Urotensin II (UT II) is an important factor of cellular homeostasis. This regulatory peptide is
involved in the pathophysiology of many disorders. For example, it plays an important role in the pathogenesis
of acute and chronic diseases, stressful and adaptive reactions of the body, in the development of
cardiovascular pathologies, metabolic syndrome, inflammation, liver cirrhosis, renal failure, diabetic
nephropathy, reproductive dysfunction, progression of psychosomatic, psychoendocrinal and psychiatric
disorders. In this concern, the involvement of UT II in the pathophysiology of many processes determines
the perspectives for the development of blockers of urotensin receptors for the treatment of the
aforementioned diseases. It is important that even today this kind of perspective is feasible due to the
synthesis of a series of GPR14 blockers. The objective of this review is to discuss current molecular
mechanisms of biological activity, regulatory functions of UT II, its role in the pathogenesis of different
nosologies, as well as analysis of the possible routes of exposure to GPR14 as potential therapeutic targets.
Keywords: Urotensin II, regulatory peptides, molecular targets of Urotensin II in cardiovascular, nervous, hormonal systems,
stress, kidney, sexual function, cancer, G-protein-coupled receptors; drug design.
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