Modulation of prion by small molecules: from monovalent to bivalent and multivalent ligands.
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.
Departamento de Química Orgánica y Farmacéutica, Universidad Complutense, 28040 Madrid, Spain. josecm@farm.ucm.es.
Matteo
M
Staderini
Giuseppe
G
Legname
Maria Laura
ML
Bolognesi
J Carlos
JC
Menéndez
D000818:Animals; D015195:Drug Design; D006801:Humans; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D017096:Prion Diseases / Q000188:drug therapy*; D011328:Prions / Q000037:antagonists & inhibitors*; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use
D008024:Ligands; D011328:Prions; D054852:Small Molecule Libraries