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Towards Targeting the Urotensinergic System: Overview and Challenges

Nassour, Hassan, Iddir, Mustapha et Chatenet, d (2019). Towards Targeting the Urotensinergic System: Overview and Challenges Trends in Pharmacological Sciences , vol. 40 , nº 10. p. 725-734. DOI: 10.1016/j.tips.2019.08.005.

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Résumé

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 garnered significant attention due to its involvement in the initiation and/or the evolution of various diseases. Accordingly, multiple studies using animal models have demonstrated that UT antagonists may have utility as potential therapeutic agents for treating atherosclerosis, pulmonary arterial hypertension, heart failure, and cancer. Unfortunately, clinical investigations of UT antagonist candidates showed limited efficacy in humans. This system, which has yet to be effectively targeted, therefore remains to be therapeutically exploited. Here, we discuss various hypotheses that could explain the in vivo failure of UT antagonists.

Type de document: Article
Mots-clés libres: bias agonism; functional selectivity; interspecies variability; probe-dependent action; urotensin II; urotensin II-related peptide
Centre: Centre INRS-Institut Armand Frappier
Date de dépôt: 22 juill. 2021 21:52
Dernière modification: 22 juill. 2021 21:52
URI: https://espace.inrs.ca/id/eprint/11647

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