Skip to Content
Merck
  • BRG1 Loss Predisposes Lung Cancers to Replicative Stress and ATR Dependency.

BRG1 Loss Predisposes Lung Cancers to Replicative Stress and ATR Dependency.

Cancer research (2020-07-22)
Manav Gupta, Carla P Concepcion, Caroline G Fahey, Hasmik Keshishian, Arjun Bhutkar, Christine F Brainson, Francisco J Sanchez-Rivera, Patrizia Pessina, Jonathan Y Kim, Antoine Simoneau, Margherita Paschini, Mary C Beytagh, Caroline R Stanclift, Monica Schenone, D R Mani, Chendi Li, Audris Oh, Fei Li, Hai Hu, Angeliki Karatza, Roderick T Bronson, Alice T Shaw, Aaron N Hata, Kwok-Kin Wong, Lee Zou, Steven A Carr, Tyler Jacks, Carla F Kim
ABSTRACT

Inactivation of SMARCA4/BRG1, the core ATPase subunit of mammalian SWI/SNF complexes, occurs at very high frequencies in non-small cell lung cancers (NSCLC). There are no targeted therapies for this subset of lung cancers, nor is it known how mutations in BRG1 contribute to lung cancer progression. Using a combination of gain- and loss-of-function approaches, we demonstrate that deletion of BRG1 in lung cancer leads to activation of replication stress responses. Single-molecule assessment of replication fork dynamics in BRG1-deficient cells revealed increased origin firing mediated by the prelicensing protein, CDC6. Quantitative mass spectrometry and coimmunoprecipitation assays showed that BRG1-containing SWI/SNF complexes interact with RPA complexes. Finally, BRG1-deficient lung cancers were sensitive to pharmacologic inhibition of ATR. These findings provide novel mechanistic insight into BRG1-mutant lung cancers and suggest that their dependency on ATR can be leveraged therapeutically and potentially expanded to BRG1-mutant cancers in other tissues. SIGNIFICANCE: These findings indicate that inhibition of ATR is a promising therapy for the 10% of non-small cell lung cancer patients harboring mutations in SMARCA4/BRG1. GRAPHICAL ABSTRACT: http://cancerres.aacrjournals.org/content/canres/80/18/3841/F1.large.jpg.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
PTP Assay Kit 1, PTP Assay Kit 1 can be used to detect PTP-1B activity by dephosphorylation of the phosphopeptide (RRLIEDAEpYAARG) using malachite green detection, or by hydrolysis of pNPP.
Sigma-Aldrich
D-α-Tocopherol polyethylene glycol 1000 succinate, BioXtra, water soluble vitamin E conjugate
Sigma-Aldrich
Hydroxyurea, 98%, powder
Sigma-Aldrich
5-Chloro-2′-deoxyuridine, thymidine analog
Sigma-Aldrich
Dimethyl sulfoxide, sterile-filtered, BioPerformance Certified, meets EP, USP testing specifications, suitable for hybridoma