[HTML][HTML] Presenilin-1 and-2 are molecular targets for γ-secretase inhibitors

D Seiffert, JD Bradley, CM Rominger… - Journal of Biological …, 2000 - ASBMB
Presenilins are integral membrane protein involved in the production of amyloid β-protein.
Mutations of the presenilin-1 and-2 gene are associated with familial Alzheimer's disease
and are thought to alter γ-secretase cleavage of the β-amyloid precursor protein, leading to
increased production of longer and more amyloidogenic forms of Aβ, the 4-kDa β-peptide.
Here, we show that radiolabeled γ-secretase inhibitors bind to mammalian cell membranes,
and a benzophenone analog specifically photocross-links three major membrane …