Please use this identifier to cite or link to this item:
Scopus Web of Science® Altmetric
Type: Journal article
Title: Development of a novel cell-based assay system EPISSAY for screening epigenetic drugs and liposome formulated decitabine
Author: Lim, S.
Kumar, R.
Akkamsetty, Y.
Wang, W.
Ho, K.
Neilsen, P.
Walther, D.
Suetani, R.
Prestidge, C.
Callen, D.
Citation: BMC Cancer, 2013; 13(113):1-11
Publisher: BioMed Central Ltd.
Issue Date: 2013
ISSN: 1471-2407
Statement of
Sue Ping Lim, Raman Kumar, Yamini Akkamsetty, Wen Wang, Kristen Ho, Paul M. Neilsen, Diego J. Walther, Rachel J. Suetani, Clive Prestidge and David F. Callen
Abstract: BACKGROUND: Despite the potential of improving the delivery of epigenetic drugs, the subsequent assessment of changes in their epigenetic activity is largely dependent on the availability of a suitable and rapid screening bioassay. Here, we describe a cell-based assay system for screening gene reactivation. METHODS: A cell-based assay system (EPISSAY) was designed based on a silenced triple-mutated bacterial nitroreductase TMnfsB fused with Red-Fluorescent Protein (RFP) expressed in the non-malignant human breast cell line MCF10A. EPISSAY was validated using the target gene TXNIP, which has previously been shown to respond to epigenetic drugs. The potency of a epigenetic drug model, decitabine, formulated with PEGylated liposomes was also validated using this assay system. RESULTS: Following treatment with DNA methyltransferase (DNMT) and histone deacetylase (HDAC) inhibitors such as decitabine and vorinostat, increases in RFP expression were observed, indicating expression of RFP-TMnfsB. The EPISSAY system was then used to test the potency of decitabine, before and after PEGylated liposomal encapsulation. We observed a 50% higher potency of decitabine when encapsulated in PEGylated liposomes, which is likely to be due to its protection from rapid degradation. CONCLUSIONS: The EPISSAY bioassay system provides a novel and rapid system to compare the efficiencies of existing and newly formulated drugs that reactivate gene expression.
Keywords: Cell-based assay system; decitabine; liposomes; nanotechnology; CB1954; nitroreductase
Description: Extent: 11 p.
Rights: © 2013 Lim et al.; licensee BioMed Central Ltd. This is an Open Access article distributed under the terms of the CreativeCommons Attribution License (, which permits unrestricted use, distribution, andreproduction in any medium, provided the original work is properly cited.
RMID: 0020128750
DOI: 10.1186/1471-2407-13-113
Appears in Collections:Medicine publications

Files in This Item:
File Description SizeFormat 
hdl_79522.pdfPublished version604.37 kBAdobe PDFView/Open

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.