Yousif, Ali Munaim (2015) Synthesis of New Ligands of Urokinase Receptor and New Urotensin-II Derivatives. [Tesi di dottorato]
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| Item Type: | Tesi di dottorato |
|---|---|
| Resource language: | English |
| Title: | Synthesis of New Ligands of Urokinase Receptor and New Urotensin-II Derivatives |
| Creators: | Creators Email Yousif, Ali Munaim alimunaim.yousif@unina.it |
| Date: | 31 March 2015 |
| Institution: | Università degli Studi di Napoli Federico II |
| Department: | Farmacia |
| Scuola di dottorato: | Scienze farmaceutiche |
| Dottorato: | Scienza del farmaco |
| Ciclo di dottorato: | 27 |
| Coordinatore del Corso di dottorato: | nome email D'Auria, Maria Valeria madauria@unina.it |
| Tutor: | nome email Grieco, Paolo UNSPECIFIED Lubell, William D. UNSPECIFIED |
| Date: | 31 March 2015 |
| Keywords: | UII upar peptide chemistry |
| Settori scientifico-disciplinari del MIUR: | Area 03 - Scienze chimiche > CHIM/09 - Farmaceutico tecnologico applicativo |
| Date Deposited: | 10 Apr 2015 11:56 |
| Last Modified: | 28 Apr 2016 01:00 |
| URI: | http://www.fedoa.unina.it/id/eprint/10547 |
| DOI: | 10.6092/UNINA/FEDOA/10547 |
Collection description
Unit 1: The urokinase-type plasminogen activator receptor (uPAR) is involved in the regulation of cell migration. The uPAR is formed by three domains connected by short linker region. The Ser88-Arg-Ser- Arg-Tyr92 is the minimum chemotactic sequence of uPAR required to induce the same intracellular signaling as result of its binding with formyl peptide receptor (FPRs). With aim to perform a SAR study on this sequence we have synthesized a large peptide library using phosphorylated amino acids, non-coded amino acids, D-amino acid scan and cyclic analogues. A new two potent inhibitors of cell migration, uPAR2 and uPAR18, have been identified represented, respectivetly, by the analogue with phosphorylated Ser90 and the analogue with cyclic conformation. Unit 2: Urotensin II (U-II), is a cyclic peptid has been described as the most potent vasoconstrictor documented. The vasocontriction effect of U-II is a result of the binding with its receptor UT receptor. The cyclic region of U-II, c[Cys-Phe-Trp-Lys-Tyr-Cys], plays an essential role in terms of affinity for UT receptor. We developed new two different libraries of U-II analogues carried structure modification on the peptide bond to explore new SARs on the cyclic region of U-II. Peptoids analogues represent the first library whose the side chain are appended to N-atom rather than the α- Carbon. The second library represented by N-aminosulfamide analogues (azasulfurylpeptides), a class of peptidomimetics, in which the CαH and the carbonyl are respectively replaced by a nitrogen atom and a sulfonyl group.
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