Discovery of a Class of Diketopiperazines as Antiprion Compounds (pages 1324–1334)
Maria Laura Bolognesi, Hoang Ngoc Ai Tran, Matteo Staderini, Alessandra Monaco, Alberto López-Cobeñas, Salvatore Bongarzone, Xevi Biarnés, Pilar López-Alvarado, Nieves Cabezas, Maria Caramelli, Paolo Carloni, J. Carlos Menéndez and Giuseppe Legname
Version of Record online: 10 JUN 2010 | DOI: 10.1002/cmdc.201000133
Planarity is key: Thanks to a planar conformation, DKP analogues perturb PrP amyloid fibril formation in vitro. Moreover, one compound inhibits prion replication in the low micromolar range in scrapie-infected GT1 cells. Lead compounds for the further development of therapeutic agents against prion diseases, or useful chemical probes, were identified.