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Literature summary for 3.4.23.46 extracted from

  • Georgievska, B.; Gustavsson, S.; Lundkvist, J.; Neelissen, J.; Eketjaell, S.; Ramberg, V.; Bueters, T.; Agerman, K.; Jureus, A.; Svensson, S.; Berg, S.; Faelting, J.; Lendahl, U.
    Revisiting the peripheral sink hypothesis: inhibiting BACE1 activity in the periphery does not alter beta-amyloid levels in the CNS (2015), J. Neurochem., 132, 477-486.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4-fluoro-1-(pyridin-4-yl)-1-[3-(pyrimidin-5-yl)phenyl]-1H-isoindol-3-amine i.e. AZ2000. Inhibitor with improved brain disposition, reduces amyloid beta levels in both brain and periphery already after acute dosing. Mice heterozygous for BACE1, display a 62% reduction in plasma amyloid beta40 levels, whereas brain amyloid beta40 is only lowered by 11% Mus musculus

Organism

Organism UniProt Comment Textmining
Mus musculus P56818
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General Information

General Information Comment Organism
physiological function selective inhibition of peripheral BACE1 activity in wild-type mice or mice over-expressing amyloid precursor protein reduces amyloid beta levels in the periphery but not in the brain, not even after chronic treatment over several months. BACE1 inhibitor 4-fluoro-1-(pyridin-4-yl)-1-[3-(pyrimidin-5-yl)phenyl]-1H-isoindol-3-amine with improved brain disposition reduces amyloid beta levels in both brain and periphery already after acute dosing. Mice heterozygous for BACE1, display a 62% reduction in plasma amyloid beta40 levels, whereas brain amyloid beta40 is only lowered by 11% Mus musculus