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J Med Chem. 2002 Sep 26;45(20):4391-4.

A new, potent urotensin II receptor peptide agonist containing a Pen residue at the disulfide bridge.

Author information

1
Department of Pharmaceutical and Toxicological Chemistry, University of Naples Federico II, I-80131 Naples, Italy.

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.

PMID:
12238917
DOI:
10.1021/jm025549i
[Indexed for MEDLINE]

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