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8 results on '"Santicioli P"'

2. NMR structure of Urotensin Peptide Asp-c[Cys-Phe-(N-Me)Trp-Lys-Tyr-Cys]-Val in SDS solution

Author

Brancaccio, D., primary, Carotenuto, A., additional, Merlino, F., additional, Billard, E., additional, Yousif, A.M., additional, Di Maro, S., additional, Abate, L., additional, Bellavita, R., additional, D'Emmanuele di Villa Bianca, R., additional, Santicioli, P., additional, Marinelli, L., additional, Novellino, E., additional, Hebert, T.E., additional, Lubell, W.D., additional, Chatenet, D., additional, and Grieco, P., additional

Published
2019
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3. NMR structure of Urotensin Peptide Asp-c[Cys-Phe-Trp-(N-Me)Lys-Tyr-Cys]-Val in SDS solution

Author

Brancaccio, D., primary, Carotenuto, A., additional, Merlino, F., additional, Billard, E., additional, Yousif, A.M., additional, Di Maro, S., additional, Abate, L., additional, Bellavita, R., additional, D'Emmanuele di Villa Bianca, R., additional, Santicioli, P., additional, Marinelli, L., additional, Novellino, E., additional, Hebert, T.E., additional, Lubell, W.D., additional, Chatenet, D., additional, and Grieco, P., additional

Published
2019
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4. Gender-related differential effect of tachykinin NK2 receptor-mediated visceral hyperalgesia in guinea pig colon

Author

Bellucci, F., Bueno, Lionel, Bugianesi, R., Crea, A., D'Aranno, V., Meini, Stephania, Santicioli, P., Tramontana, M., Maggi, C. A., Pharmacology Department, University, ToxAlim (ToxAlim), Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Institut National Polytechnique (Toulouse) (Toulouse INP), Université Fédérale Toulouse Midi-Pyrénées-Ecole Nationale Vétérinaire de Toulouse (ENVT), Institut National Polytechnique (Toulouse) (Toulouse INP), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Ecole d'Ingénieurs de Purpan (INPT - EI Purpan), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-Institut National de la Recherche Agronomique (INRA), Menarini Ricerche S.p.A, Partenaires INRAE, and Menarini Richerche S.p.A

Subjects
Male, Colon, brain, [SDV]Life Sciences [q-bio], Guinea Pigs, Thiophenes, localization, substance-p, sex, Animals, Sex Characteristics, binding-sites, Dipeptides, Receptors, Neurokinin-2, Visceral Pain, Colitis, Research Papers, irritable-bowel-syndrome, Disease Models, Animal, publication, Trinitrobenzenesulfonic Acid, Hyperalgesia, 5-ht3 antagonist, Female, neurokinin, pharmacology
Abstract

International audience; Background and PurposeThe tachykinin NK2 receptor antagonist ibodutant is under Phase III clinical investigation to treat female patients with irritable bowel syndrome. The aim of this study was to investigate the NK2 receptor-related gender specificity in a model of colitis. Experimental ApproachColitis was induced by rectal instillation of 2,4,6-trinitrobenzenesulfonic acid (TNBS, 0.5mL, 30mgmL(-1) in 30% ethanol) in female and male guinea pigs. Electromyographic recording of the responses to colorectal distension (CRD) was made 3days later. Ibodutant (0.33 , 0.65, 1.9 and 6.5mgkg(-1)) was given s.c., 30min before CRD. Release of neurokinin A and substance P from isolated mucosal and smooth muscle tissues following treatment with KCl (80mM) or capsaicin (10M) was measured by EIA. Plasma pharmacokinetics of ibodutant following a single s.c. administration (0.73 or 2.1mgkg(-1)) were measured over 24h. Key ResultsIbodutant did not affect abdominal contractions in control animals. After TNBS-induced colitis, ibodutant prevented the increased visceral hypersensitivity to CRD in females, at lower doses than in males. Ibodutant pharmacokinetics did not differ between females and males. Tachykinins release was greater in smooth muscle than in mucosal samples. Capsaicin-stimulated release of tachykinins from inflamed mucosal samples from females was significantly lower than in males. Conclusions and ImplicationsIbodutant prevented abdominal nociception in a model of visceral hypersensitivity in guinea pigs with a greater efficacy in females than in males. Our results highlight a gender-related difference in colonic visceral hypersensitivity and mucosal nerve activation.

Published
2015
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7. Functional Selectivity Revealed by N-Methylation Scanning of Human Urotensin II and Related Peptides

Author

Alfonso Carotenuto, Paolo Grieco, William D. Lubell, Rosa Bellavita, Ettore Novellino, Etienne Billard, Diego Brancaccio, Paola Santicioli, Ali Munaim Yousif, David Chatenet, Salvatore Di Maro, Terence E. Hébert, Roberta d'Emmanuele di Villa Bianca, Francesco Merlino, Luigi Abate, Luciana Marinelli, Merlino, F., Billard, E., Yousif, A. M., Di Maro, S., Brancaccio, D., Abate, L., Carotenuto, A., Bellavita, R., D'Emmanuele Di Villa Bianca, R., Santicioli, P., Marinelli, L., Novellino, E., Hebert, T. E., Lubell, W. D., Chatenet, D., Grieco, P., Merlino, Francesco, Billard, Etienne, Yousif, Ali Munaim, Di Maro, Salvatore, Brancaccio, Diego, Abate, Luigi, Carotenuto, Alfonso, Bellavita, Rosa, d'Emmanuele di Villa Bianca, Roberta, Santicioli, Paolo, Marinelli, Luciana, Novellino, Ettore, Hébert, Terence, Lubell, William D, Chatenet, David, Grieco, Paolo, University of Naples Federico II, Institut Armand Frappier (INRS-IAF), Institut National de la Recherche Scientifique [Québec] (INRS)-Réseau International des Instituts Pasteur (RIIP), Menarini Ricerche [Florence], McGill University = Université McGill [Montréal, Canada], Université de Montréal (UdeM), and The study was supported by Canadian Institutes of Health Research (CIHR) (MOP-142184) and the Natural Sciences and Engineering Research Council of Canada (NSERC) (RGPIN-2015-04848) to D.C. We thank the Canadian Institutes of Health Research (CIHR) and the Natural Sciences and Engineering Research Council of Canada (NSERC) for funding

Subjects
Untranslated region, Male, Protein Conformation, [SDV]Life Sciences [q-bio], Peptide Hormones, Urotensins, Peptide, CHO Cells, Urotensin-II receptor, Ligands, 01 natural sciences, Methylation, Receptors, G-Protein-Coupled, Rats, Sprague-Dawley, 03 medical and health sciences, chemistry.chemical_compound, Protein structure, Cricetulus, Drug Discovery, Urotensin-II, peptide synthesis, NMR spectroscopy, N-methylation, Functional selectivity, Animals, Humans, Nuclear Magnetic Resonance, Biomolecular, 030304 developmental biology, chemistry.chemical_classification, 0303 health sciences, Intracellular Signaling Peptides and Proteins, Biological activity, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, HEK293 Cells, chemistry, Biochemistry, Molecular Medicine, Urotensin-II
Abstract

International audience; In accordance with their common but also divergent physiological actions, human urotensin II (1) and urotensin II-related peptide (2) could stabilize specific urotensin II receptor (UTR) conformations, thereby activating different signaling pathways, a feature referred to as biased agonism or functional selectivity. Sequential N-methylation of the amides in the conserved core sequence of 1, 2, and fragment U-II4-11 (3) shed light on structural requirements involved in their functional selectivity. Thus, 18 N-methylated UTR ligands were synthesized and their biological profiles evaluated using in vitro competition binding assays, ex vivo rat aortic ring bioassays and BRET-based biosensor experiments. Biological activity diverged from that of the parent structures contingent on the location of amide methylation, indicating relevant hydrogen-bond interactions for the function of the endogenous peptides. Conformational analysis of selected N-methyl analogs indicated the importance of specific amide residues of 2 for the distinct pharmacology relative to 1 and 3.

Published
2019
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8. Structure-Activity Study of the Peptides P5U and Urantide by the Development of Analogues Containing Uncoded Amino Acids at Position 9.

Author

Merlino F, Brancaccio D, Yousif AM, Piras L, Campiglia P, Gomez-Monterrey I, Santicioli P, Meini S, Maggi CA, Novellino E, Carotenuto A, and Grieco P

Subjects
Amino Acids chemistry, Animals, Dose-Response Relationship, Drug, Humans, Male, Molecular Structure, Peptides chemistry, Rats, Rats, Wistar, Structure-Activity Relationship, Amino Acids pharmacology, Peptide Fragments chemistry, Peptide Fragments pharmacology, Peptides pharmacology, Receptors, G-Protein-Coupled agonists, Receptors, G-Protein-Coupled antagonists & inhibitors, Urotensins chemistry, Urotensins pharmacology
Abstract

Previous modifications of the peptide sequence of human urotensin-II (U-II) led to the identification of two well-known ligands: P5U and urantide. These derivatives are considered to be the most representative agonist and antagonist, respectively, at the human urotensin receptor (UT). Optimization of P5U and urantide was carried out to stabilize specific conformations that may suggest new elements for discriminating agonist versus antagonist activity. We studied novel derivatives containing uncoded amino acids. In particular, the Tyr(9) residue of both P5U and urantide was replaced with nonaromatic hydrophobic bulky residues, as well as conformationally constrained aromatic moieties to generate eight novel derivatives. These analogues further contributed to determining the influence of such residues on binding affinity for and biological activity at UT. One of these eight peptides was also investigated by NMR spectroscopy and docking studies owing to its peculiar conformational properties and mode of interaction with UT. This structure-activity study is aimed at a more thorough examination of the role of tyrosine in modulating the agonism/antagonism of human U-II., (© 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Published
2016
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