International union of basic and clinical pharmacology. XCII. Urotensin II, urotensin II–related peptide, and their receptor: From structure to function

H Vaudry, J Leprince, D Chatenet, A Fournier… - Pharmacological …, 2015 - Elsevier
Urotensin II (UII) is a cyclic neuropeptide that was first isolated from the urophysis of teleost
fish on the basis of its ability to contract the hindgut. Subsequently, UII was characterized in …

Unnatural amino acids: strategies, designs, and applications in medicinal chemistry and drug discovery

KK Sharma, K Sharma, K Rao, A Sharma… - Journal of Medicinal …, 2024 - ACS Publications
Peptides can operate as therapeutic agents that sit within a privileged space between small
molecules and larger biologics. Despite examples of their potential to regulate receptors and …

Allosteric modulator leads hiding in plain site: Developing peptide and peptidomimetics as GPCR allosteric modulators

KM Olson, JR Traynor, A Alt - Frontiers in Chemistry, 2021 - frontiersin.org
Allosteric modulators (AMs) of G-protein coupled receptors (GPCRs) are desirable drug
targets because they can produce fewer on-target side effects, improved selectivity, and …

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 …

Identification of a sacral, visceral sensory transcriptome in embryonic and adult mice

CJA Smith-Anttila, EA Mason, CA Wells, BJ Aronow… - Eneuro, 2020 - eneuro.org
Visceral sensory neurons encode distinct sensations from healthy organs and initiate pain
states that are resistant to common analgesics. Transcriptome analysis is transforming our …

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 …

Update on the urotensinergic system: new trends in receptor localization, activation, and drug design

D Chatenet, TTM Nguyen, M Létourneau… - Frontiers in …, 2013 - frontiersin.org
The urotensinergic system plays central roles in the physiological regulation of major
mammalian organ systems, including the cardiovascular system. As a matter of fact, this …

Design, synthesis, and biological assessment of biased allosteric modulation of the urotensin II receptor using achiral 1, 3, 4-Benzotriazepin-2-one turn mimics

A Douchez, E Billard, TE Hebert… - Journal of Medicinal …, 2017 - ACS Publications
Benzotriazepin-2-ones were designed to mimic the suggested bioactive γ-turn conformation
of the Bip-Lys-Tyr tripeptide in Urocontrin ([Bip4] URP), which modulates the urotensin II …