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Updated: Jan 19, 2026
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Towards Targeting the Urotensinergic System: Overview and Challenges
Hassan Nassour1, Mustapha Iddir1, David Chatenet1
1Institut National de la Recherche Scientifique, Institut Armand-Frappier, Groupe de Recherche en Ingénierie des Peptides et en Pharmacothérapie (GRIPP), Université du Québec, Ville de Laval, QC, Canada.
Trends in Pharmacological Sciences
|September 11, 2019
Summary
The urotensinergic system, involving urotensin II (UII) and its receptor (UT), shows promise for treating diseases. However, UT antagonists failed in human trials, requiring new therapeutic strategies.
Area of Science:
- Pharmacology
- Cardiovascular Research
- Oncology
Background:
- The urotensinergic system, comprising the G protein-coupled receptor (UT) and its ligands urotensin II (UII) and urotensin II-related peptide (URP), is implicated in various diseases.
- Preclinical studies in animal models suggest UT antagonists are potential therapeutics for atherosclerosis, pulmonary arterial hypertension, heart failure, and cancer.
Purpose of the Study:
- To explore hypotheses explaining the limited efficacy of UT antagonists in human clinical trials.
- To identify potential reasons for the failure of UT antagonists in vivo despite promising preclinical data.
Main Methods:
- Review and analysis of existing literature on the urotensinergic system.
- Discussion of potential biological and pharmacological factors contributing to the in vivo failure of UT antagonists.
Main Results:
- Clinical investigations of UT antagonist candidates demonstrated limited efficacy in humans.
- The urotensinergic system remains a therapeutic target that has yet to be effectively exploited.
Conclusions:
- The failure of UT antagonists in vivo necessitates a deeper understanding of the urotensinergic system's complexity in humans.
- Further research is required to overcome the challenges in therapeutically targeting the urotensinergic system for disease treatment.
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