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Oncogene
Article
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Oncogene
Article . 2014 . Peer-reviewed
License: Springer TDM
Data sources: Crossref
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ATR inhibition preferentially targets homologous recombination-deficient tumor cells

Authors: Krajewska, M.; Fehrmann, R. S. N.; Schoonen, P. M.; Labib, S.; de Vries, E. G. E.; Franke, L.; van Vugt, M. A. T. M.;

ATR inhibition preferentially targets homologous recombination-deficient tumor cells

Abstract

Homologous recombination (HR) is required for faithful repair of double-strand DNA breaks. Defects in HR repair cause severe genomic instability and challenge cellular viability. Paradoxically, various cancers are HR defective and have apparently acquired characteristics to survive genomic instability. We aimed to identify these characteristics to uncover therapeutic targets for HR-deficient cancers. Cytogenetic analysis of 1143 ovarian cancers showed that the degree of genomic instability was correlated to amplification of replication checkpoint genes ataxia telangiectasia and Rad3-related kinase (ATR) and CHEK1. To test whether genomic instability leads to increased reliance on replication checkpoint signaling, we inactivated Rad51 to model HR-related genomic instability. Rad51 inactivation caused defective HR repair and induced aberrant replication dynamics. Notably, inhibition of Rad51 led to increased ATR/checkpoint kinase-1 (Chk1)-mediated replication stress signaling. Importantly, inhibition of ATR or Chk1 preferentially killed HR-deficient cancer cells. Combined, our data show that defective HR caused by Rad51 inhibition results in differential sensitivity for ATR and Chk1 inhibitors, implicating replication checkpoint kinases as potential drug targets for HR-defective cancers.

Country
Netherlands
Related Organizations
Keywords

Cell Survival, CANCER SUSCEPTIBILITY GENE, INDUCED REPLICATIVE STRESS, Antineoplastic Agents, Ataxia Telangiectasia Mutated Proteins, Thiophenes, EMBRYONIC CELLULAR PROLIFERATION, MOUSE, MAMMALIAN-CELLS, Neoplasms, Humans, Urea, Molecular Targeted Therapy, Sulfones, Homologous Recombination, MUTATIONS, BRCA2, TRANSFORMATION, STRAND BREAK REPAIR, Drug Resistance, Neoplasm, Pyrazines, Checkpoint Kinase 1, MCF-7 Cells, RAD51 RECOMBINASE, Protein Kinases, HeLa Cells, Signal Transduction

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    82
    popularity
    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
    Top 10%
    influence
    This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    Top 10%
    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
    Top 10%
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selected citations
These citations are derived from selected sources.
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
82
Top 10%
Top 10%
Top 10%
bronze