New insight into the binding mode of peptides at urotensin-II receptor by Trp-constrained analogues of P5U and urantide(605 views) 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
Paper type: Journal Article, Research Support, Non-U. S. Gov'T,
Impact factor: 1.862, 5-year impact factor: 1.715
Url: Not available.
Keywords: 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: *** IBB - CNR ***
Department of Pharmacy, University of Naples Federico II, I-80131 Naples, Italy.,
References: Not available.
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
Antonini A, Vitale C, Barone P, Cilia R, Righini A, Bonuccelli U, Abbruzzese G, Ramat S, Petrone A, Quatrale R, Marconi R, Ceravolo R, Stefani A, Lopiano L, Zappia M, Capus L, Morgante L, Tamma F, Tinazzi M, Colosimo C, Guerra UP, Valzania F, Fagioli G, Distefano A, Bagnato A, Feggi L, Anna S, Maria Teresa Rosaria De Cr, Nobili F, Mazzuca N, Baldari S, Eleopra R, Bestetti A, Benti R, Varrone A, Volterrani D, Massa R, Stocchi F, Schillaci O, Dore F, Zibetti M, Castellano G, Battista SG, Giorgetti G * The relationship between cerebral vascular disease and parkinsonism: The VADO study(601 views) Parkinsonism Relat D (ISSN: 1353-8020, 1873-5126, 1873-5126electronic), 2012; 18(6): 775-780. Impact Factor:3.274 ViewExport to BibTeXExport to EndNote
Hesse B, Tagil K, Cuocolo A, Anagnostopoulos C, Bardies M, Bax J, Bengel F, Busemann Sokole E, Davies G, Dondi M, Edenbrandt L, Franken P, Kjaer A, Knuuti J, Lassmann M, Ljungberg M, Marcassa C, Marie PY, Mckiddie F, O'connor M, Prvuolovich E, Underwood R * 3. 0 T perfusion MR imaging(879 views) Rivista Di Neuroradiologia (ISSN: 1120-9976), 2004; 17(6): 807-812. Impact Factor:0.023 ViewExport to BibTeXExport to EndNote