New insight into the binding mode of peptides at urotensin-II receptor by Trp-constrained analogues of P5U and urantide(459 views visite) Carotenuto A, Auriemma L, Merlino F, Limatola A, Campiglia P, Gomez-monterrey I, Di Villa Bianca R, Brancaccio D, Santicioli P, Meini S, Maggi CA, Novellino E, Grieco P
Keywords Parole chiave: Humans, Nuclear Magnetic Resonance, Biomolecular, Peptide Fragments, Chemical Synthesis, Chemistry, Peptide Hormones, Agonists, Cyclic, Protein Conformation, Structure-Activity Relationship, Tryptophan, Analogs, Derivatives, Urotensins, Vasoconstrictor Agents,
Affiliations Affiliazioni: *** IBB - CNR ***
Department of Pharmacy, University of Naples Federico II, I-80131 Naples, Italy.,
References Riferimenti: Not available. Non disponibili.
New insight into the binding mode of peptides at urotensin-II receptor by Trp-constrained analogues of P5U and urantide
Urotensin II (U-II) is a disulfide bridged peptide hormone identified as the ligand of a G-protein-coupled receptor. Human U-II (H-Glu-Thr-Pro-Asp-c[Cys-Phe-Trp-Lys-Tyr-Cys]-Val-OH) has been described as the most potent vasoconstrictor compound identified to date. We have recently identified both a superagonist of human U-II termed P5U (H-Asp-c[Pen-Phe-Trp-Lys-Tyr-Cys]-Val-OH) and the compound termed urantide (H-Asp-c[Pen-Phe-D-Trp-Orn-Tyr-Cys]-Val-OH), which is the most potent UT receptor peptide antagonist described to date. In the present study, we have synthesized four analogues of P5U and urantide in which the Trp(7) residue was replaced by the highly constrained L-Tpi and D-Tpi residues. The replacement of the Trp(7) by Tpi led to active analogues. Solution NMR analysis allowed improving the knowledge on conformation-activity relationships previously reported on UT receptor ligands.
New insight into the binding mode of peptides at urotensin-II receptor by Trp-constrained analogues of P5U and urantide
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