antiprion

TCS PrP Inhibitor 13 (5-(4-Nitrophenyl)-2-Phenyl-4H-Pyrazol-3-One) is an antiprion agent inhibiting protease-resistant prion protein (PrP-res) accumulation.

Chloroguanabenz is an antiprion agent and a derivative of the α2-adrenergic receptor agonist guanabenz . It inhibits prion formation in yeast and mammalian cell-based assays. Chloroguanabenz reduces the levels of both soluble and aggregated forms of the truncated Huntingtin derivative Htt48 in an HEK293T cellular model of Huntington's disease.

6-Amino-8-trifluoromethylphenanthridine (6A-8tFP) is an antiprion agent and a derivative of 6-aminophenanthridine . It inhibits protein folding activity of the ribosome (PFAR) when used at a concentration of 150 μM. 6A-8tFP directly competes with protein substrates for the ribosomal active site.

IND45193, an antiprion agent, acts by reducing PrP(Sc) levels in dividing and stationary-phase cells.

BiCAPPA, a pioneering bivalent antiprion ligand, effectively reduces the infectious conformational form of prion protein (PrP Sc) in scrapie-infected cells, achieving this at a concentration (EC 50) of 0.32 μM.

l-Atabrine dihydrochloride displays antiprion activity. l-Atabrine dihydrochloride is a less active enantiomer of quinacrine.

IND81 is an antiprion agent that works by extending the lives of prion-infected animals.

Quinoprazine, a powerful inhibitor of Vaccinia virus DNA synthesis (IC50 = 10 μM), exhibits notable antimalarial activity against Plasmodium berghei. Additionally, it demonstrates significant antiprion potency, effectively reducing levels of PrPSc [1]-[5].

6-Aminophenanthridine is an antiprion agent. It inhibits prion formation in yeast- and mammalian-based screening assays when used alone and, to a greater extent, when used in combination with the α2-adrenergic receptor agonist guanabenz . 6-Aminophenanthridine (300 μM) inhibits protein folding activity of the ribosome (PFAR) by directly competing with protein substrates for the active site and decreases the yield of refolded protein without affecting the refolding rate. It prevents progressive wing position defects in a Drosophila model of oculopharyngeal muscular dystrophy (OPMD) when larvae are raised on medium containing doses ranging from 300 to 400 μM and in adults following dietary administration of 1-3 mM doses. 6-Aminophenanthridine also reduces muscle degeneration and decreases the number of nuclear inclusions in thoracic muscle in a Drosophila model of OPMD.