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Journal of Amino Acids
Volume 2013 (2013), Article ID 979016, 15 pages
Review Article

Urotensin-II Ligands: An Overview from Peptide to Nonpeptide Structures

1Department of Pharmacy, University of Naples Federico II, 80131 Naples, Italy
2Department of Biochemistry, Biophysics and General Pathology, Second University of Naples, 80138 Naples, Italy

Received 2 December 2012; Accepted 14 January 2013

Academic Editor: Giuseppe De Rosa

Copyright © 2013 Francesco Merlino et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


Urotensin-II was originally isolated from the goby urophysis in the 1960s as a vasoactive peptide with a prominent role in cardiovascular homeostasis. The identification of human isoform of urotensin-II and its specific UT receptor by Ames et al. in 1999 led to investigating the putative role of the interaction U-II/UT receptor in multiple pathophysiological effects in humans. Since urotensin-II is widely expressed in several peripheral tissues including cardiovascular system, the design and development of novel urotensin-II analogues can improve knowledge about structure-activity relationships (SAR). In particular, since the modulation of the U-II system offers a great potential for therapeutic strategies related to the treatment of several diseases, like cardiovascular diseases, the research of selective and potent ligands at UT receptor is more fascinating. In this paper, we review the developments of peptide and nonpeptide U-II structures so far developed in order to contribute also to a more rational and detectable design and synthesis of new molecules with high affinity at the UT receptor.