Title:Modulation of Prion by Small Molecules: From Monovalent to Bivalent and Multivalent Ligands
VOLUME: 13 ISSUE: 19
Author(s):Matteo Staderini, Giuseppe Legname, Maria Laura Bolognesi and J. Carlos Menéndez
Affiliation:Departamento de Química Orgánica y Farmacéutica, Universidad Complutense, 28040 Madrid, Spain.
Keywords:Prion protein, protein misfolding diseases, neurodegenerative diseases, protein-protein interaction, bifunctional
ligands, molecular tweezers, palindromic compounds.
Abstract:Prion diseases are fatal neurodegenerative disorders that affect humans and animals and for which no pharmacological
treatment is available. Compounds consisting of two identical moieties joined via an appropriate spacer (i.e. bivalent
compounds) have turned out to be effective tools to prevent prion fibril formation and exhibit an improved biological
profile with regard to the corresponding monovalent derivatives. In this review we discuss the importance of the bivalent
strategy as a viable approach to design new chemical entities to combat prion diseases.
