Waking up dormant tumor suppressor genes with zinc fingers, TALEs and the CRISPR/dCas9 system

The aberrant epigenetic silencing of tumor suppressor genes (TSGs) plays a major role during carcinogenesis and regaining these dormant functions by engineering of sequence-specific epigenome editing tools offers a unique opportunity for targeted therapies. However, effectively normalizing the expre...

Full description

Bibliographic Details
Main Authors: Garcia-Bloj, B., Moses, C., Sgro, A., Plani-Lam, J., Arooj, Mahira, Duffy, C., Thiruvengadam, S., Sorolla, A., Rashwan, R., Mancera, Ricardo, Leisewitz, A., Swift-Scanlan, T., Corvalan, A., Blancafort, P.
Format: Journal Article
Published: Impact Journals LLC 2016
Online Access:http://hdl.handle.net/20.500.11937/22885
_version_ 1848750997927624704
author Garcia-Bloj, B.
Moses, C.
Sgro, A.
Plani-Lam, J.
Arooj, Mahira
Duffy, C.
Thiruvengadam, S.
Sorolla, A.
Rashwan, R.
Mancera, Ricardo
Leisewitz, A.
Swift-Scanlan, T.
Corvalan, A.
Blancafort, P.
author_facet Garcia-Bloj, B.
Moses, C.
Sgro, A.
Plani-Lam, J.
Arooj, Mahira
Duffy, C.
Thiruvengadam, S.
Sorolla, A.
Rashwan, R.
Mancera, Ricardo
Leisewitz, A.
Swift-Scanlan, T.
Corvalan, A.
Blancafort, P.
author_sort Garcia-Bloj, B.
building Curtin Institutional Repository
collection Online Access
description The aberrant epigenetic silencing of tumor suppressor genes (TSGs) plays a major role during carcinogenesis and regaining these dormant functions by engineering of sequence-specific epigenome editing tools offers a unique opportunity for targeted therapies. However, effectively normalizing the expression and regaining tumor suppressive functions of silenced TSGs by artificial transcription factors (ATFs) still remains a major challenge. Herein we describe novel combinatorial strategies for the potent reactivation of two class II TSGs, MASPIN and REPRIMO, in cell lines with varying epigenetic states, using the CRISPR/dCas9 associated system linked to a panel of effector domains (VP64, p300, VPR and SAM complex), as well as with protein-based ATFs, Zinc Fingers and TALEs. We found that co-delivery of multiple effector domains using a combination of CRISPR/dCas9 and TALEs or SAM complex maximized activation in highly methylated promoters. In particular, CRISPR/dCas9 VPR with SAM upregulated MASPIN mRNA (22,145-fold change) in H157 lung cancer cells, with accompanying re-expression of MASPIN protein, which led to a concomitant inhibition of cell proliferation and induction of apoptotic cell death. Consistently, CRISPR/dCas9 VP64 with SAM upregulated REPRIMO (680-fold change), which led to phenotypic reprogramming in AGS gastric cancer cells. Altogether, our results outlined novel sequence-specific, combinatorial epigenome editing approaches to reactivate highly methylated TSGs as a promising therapy for cancer and other diseases.
first_indexed 2025-11-14T07:45:44Z
format Journal Article
id curtin-20.500.11937-22885
institution Curtin University Malaysia
institution_category Local University
last_indexed 2025-11-14T07:45:44Z
publishDate 2016
publisher Impact Journals LLC
recordtype eprints
repository_type Digital Repository
spelling curtin-20.500.11937-228852017-09-13T13:57:42Z Waking up dormant tumor suppressor genes with zinc fingers, TALEs and the CRISPR/dCas9 system Garcia-Bloj, B. Moses, C. Sgro, A. Plani-Lam, J. Arooj, Mahira Duffy, C. Thiruvengadam, S. Sorolla, A. Rashwan, R. Mancera, Ricardo Leisewitz, A. Swift-Scanlan, T. Corvalan, A. Blancafort, P. The aberrant epigenetic silencing of tumor suppressor genes (TSGs) plays a major role during carcinogenesis and regaining these dormant functions by engineering of sequence-specific epigenome editing tools offers a unique opportunity for targeted therapies. However, effectively normalizing the expression and regaining tumor suppressive functions of silenced TSGs by artificial transcription factors (ATFs) still remains a major challenge. Herein we describe novel combinatorial strategies for the potent reactivation of two class II TSGs, MASPIN and REPRIMO, in cell lines with varying epigenetic states, using the CRISPR/dCas9 associated system linked to a panel of effector domains (VP64, p300, VPR and SAM complex), as well as with protein-based ATFs, Zinc Fingers and TALEs. We found that co-delivery of multiple effector domains using a combination of CRISPR/dCas9 and TALEs or SAM complex maximized activation in highly methylated promoters. In particular, CRISPR/dCas9 VPR with SAM upregulated MASPIN mRNA (22,145-fold change) in H157 lung cancer cells, with accompanying re-expression of MASPIN protein, which led to a concomitant inhibition of cell proliferation and induction of apoptotic cell death. Consistently, CRISPR/dCas9 VP64 with SAM upregulated REPRIMO (680-fold change), which led to phenotypic reprogramming in AGS gastric cancer cells. Altogether, our results outlined novel sequence-specific, combinatorial epigenome editing approaches to reactivate highly methylated TSGs as a promising therapy for cancer and other diseases. 2016 Journal Article http://hdl.handle.net/20.500.11937/22885 10.18632/oncotarget.11142 Impact Journals LLC fulltext
spellingShingle Garcia-Bloj, B.
Moses, C.
Sgro, A.
Plani-Lam, J.
Arooj, Mahira
Duffy, C.
Thiruvengadam, S.
Sorolla, A.
Rashwan, R.
Mancera, Ricardo
Leisewitz, A.
Swift-Scanlan, T.
Corvalan, A.
Blancafort, P.
Waking up dormant tumor suppressor genes with zinc fingers, TALEs and the CRISPR/dCas9 system
title Waking up dormant tumor suppressor genes with zinc fingers, TALEs and the CRISPR/dCas9 system
title_full Waking up dormant tumor suppressor genes with zinc fingers, TALEs and the CRISPR/dCas9 system
title_fullStr Waking up dormant tumor suppressor genes with zinc fingers, TALEs and the CRISPR/dCas9 system
title_full_unstemmed Waking up dormant tumor suppressor genes with zinc fingers, TALEs and the CRISPR/dCas9 system
title_short Waking up dormant tumor suppressor genes with zinc fingers, TALEs and the CRISPR/dCas9 system
title_sort waking up dormant tumor suppressor genes with zinc fingers, tales and the crispr/dcas9 system
url http://hdl.handle.net/20.500.11937/22885