Yousif, Ali Munaim
(2015)
Synthesis of New Ligands of Urokinase
Receptor and New Urotensin-II
Derivatives.
[Tesi di dottorato]
| Tipologia del documento: |
Tesi di dottorato
|
| Lingua: |
English |
| Titolo: |
Synthesis of New Ligands of Urokinase
Receptor and New Urotensin-II
Derivatives |
| Autori: |
| Autore | Email |
|---|
| Yousif, Ali Munaim | alimunaim.yousif@unina.it |
|
| Data: |
31 Marzo 2015 |
| Istituzione: |
Università degli Studi di Napoli Federico II |
| Dipartimento: |
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 | [non definito] | | Lubell, William D. | [non definito] |
|
| Data: |
31 Marzo 2015 |
| Parole chiave: |
UII upar peptide chemistry |
| Settori scientifico-disciplinari del MIUR: |
Area 03 - Scienze chimiche > CHIM/09 - Farmaceutico tecnologico applicativo |
[error in script]
[error in script]
| Depositato il: |
10 Apr 2015 11:56 |
| Ultima modifica: |
28 Apr 2016 01:00 |
| URI: |
http://www.fedoa.unina.it/id/eprint/10547 |
| DOI: |
10.6092/UNINA/FEDOA/10547 |
Abstract
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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