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Figure 3 | Molecular Medicine

Figure 3

From: Selective Antihypertensive Dihydropyridines Lower Aβ Accumulation by Targeting both the Production and the Clearance of Aβ across the Blood-Brain Barrier

Figure 3

Effect of antihypertensive calcium channel blockers on human BACE-1 activity using cell free assays. (A) BACE-1 mediated proteolytic process of a FRET peptide substrate containing the Swedish peptide sequence (EVNLDAEFK) as a function of time. The inhibitor BACE-IV was used as a reference inhibitor for BACE-1. (B) Quantification of BACE-1 activity using the chemoluminescent HitHunter assay. Data show that calcium channel blockers do not inhibit BACE-1 activity directly and, in particular nilvadipine and amlodipine (no statistically significant main effect of nilvadipine and amlodipine doses was observed by ANOVA (P > 0.05)) do not have any impact on BACE-1 activity for the dose range tested.

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Molecular Medicine

ISSN: 1528-3658