NDLI: A graphene oxide-based fluorescent scheme for the determination of the activity of the β-site amyloid precursor protein (BACE1) and its inhibitors

Content Provider	Springer Nature Link
Author	Liu, Lin Xia, Ning Yu, Jie
Copyright Year	2015
Abstract	The enzyme cleaving the beta-site amyloid precursor protein (BACE1) is a prime therapeutic target for treatment of Alzheimer’s disease (AD). Hence, improved high-throughput methods for probing the activity of BACE1 are crucial with respect to the discovery of novel drugs for treatment and prevention of AD. We describe a graphene oxide (GO)-based fluorescent platform for the determination of BACE1 activity and screening of its inhibitors. It is found that covalent linkage of the fluorescein isothiocyanate (FITC)-labeled enzyme substrate (of sequence GTEEISEVNLDAEFRHDSGYKK) to GO results in quenching of the FITC fluorescence, but that on peptide cleavage by BACE1, FITC is released from the GO surface and fluorescence is restored. In contrast to other fluorescent assays, the method presented here shows much higher quenching efficiency and sensitivity, and it can be used at pH value of 4.5 where BACE1 exhibits higher activity. The inhibition of BACE1 activity by a potential inhibitor results in retarded fluorescence recovery. The half-maximum inhibition value of a well-known BACE1 inhibitor was found to be 82.7 nM, which is in agreement with the value reported earlier. In our perception, this method represents a valuable tool for screening of BACE1 inhibitors and discovery of AD drugs in a high-throughput screening format using microplate readers. Graphical abstract Covalent immobilization of a fluorescently labeled substrate for the beta-site amyloid precursor protein (BACE1) on graphene oxide (GO) induces fluorescence quenching. Peptide cleavage by BACE1 leads to the release of FITC from the GO surface; consequently, an enhanced fluorescence signal from FITC is observed
Starting Page	265
Ending Page	271
Page Count	7
File Format	PDF
ISSN	00263672
Journal	Microchimica Acta
Volume Number	183
Issue Number	1
e-ISSN	14365073
Language	English
Publisher	Springer Vienna
Publisher Date	2015-09-23
Publisher Place	Vienna
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Beta-site amyloid precursor protein BACE1 Enzyme substrate Enzyme inhibition Fluorescent assay Quenching Alzheimer’s disease Nanochemistry Nanotechnology Characterization and Evaluation of Materials Analytical Chemistry Microengineering
Content Type	Text
Resource Type	Article
Subject	Analytical Chemistry

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