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Structure-activity relationship study of position 4 in the urotensin-II receptor ligand U-II(4-11)

Erika Marzola, Valeria Camarda, Madura Batuwangala, David G Lambert, Girolamo Calo', Remo Guerrini, Claudio Trapella, Domenico Regoli, Roberto Tomatis, Severo Salvadori
Peptides 2008, 29 (5): 674-9
17822806
In the present study we describe the synthesis and biological evaluation of 24 analogues of the urotensin II (U-II) fragment U-II(4-11) substituted in position 4 with coded and non-coded aromatic amino acids. All of the new analogues behaved as full U-II receptor (UT) agonists. Our results indicated that aromaticity is well tolerated, size, length and chirality of the side chain are not important, while substituents with a nitrogen atom are preferred. Thus acylation of U-II(5-11) with small groups bearing nitrogen atoms could be instrumental in future studies for the identification of novel potent UT receptor ligands.

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