BiCAPPA is the first bivalent antiprion ligand. BiCAPPA can decrease infectious conformational form of prion protein (PrPSc) from scrapie-infected cells, with an EC50 of 0.32 μM.
BiCAPPA (10 nM-2 μM; 5 d) decreases proteinase K-resistant PrPSc from scrapie-infected mouse hypothalamus cells, with an EC50 of 0.32 μM[2].
References:
[1]. Uliassi E, et, al. 10-Medicinal Chemistry of Hybrids for Neurodegenerative Diseases. Design of Hybrid Molecules for Drug Development. 2017, Pages 259-277.
[2]. Bongarzone S, et, al. Parallel synthesis, evaluation, and preliminary structure-activity relationship of 2,5-diamino-1,4-benzoquinones as a novel class of bivalent anti-prion compound. J Med Chem. 2010 Nov 25;53(22):8197-201.
















