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Development and pharmacological characterization of "caged" urotensin II analogs.

Abstract : Urotensin-II (U-II) is a cyclic 11-amino acid peptide known as a potent mammalian vasoconstrictor. To study some purported intracellular actions of U-II, masked analogs of this peptide, becoming biologically active only upon UV exposure, were developed. Those analogs described as "caged" were derivatized with a photolabile 4,5-dimethoxynitrobenzyl group on the side chain of Lys-8 or Tyr-9. Both caged analogs of U-II showed a major decrease in their affinity towards the UT receptor. Nevertheless, upon UV irradiation, the native and biologically active U-II peptide was recovered. Thus, this work describes the development of new "caged" U-II derivatives and demonstrates that vasoactivity of U-II can be controlled by masking and unmasking two key residues.
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Contributor : Charles M. Dozois Connect in order to contact the contributor
Submitted on : Friday, May 3, 2013 - 1:17:38 AM
Last modification on : Friday, March 27, 2020 - 3:18:03 PM

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Steve Bourgault, Myriam Létourneau, Alain Fournier. Development and pharmacological characterization of "caged" urotensin II analogs.. Peptides, Elsevier, 2005, 26 (8), pp.1475-80. ⟨10.1016/j.peptides.2005.03.019⟩. ⟨pasteur-00820036⟩



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