Urotensin-II receptor peptide agonists

Medicinal Research Reviews
Alfonso CarotenutoPaolo Rovero

Abstract

Urotensin II (U-II) has been known for over 30 years as an important teleost fish hormone, but only recently has it been recognized as the endogenous ligand of a new human G-protein-coupled receptor (GPCR) homologous to the GPR14 orphan receptor from rat. Human U-II was found to be a potent vasoconstrictor, widely distributed in human tissues, possibly contributing to several human cardiovascular diseases. It thus has become a major target of medicinal chemistry research. The common structural feature of U-II peptides from different species is the C-terminal portion, characterized by the disulfide bridged cyclic hexapeptide Cys-Phe-Trp-Lys-Tyr-Cys. The few structure-activity relationship studies reported to date attributed a critical role to this portion, with the Trp-Lys-Tyr motif appearing as the key determinant of U-II bioactivity. Consequently, this shorter cyclic peptide was used as a template for the development of several synthetic analogues, among which a superagonist, termed P5U: H-Asp-cyclo(Pen-Phe-Trp-Lys-Tyr-Cys)-Val-OH. Conformational studies confirmed the important role of hU-II C-terminal cyclic portion, enabling the development of 3D pharmacophore models. These findings should lead to the design of new, potent a...Continue Reading

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Citations

Apr 28, 2010·Naunyn-Schmiedeberg's Archives of Pharmacology·Benjamin D HuntDavid G Lambert
Nov 5, 2016·Journal of Medicinal Chemistry·Sebastian BandholtzCarsten Grötzinger
Nov 6, 2008·Journal of Child Neurology·Ugur BicakCengiz Yakinci
Dec 21, 2013·Archiv der Pharmazie·Diego BrancaccioAlfonso Carotenuto
Mar 26, 2013·Journal of Peptide Science : an Official Publication of the European Peptide Society·Alfonso CarotenutoPaolo Grieco

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