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.

A New, Potent Urotensin II Receptor Peptide Agonist Containing a Pen Residue at the Disulfide Bridge / Grieco, Paolo; Carotenuto, Alfonso; Campiglia, P.; Zampelli, E.; Patacchini, R.; Maggi, C.; Novellino, E.; Rovero, P.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 45:20(2002), pp. 4391-4394. [10.1021/jm025549i]

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

GRIECO, PAOLO;CAROTENUTO, ALFONSO;NOVELLINO E.;
2002

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.
2002
A New, Potent Urotensin II Receptor Peptide Agonist Containing a Pen Residue at the Disulfide Bridge / Grieco, Paolo; Carotenuto, Alfonso; Campiglia, P.; Zampelli, E.; Patacchini, R.; Maggi, C.; Novellino, E.; Rovero, P.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 45:20(2002), pp. 4391-4394. [10.1021/jm025549i]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/136661
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