its receptor …

Urokinase receptor derived peptides as potent inhibitors of the formyl peptide receptor type 1-triggered cell migration

AM Yousif, V Ingangi, F Merlino, D Brancaccio… - European Journal of …, 2018 - Elsevier
The receptor for the urokinase-type plasminogen activator (uPAR) is a widely recognized
master regulator of cell migration. We and others have previously documented that the …

Urotensin-II peptidomimetic incorporating a non-reducible 1, 5-triazole disulfide bond reveals a pseudo-irreversible covalent binding mechanism to the urotensin G …

S Pacifico, A Kerckhoffs, AJ Fallow… - Organic & …, 2017 - pubs.rsc.org
The urotensin-II receptor (UTR) is a class A GPCR that predominantly binds to the
pleiotropic cyclic peptide urotensin-II (U-II). U-II is constrained by a disulfide bridge that …

Discovery of new allosteric modulators of the urotensinergic system through substitution of the urotensin II-related peptide (URP) phenylalanine residue

E Billard, TE Hébert, D Chatenet - Journal of Medicinal Chemistry, 2018 - ACS Publications
Urotensin II (UII) and urotensin II-related peptide (URP) are functionally selective,
suggesting that these two hormones might play distinct physiological role through different …