
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.
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
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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| impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network. | Top 10% |
