Replacing Cys5 by Pen (penicillamine, b,b-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 disulfide bridge / P. GRIECO; A. CAROTENUTO;P. CAMPIGLIA; E. ZAMPELLI; R. PATACCHINI; C. MAGGI; E. NOVELLINO; P. ROVERO. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 45:(2002), pp. 4391-4394. [10.1021/jm025549i]
A new potent urotensin II receptor peptide agonist containing a Pen residue at disulfide bridge.
ROVERO, PAOLO
2002
Abstract
Replacing Cys5 by Pen (penicillamine, b,b-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.
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