Biochemistry · 2002 · 350 citations · 15 references
Life SciencesMolecular BiologyNeuroscienceMolecular NeurobiologyMolecular NeuroscienceNeurodegenerationAlzheimer DiseaseAmyloid FormationNeurodegenerative DiseasesNeurodegenerative DisordersProteolytic EnzymesProteolytic ProcessingAmyloid Beta PeptidesCleavage Site IdentificationCleavage Site MappingGamma Secretase InhibitionGamma-secretase ProcessingPresenilin MutationsSite-directed CleavageTransmembrane Proteins
Proteolytic processing of the transmembrane domain of the amyloid precursor protein (APP) is a key component of Alzheimer's disease pathogenesis. Using C-terminally tagged APP derivatives, we have identified by amino-terminal sequencing a novel cleavage site of APP, at Leu-49, distal to the gamma-secretase site. This was termed -cleavage. Brefeldin A treatment and pulse-chase experiments indicate that this cleavage occurs late in the secretory pathway. The level of -cleavage is decreased by expression of presenilin-1 mutants known to impair Abeta formation, and it is sensitive to the gamma-secretase inhibitors MDL28170 and L-685,458. Remarkably, it shares similarities with site 3 cleavage of Notch-1: membrane topology, cleavage before a valine, dependence on presenilins, and inhibition profile.
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Purification and cloning of amyloid precursor protein β-secretase from human brain
Sukanto Sinha, John P. Anderson, Robin Barbour et al. · Nature · 1999 · 1.6K citations