GLYCODRUGS

Glycodrugs: new strategies for controlling the activity of glycosidase enzymes and their application in therapies for lysosomal storage diseases and cancer

 Coordinatore UNIVERSIDAD DE SEVILLA 

 Organization address address: CALLE S. FERNANDO 4
city: SEVILLA
postcode: 41004

contact info
Titolo: Prof.
Nome: Carmen
Cognome: Ortiz-Mellet
Email: send email
Telefono: +34 954 559806
Fax: +34 954 624960

 Nazionalità Coordinatore Spain [ES]
 Totale costo 100˙000 €
 EC contributo 100˙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-2012-CIG
 Funding Scheme MC-CIG
 Anno di inizio 2013
 Periodo (anno-mese-giorno) 2013-07-01   -   2017-06-30

 Partecipanti

# participant  country  role  EC contrib. [€] 
1    UNIVERSIDAD DE SEVILLA

 Organization address address: CALLE S. FERNANDO 4
city: SEVILLA
postcode: 41004

contact info
Titolo: Prof.
Nome: Carmen
Cognome: Ortiz-Mellet
Email: send email
Telefono: +34 954 559806
Fax: +34 954 624960

ES (SEVILLA) coordinator 100˙000.00

Mappa


 Word cloud

Esplora la "nuvola delle parole (Word Cloud) per avere un'idea di massima del progetto.

er    specificity    strategies    enzymes    glycomimetics    cancer    cells    lysosomal    designed    alpha    lsds    enzyme    golgi    chaperones    disease    incorporating    substituents    beta    compounds    glycosidases   

 Obiettivo del progetto (Objective)

'This project aims to new strategies for the preparation of glycomimetics specifically designed to regulate the activity of enzymes involved in pathological processes (glycodrugs). We will focus on the design of glycomimetics to modulate the activity of glycosidases. Particular emphasis will be placed at developing diversity-oriented synthetic strategies to optimize specificity. The target applications are two: elaboration of chemical chaperones for the treatment of lysosomal storage disorders (LSDs; Gaucher disease, Fabry disease and gangliosidosis GM1), and the development of compounds with antiproliferative activity in breast cancer. Compounds able to establish specific interactions with regions of lysosomal glycosidases (beta-glucocerebrosidase and alpha- and beta-galactosidases) surrounding the active site will be designed by incorporating substituents with well-defined orientation. In addition, pH-sensitive elements that will allow an effective bond to the enzyme in the endoplasmic reticulum (ER) will be inserted, forcing the correct folding and providing the traffic to the Golgi apparatus, and at the same time the dissociation of the enzyme:chaperone complex in the lysosome, and thus favouring the rescue of the mutant proteins that cause the disease and the processing of the substrate. Molecular vehicles will also be developed for the directed transport of these chaperones to cells particularly affected in patients with LSDs. For biodistribution studies, labelled derivatives with fluorescent probes will be prepared. The ability to control the specificity of action by incorporating pseudoaglyconic substituents in bicyclic skeletons sp2-iminosugar-type, also allows the design of specific inhibitors for alpha-glucosidases (ER) or for alpha-mannosidases (Golgi). These enzymes are involved in the aberrant glycosylation of N-glycoproteins in tumor cells, so that its control represents a therapeutic strategy against cancer.'

Altri progetti dello stesso programma (FP7-PEOPLE)

DOTOS (2014)

DOT1L in Osteoarthritis

Read More  

IMAGING LYMPHOMA (2010)

New imaging methods for detecting treatment response in lymphoma

Read More  

METAG (2009)

A new 2D-LC approach for quantitative proteomics using MeCAT labeling and multidimensional chromatography coupled to ultra-high-resolution FT-MS-MS and ICP-MS

Read More