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Arch Pharm (Weinheim). 2014 Mar;347(3):185-92. doi: 10.1002/ardp.201300269. Epub 2013 Dec 4.

Urantide conformation and interaction with the urotensin-II receptor.

Author information

1
Department of Pharmacy, University of Naples "Federico II", Naples, Italy.

Abstract

Urotensin II (U-II) is a disulfide bridged peptide hormone identified as the ligand of a G protein-coupled receptor. Human U-II (H-Glu-Thr-Pro-Asp-c[Cys-Phe-Trp-Lys-Tyr-Cys]-Val-OH) has been described as the most potent vasoconstrictor compound identified to date. We have previously identified the compound termed urantide (H-Asp-c[Pen-Phe-DTrp-Orn-Tyr-Cys]-Val-OH), which is the most potent UT receptor (UTR) antagonist described to date. Urantide may have potential clinical value in the treatment of atherosclerosis. In the present study, we studied the conformational preferences of urantide in DPC micelles and developed a urantide/UTR interaction model. This model can help the design of novel peptides and small molecules as UTR antagonists.

KEYWORDS:

Atherosclerosis; Conformation by NMR; Docking studies; Therapeutic peptide; Urotensin-II

PMID:
24357333
DOI:
10.1002/ardp.201300269
[Indexed for MEDLINE]

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