Modulation of Prion by Small Molecules: From Monovalent to Bivalent and Multivalent Ligands

Author(s): Matteo Staderini, Giuseppe Legname, Maria Laura Bolognesi, J. Carlos Menéndez

Journal Name: Current Topics in Medicinal Chemistry

Volume 13 , Issue 19 , 2013

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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.

Keywords: Prion protein, protein misfolding diseases, neurodegenerative diseases, protein-protein interaction, bifunctional ligands, molecular tweezers, palindromic compounds.

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Article Details

Year: 2013
Page: [2491 - 2503]
Pages: 13
DOI: 10.2174/15680266113136660176
Price: $65

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PDF: 13