Key result
New urantide conformational model defines UTR interactions to guide novel receptor antagonist design.
Why the study?
Urantide is the most potent UT receptor antagonist described to date and may have clinical value in atherosclerosis, but its conformational preferences and interaction with the UTR were not characterized.
Answers are grounded in this paper and cite their sources.
The developed urantide/UTR interaction model provides a structural basis for designing novel UT receptor antagonists with potential applications in atherosclerosis.
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.
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Brancaccio et al. (2013) studied this question. Urantide was evaluated on Conformational preferences and interaction model. A urantide/UTR interaction model was developed based on the conformational preferences of urantide in DPC micelles to aid in the design of novel UTR antagonists.
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