Key result
Azasulfuryl-UII(4-11) derivatives 7-9 exhibited weak affinity for the UT receptor but reduced up to 50% of the effects of UII and URP without affecting their potency.
Novel azasulfuryl-UII(4-11) derivatives demonstrate partial antagonistic properties against urotensin II and urotensin II-related peptide in rat aortic rings.
Cyclic azasulfuryl (As) peptide analogs of the urotensin II (UII, 1, H-Glu-Thr-Pro-Asp-c[Cys-Phe-Trp-Lys-Tyr-Cys]-Val-OH) fragment 4-11 were synthesized to explore the influences of backbone structure on biological activity. N-Aminosulfamides were inserted as surrogates of the Trp(7) and Lys(8) residues in the biologically relevant Trp-Lys-Tyr triad. A combination of solution- and solid-phase methods were used to prepare novel UII((4-11)) analogs 6-11 by routes featuring alkylation of azasulfuryl-glycine tripeptide precursors to install various side chains. The pharmacological profiles of derivatives 6-11 were tested in vitro using a competitive binding assay and ex vivo using a rat aortic ring bioassay. Although the analogs exhibited weak affinity for the urotensin II receptor (UT) without agonistic activity, azasulfuryl-UII((4-11)) derivatives 7-9 reduced up to 50% of the effects of UII and urotensin II-related peptide (URP) without affecting their potency.
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Merlino et al. (2016) studied this question. Urotensin II(4-11) Azasulfuryl Peptides vs. Urotensin II and urotensin II-related peptide was evaluated on Affinity for the urotensin II receptor (UT) and agonistic/antagonistic activity. Azasulfuryl-UII(4-11) derivatives 7-9 exhibited weak affinity for the UT receptor but reduced up to 50% of the effects of UII and URP without affecting their potency.
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