Design and Development of novel Heparanase inhibitors able to modulate autophagy

Anno
2020
Proponente Roberta Costi - Professore Associato
Sottosettore ERC del proponente del progetto
LS7_4
Componenti gruppo di ricerca
Componente Categoria
Antonella Capozzi Componenti strutturati del gruppo di ricerca
Flaminia Campo Dottorando/Assegnista/Specializzando componente non strutturato del gruppo di ricerca
Lamberto Tomassini Componenti strutturati del gruppo di ricerca
Abstract

The aim of the project is the development of compounds with selective inhibition against the heparanase enzyme and their evaluation as modulators in autophagy. This group has already identified: i) a class of benzoimidazoles that inhibit heparanase. This is a strong basis for rational drug design of specific Heparanase inhibitors.
Heparanase (Hpse) is the only known mammalian endo-ß-D-glucuronidase capable of cleaving heparan sulphate residues of proteoglycans, an activity highly implicated in a wide variety of biological processes . More recently, the role of Hpse in modulating autophagy in normal and malignant cells has been established thereby conferring growth advantages as well as resistance to chemotherapy.. Autophagy may represent a functional processing event creating a substrate for autoreactivity. It follow that the research in this field may contribute to clarify whether endogenous or pharmacological regulation of autophagy might aid in the development of new treatments for human diseases in which autophagy is not functioning properly.

ERC
LS7_4, PE5_11, PE5_17
Keywords:
CHIMICA FARMACEUTICA, SCOPERTA E DESIGN DI FARMACI, CHIMICA DELLE SOSTANZE NATURALI

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