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Start Over Author "Yousif Ali" Journal journal of medicinal chemistry
8 results on '"Yousif Ali"'

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

Author

Merlino, Francesco, primary, Billard, Étienne, additional, Yousif, Ali M., additional, Di Maro, Salvatore, additional, Brancaccio, Diego, additional, Abate, Luigi, additional, Carotenuto, Alfonso, additional, Bellavita, Rosa, additional, d’Emmanuele di Villa Bianca, Roberta, additional, Santicioli, Paolo, additional, Marinelli, Luciana, additional, Novellino, Ettore, additional, Hébert, Terence E., additional, Lubell, William D., additional, Chatenet, David, additional, and Grieco, Paolo, additional

Published
2019
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2. Development of Macrocyclic Peptidomimetics Containing Constrained α,α-Dialkylated Amino Acids with Potent and Selective Activity at Human Melanocortin Receptors

Author

Merlino, Francesco, primary, Zhou, Yang, additional, Cai, Minying, additional, Carotenuto, Alfonso, additional, Yousif, Ali M., additional, Brancaccio, Diego, additional, Di Maro, Salvatore, additional, Zappavigna, Silvia, additional, Limatola, Antonio, additional, Novellino, Ettore, additional, Grieco, Paolo, additional, and Hruby, Victor J., additional

Published
2018
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5. Lead Optimization of P5U and Urantide: Discovery of Novel Potent Ligands at the Urotensin-II Receptor

Author

Carotenuto, Alfonso, primary, Auriemma, Luigia, additional, Merlino, Francesco, additional, Yousif, Ali Munaim, additional, Marasco, Daniela, additional, Limatola, Antonio, additional, Campiglia, Pietro, additional, Gomez-Monterrey, Isabel, additional, Santicioli, Paolo, additional, Meini, Stefania, additional, Maggi, Carlo A., additional, Novellino, Ettore, additional, and Grieco, Paolo, additional

Published
2014
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6. Urotensin II(4-11) Azasulfuryl Peptides: Synthesis and Biological Activity.

Author

Merlino, Francesco, Yousif, Ali M., Billard, Étienne, Dufour-Gallant, Julien, Turcotte, Stéphane, Grieco, Paolo, Chatenet, David, and Lubell, William D.

Subjects
*PEPTIDE derivatives, *UROTENSINS, *ALKYLATION, *BINDING site assay, *LABORATORY rats
Abstract

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 Trp7 and Lys8 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. [ABSTRACT FROM AUTHOR]

Published
2016
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8. Lead optimization of P5U and urantide: discovery of novel potent ligands at the urotensin-II receptor

Author

Ali Munaim Yousif, Luigia Auriemma, Paolo Grieco, Paolo Santicioli, Daniela Marasco, Carlo Alberto Maggi, Stefania Meini, Isabel Gomez-Monterrey, Alfonso Carotenuto, Pietro Campiglia, Francesco Merlino, Antonio Limatola, Ettore Novellino, Carotenuto, Alfonso, Auriemma, Luigia, Merlino, Francesco, Yousif, ALI MUNAIM, Marasco, Daniela, Limatola, Antonio, Pietro, Campiglia, GOMEZ MONTERREY, ISABEL MARIA, Paolo, Santicioli, Stefania, Meini, Carlo A., Maggi, Novellino, Ettore, and Grieco, Paolo

Subjects
Models, Molecular, Stereochemistry, Urotensins, Molecular Conformation, Urotensin-II receptor, ligand, Ligands, Peptides, Cyclic, Peptide Synthesi, Receptors, G-Protein-Coupled, chemistry.chemical_compound, Residue (chemistry), Structure-Activity Relationship, Drug Discovery, Aromatic amino acids, Bioassay, Structure–activity relationship, Humans, Receptor, Dose-Response Relationship, Drug, Drug discovery, Chemistry, Antagonist, urotensin II, Peptide Fragments, Biochemistry, Molecular Medicine
Abstract

We have optimized 1 (P5U) and urantide, two important ligands at the h-UT receptor, designing several analogues by the exchange of the Tyr9 residue with different unnatural aromatic amino acids. This study allowed us to discover novel ligands with improved activity. In particular, the replacement of the Tyr9 residue by (pCN)Phe or (pNO2)Phe within the urantide sequence led to compounds 13 (UPG-83) and 15 (UPG-95), respectively, which showed pure antagonist activity toward UT receptor in a rat aorta bioassay. More interestingly, the replacement of the Tyr9 in 1 sequence with the Btz or the (3,4-Cl)Phe residues led to superagonists 6 (UPG-100) and 10 (UPG-92) with pEC50 values at least 1.4 log higher than that of 1, being the most potent UT agonists discovered to date. Compounds 10 and 13 showed also a good stability in a serum proteolytic assay. These ligands represent new useful tools to further characterize the urotensinergic system in human physiopathology.

Published
2014

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