False HDAC Inhibition by Aurone Compound.

Abstract:

:Fluorescence assays are useful tools for estimating enzymatic activity. Their simplicity and manageability make them suitable for screening enzyme inhibitors in drug discovery studies. However, researchers need to pay attention to compounds that show auto-fluorescence and quench fluorescence, because such compounds lower the accuracy of the fluorescence assay systems by producing false-positive or negative results. In this study, we found that aurone compound 7, which has been reported as a histone deacetylase (HDAC) inhibitor, gave false-positive results. Although compound 7 was identified by an in vitro HDAC fluorescence assay, it did not show HDAC inhibitory activity in a cell-based assay, leading us to suspect its in vitro HDAC inhibitory activity. As a result of verification experiments, we found that compound 7 interferes with the HDAC fluorescence assay by quenching the HDAC fluorescence signal. Our findings underscore the faults of fluorescence assays and call attention to careless interpretation.

authors

Itoh Y,Suzuki M,Matsui T,Ota Y,Hui Z,Tsubaki K,Suzuki T

doi

10.1248/cpb.c16-00123

subject

Has Abstract

pub_date

2016-01-01 00:00:00

pages

1124-8

issue

8

eissn

0009-2363

issn

1347-5223

journal_volume

64

pub_type

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