Structure-based design of potent and selective cell-permeable inhibitors of human β-secretase (BACE-1)
SJ Stachel, CA Coburn, TG Steele… - Journal of medicinal …, 2004 - ACS Publications
SJ Stachel, CA Coburn, TG Steele, KG Jones, EF Loutzenhiser, AR Gregro, HA Rajapakse…
Journal of medicinal chemistry, 2004•ACS PublicationsWe describe the development of cell-permeable β-secretase inhibitors that demonstratively
inhibit the production of the secreted amino terminal fragment of an artificial amyloid
precursor protein in cell culture. In addition to potent inhibition in a cell-based assay (IC50<
100 nM), these inhibitors display impressive selectivity against other biologically relevant
aspartyl proteases.
inhibit the production of the secreted amino terminal fragment of an artificial amyloid
precursor protein in cell culture. In addition to potent inhibition in a cell-based assay (IC50<
100 nM), these inhibitors display impressive selectivity against other biologically relevant
aspartyl proteases.
We describe the development of cell-permeable β-secretase inhibitors that demonstratively inhibit the production of the secreted amino terminal fragment of an artificial amyloid precursor protein in cell culture. In addition to potent inhibition in a cell-based assay (IC50 < 100 nM), these inhibitors display impressive selectivity against other biologically relevant aspartyl proteases.
ACS Publications