SUZUKI PEPTIDES

"Peptide ligands with restricted mobility through a Suzuki reaction: design, synthesis and evaluation"

Coordinatore	FUNDACIO INSTITUT DE RECERCA BIOMEDICA (IRB BARCELONA)    more  Organization address address: CARRER BALDIRI REIXAC 10-12 PARC SCIENTIFIC DE BARCELONA city: BARCELONA postcode: 8028 contact info Titolo: Ms. Nome: Stel.La Cognome: Serra Email: send email Telefono: -591 Fax: +34 93 403 71 14
Nazionalità Coordinatore	Spain [ES]
Totale costo	45˙000 €
EC contributo	45˙000 €
Programma	FP7-PEOPLE Specific programme "People" implementing the Seventh Framework Programme of the European Community for research, technological development and demonstration activities (2007 to 2013)
Code Call	FP7-PEOPLE-2009-RG
Funding Scheme	MC-ERG
Anno di inizio	2009
Periodo (anno-mese-giorno)	2009-10-01   -   2012-09-30

 Partecipanti

#	participant	country	role	EC contrib. [€]
1	FUNDACIO INSTITUT DE RECERCA BIOMEDICA (IRB BARCELONA)  Organization address address: CARRER BALDIRI REIXAC 10-12 PARC SCIENTIFIC DE BARCELONA city: BARCELONA postcode: 8028 contact info Titolo: Ms. Nome: Stel.La Cognome: Serra Email: send email Telefono: -591 Fax: +34 93 403 71 14	ES (BARCELONA)	coordinator	45˙000.00

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 Obiettivo del progetto (Objective)

'The aim of this research proposal is the application of the Suzuki-Miyaura reaction to the synthesis of peptidic libraries with restricted mobility. Specifically, we envision the synthesis of a family of cyclic peptides that will contain a biaryl bond, to further restrain their conformation. This biaryl bond will be obtained through a Suzuki-Miyaura set of reactions between two aromatic amino acid derivatives in the sequence. Initially, the reaction conditions will be optimized on simple models: the order in which the bicyclic peptides should be assembled, solid vs. solution-phase, Suzuki-Miyaura reaction conditions…Once the synthesis has been optimized, several peptide libraries will be prepared, progressively increasing the synthetic challenge and including D- and non-proteinogenic amino acids. The ultimate goal of the project is to obtain new series of peptides which will act as ligands of certain protein surfaces (POP, DPP-IV and VEGF), for which they will have been designed. The sequences to be synthesized will be first decided on rational design basis assisted through evolutionary algorithms and, later, based on the results obtained for the interaction with the therapeutic target. Special attention will be placed on the conformational study of such constrained molecules. The interaction of the new peptides with the proteins surfaces, as well as their ADME properties will be evaluated through different methods.'