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American Chemical Society, Journal of Medicinal Chemistry, 20(45), p. 4391-4394, 2002

DOI: 10.1021/jm025549i

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A New, Potent Urotensin II Receptor Peptide Agonist Containing a Pen Residue at the Disulfide Bridge

Journal article published in 2002 by Paolo Grieco, Alfonso Carotenuto, Pietro Campiglia, Enrico Zampelli, Riccardo Patacchini, Carlo A. Maggi, Ettore Novellino, Paolo Rovero ORCID
This paper is available in a repository.
This paper is available in a repository.

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Abstract

Replacing Cys(5) by Pen (penicillamine, beta,beta-dimethylcysteine) in the cyclic C-terminal U-II octapeptide, U-II(4-11), we have obtained a potent urotensin II (U-II) receptor agonist. Conformational analysis of solution NMR data indicated that the putative biologically active conformation of U-II is stabilized by introduction of a Pen residue. To the best of our knowledge, this is the most potent U-II receptor agonist reported to date.