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(−)-CHANA, a Fluorogenic Probe for Detecting Amyloid Binding Alcohol Dehydrogenase HSD10 Activity in Living Cells

The association of 17-hydroxysteroid dehydrogenase 10 (HSD10)
with -amyloid in the brain is known to contribute to the progression of Alzheimer¡¯s
disease. Further, it has been shown that the interaction between the purified
HSD10 and -amyloid inhibits its enzymatic activity. However, to date no system
has been developed to enable the study of HSD10 activity in intact living
cells. To address this significant shortcoming, we have developed a novel fluorogenic
probe, ()-cyclohexenyl amino naphthalene alcohol [()-CHANA], to observe
and measure the activity of HSD10 in living cells. The oxidation of ()-CHANA by
HSD10 results in the production and accumulation of a fluorescent product, which
can be measured using real-time fluorescence microscopy. This compound permits
the measurement of mitochondrial HSD10 activity and its inhibition by both
a small molecule HSD10 inhibitor and by -amyloid, in living cells. Herein, we define
the parameters under which this probe can be used. This compound is likely to
prove useful in future investigations aimed at developing therapeutic compounds
targeting the HSD10--amyloid association.