Integrated functional, gene expression and genomic analysis for the identification of cancer targets.

The majority of new drug approvals for cancer are based on existing therapeutic targets. One approach to the identification of novel targets is to perform high-throughput RNA interference (RNAi) cellular viability screens. We describe a novel approach combining RNAi screening in multiple cell lines...

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Main Authors: Elizabeth Iorns, Christopher J Lord, Anita Grigoriadis, Sarah McDonald, Kerry Fenwick, Alan Mackay, Charles A Mein, Rachael Natrajan, Kay Savage, Narinder Tamber, Jorge S Reis-Filho, Nicholas C Turner, Alan Ashworth
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2009-01-01
Series:PLoS ONE
Online Access:https://doi.org/10.1371/journal.pone.0005120
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author Elizabeth Iorns
Christopher J Lord
Anita Grigoriadis
Sarah McDonald
Kerry Fenwick
Alan Mackay
Charles A Mein
Rachael Natrajan
Kay Savage
Narinder Tamber
Jorge S Reis-Filho
Nicholas C Turner
Alan Ashworth
author_facet Elizabeth Iorns
Christopher J Lord
Anita Grigoriadis
Sarah McDonald
Kerry Fenwick
Alan Mackay
Charles A Mein
Rachael Natrajan
Kay Savage
Narinder Tamber
Jorge S Reis-Filho
Nicholas C Turner
Alan Ashworth
author_sort Elizabeth Iorns
collection DOAJ
description The majority of new drug approvals for cancer are based on existing therapeutic targets. One approach to the identification of novel targets is to perform high-throughput RNA interference (RNAi) cellular viability screens. We describe a novel approach combining RNAi screening in multiple cell lines with gene expression and genomic profiling to identify novel cancer targets. We performed parallel RNAi screens in multiple cancer cell lines to identify genes that are essential for viability in some cell lines but not others, suggesting that these genes constitute key drivers of cellular survival in specific cancer cells. This approach was verified by the identification of PIK3CA, silencing of which was selectively lethal to the MCF7 cell line, which harbours an activating oncogenic PIK3CA mutation. We combined our functional RNAi approach with gene expression and genomic analysis, allowing the identification of several novel kinases, including WEE1, that are essential for viability only in cell lines that have an elevated level of expression of this kinase. Furthermore, we identified a subset of breast tumours that highly express WEE1 suggesting that WEE1 could be a novel therapeutic target in breast cancer. In conclusion, this strategy represents a novel and effective strategy for the identification of functionally important therapeutic targets in cancer.
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spelling doaj-art-fe6d4e18e3ac4117937a53debf5472d22025-08-20T03:22:26ZengPublic Library of Science (PLoS)PLoS ONE1932-62032009-01-0144e512010.1371/journal.pone.0005120Integrated functional, gene expression and genomic analysis for the identification of cancer targets.Elizabeth IornsChristopher J LordAnita GrigoriadisSarah McDonaldKerry FenwickAlan MackayCharles A MeinRachael NatrajanKay SavageNarinder TamberJorge S Reis-FilhoNicholas C TurnerAlan AshworthThe majority of new drug approvals for cancer are based on existing therapeutic targets. One approach to the identification of novel targets is to perform high-throughput RNA interference (RNAi) cellular viability screens. We describe a novel approach combining RNAi screening in multiple cell lines with gene expression and genomic profiling to identify novel cancer targets. We performed parallel RNAi screens in multiple cancer cell lines to identify genes that are essential for viability in some cell lines but not others, suggesting that these genes constitute key drivers of cellular survival in specific cancer cells. This approach was verified by the identification of PIK3CA, silencing of which was selectively lethal to the MCF7 cell line, which harbours an activating oncogenic PIK3CA mutation. We combined our functional RNAi approach with gene expression and genomic analysis, allowing the identification of several novel kinases, including WEE1, that are essential for viability only in cell lines that have an elevated level of expression of this kinase. Furthermore, we identified a subset of breast tumours that highly express WEE1 suggesting that WEE1 could be a novel therapeutic target in breast cancer. In conclusion, this strategy represents a novel and effective strategy for the identification of functionally important therapeutic targets in cancer.https://doi.org/10.1371/journal.pone.0005120
spellingShingle Elizabeth Iorns
Christopher J Lord
Anita Grigoriadis
Sarah McDonald
Kerry Fenwick
Alan Mackay
Charles A Mein
Rachael Natrajan
Kay Savage
Narinder Tamber
Jorge S Reis-Filho
Nicholas C Turner
Alan Ashworth
Integrated functional, gene expression and genomic analysis for the identification of cancer targets.
PLoS ONE
title Integrated functional, gene expression and genomic analysis for the identification of cancer targets.
title_full Integrated functional, gene expression and genomic analysis for the identification of cancer targets.
title_fullStr Integrated functional, gene expression and genomic analysis for the identification of cancer targets.
title_full_unstemmed Integrated functional, gene expression and genomic analysis for the identification of cancer targets.
title_short Integrated functional, gene expression and genomic analysis for the identification of cancer targets.
title_sort integrated functional gene expression and genomic analysis for the identification of cancer targets
url https://doi.org/10.1371/journal.pone.0005120
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