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Keap1 loss promotes Kras-driven lung cancer and results in dependence on glutaminolysis.

作者信息

Romero Rodrigo, Sayin Volkan I, Davidson Shawn M, Bauer Matthew R, Singh Simranjit X, LeBoeuf Sarah E, Karakousi Triantafyllia R, Ellis Donald C, Bhutkar Arjun, Sánchez-Rivera Francisco J, Subbaraj Lakshmipriya, Martinez Britney, Bronson Roderick T, Prigge Justin R, Schmidt Edward E, Thomas Craig J, Goparaju Chandra, Davies Angela, Dolgalev Igor, Heguy Adriana, Allaj Viola, Poirier John T, Moreira Andre L, Rudin Charles M, Pass Harvey I, Vander Heiden Matthew G, Jacks Tyler, Papagiannakopoulos Thales

机构信息

Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, Massachusetts, USA.

Department of Biology, Massachusetts Institute of Technology, Cambridge, Massachusetts, USA.

出版信息

Nat Med. 2017 Nov;23(11):1362-1368. doi: 10.1038/nm.4407. Epub 2017 Oct 2.


DOI:10.1038/nm.4407
PMID:28967920
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5677540/
Abstract

Treating KRAS-mutant lung adenocarcinoma (LUAD) remains a major challenge in cancer treatment given the difficulties associated with directly inhibiting the KRAS oncoprotein. One approach to addressing this challenge is to define mutations that frequently co-occur with those in KRAS, which themselves may lead to therapeutic vulnerabilities in tumors. Approximately 20% of KRAS-mutant LUAD tumors carry loss-of-function mutations in the KEAP1 gene encoding Kelch-like ECH-associated protein 1 (refs. 2, 3, 4), a negative regulator of nuclear factor erythroid 2-like 2 (NFE2L2; hereafter NRF2), which is the master transcriptional regulator of the endogenous antioxidant response. The high frequency of mutations in KEAP1 suggests an important role for the oxidative stress response in lung tumorigenesis. Using a CRISPR-Cas9-based approach in a mouse model of KRAS-driven LUAD, we examined the effects of Keap1 loss in lung cancer progression. We show that loss of Keap1 hyperactivates NRF2 and promotes KRAS-driven LUAD in mice. Through a combination of CRISPR-Cas9-based genetic screening and metabolomic analyses, we show that Keap1- or Nrf2-mutant cancers are dependent on increased glutaminolysis, and this property can be therapeutically exploited through the pharmacological inhibition of glutaminase. Finally, we provide a rationale for stratification of human patients with lung cancer harboring KRAS/KEAP1- or KRAS/NRF2-mutant lung tumors as likely to respond to glutaminase inhibition.

摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27f/5677540/a7638ac94c2c/nihms901248f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27f/5677540/9d3a007a3b9a/nihms901248f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27f/5677540/a20c780f13ee/nihms901248f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27f/5677540/42d21fd0c183/nihms901248f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27f/5677540/a7638ac94c2c/nihms901248f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27f/5677540/9d3a007a3b9a/nihms901248f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27f/5677540/a20c780f13ee/nihms901248f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27f/5677540/42d21fd0c183/nihms901248f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27f/5677540/a7638ac94c2c/nihms901248f4.jpg

相似文献

[1]
Keap1 loss promotes Kras-driven lung cancer and results in dependence on glutaminolysis.

Nat Med. 2017-11

[2]
LKB1 and KEAP1/NRF2 Pathways Cooperatively Promote Metabolic Reprogramming with Enhanced Glutamine Dependence in -Mutant Lung Adenocarcinoma.

Cancer Res. 2019-4-30

[3]
Keap1 mutation renders lung adenocarcinomas dependent on Slc33a1.

Nat Cancer. 2020-6

[4]
loss promotes -driven lung adenocarcinoma and results in Psat1-mediated glutamate dependence.

EMBO Mol Med. 2019-6

[5]
Distinct initiating events underpin the immune and metabolic heterogeneity of KRAS-mutant lung adenocarcinoma.

Nat Commun. 2019-9-13

[6]
Diminished Efficacy of Programmed Death-(Ligand)1 Inhibition in STK11- and KEAP1-Mutant Lung Adenocarcinoma Is Affected by KRAS Mutation Status.

J Thorac Oncol. 2022-3

[7]
Mutations in the KEAP1-NFE2L2 Pathway Define a Molecular Subset of Rapidly Progressing Lung Adenocarcinoma.

J Thorac Oncol. 2019-7-16

[8]
Clinicopathological, microenvironmental and genetic determinants of molecular subtypes in KEAP1/NRF2-mutant lung cancer.

Int J Cancer. 2018-12-4

[9]
Molecular markers of metastatic disease in KRAS-mutant lung adenocarcinoma.

Ann Oncol. 2023-7

[10]
Phase 1 Trial of MLN0128 (Sapanisertib) and CB-839 HCl (Telaglenastat) in Patients With Advanced NSCLC (NCI 10327): Rationale and Study Design.

Clin Lung Cancer. 2021-1

引用本文的文献

[1]
Interplay of oxidative stress and antioxidant mechanisms in cancer development and progression.

Arch Toxicol. 2025-9-4

[2]
Beyond the Tissue: Unlocking NSCLC Treatment Potential Through Liquid Biopsy.

Genes (Basel). 2025-8-13

[3]
Epigenetic Mechanisms Governing Nrf2 Expression and Its Role in Ferroptosis.

Biomedicines. 2025-8-5

[4]
Targeting FSP1 triggers ferroptosis in lung cancer.

bioRxiv. 2025-8-11

[5]
NRF2 activation in cancer and overview of NRF2 small molecule inhibitors.

Arch Pharm Res. 2025-8-15

[6]
Somatic CRISPR tumorigenesis and multiomic analysis reveal a pentose phosphate pathway disruption vulnerability in MPNSTs.

Sci Adv. 2025-8-15

[7]
Oncogenic NFE2L2 mutations in plasma ctDNA and tumors are predictors and prognosticators of chemoradiation therapy in resectable esophageal squamous cell carcinoma.

Br J Cancer. 2025-8-8

[8]
Tobacco smoke alters the trajectory of lung adenocarcinoma evolution via effects on somatic selection and epistasis.

bioRxiv. 2025-7-25

[9]
Identification of a BACH1 lung cancer signature: A novel tool for understanding BACH1 biology and identifying new inhibitors.

Redox Biol. 2025-7-23

[10]
Development of PROTACs for targeted degradation of oncogenic TRK fusions.

bioRxiv. 2025-6-24

本文引用的文献

[1]
KEAP1 loss modulates sensitivity to kinase targeted therapy in lung cancer.

Elife. 2017-2-1

[2]
Keap1/Nrf2 pathway in kidney cancer: frequent methylation of KEAP1 gene promoter in clear renal cell carcinoma.

Oncotarget. 2017-2-14

[3]
Altered metabolite levels in cancer: implications for tumour biology and cancer therapy.

Nat Rev Cancer. 2016-9-23

[4]
Recurrent Loss of NFE2L2 Exon 2 Is a Mechanism for Nrf2 Pathway Activation in Human Cancers.

Cell Rep. 2016-9-6

[5]
From Krebs to clinic: glutamine metabolism to cancer therapy.

Nat Rev Cancer. 2016-10

[6]
High-throughput Phenotyping of Lung Cancer Somatic Mutations.

Cancer Cell. 2016-8-8

[7]
NRF2 Promotes Tumor Maintenance by Modulating mRNA Translation in Pancreatic Cancer.

Cell. 2016-8-11

[8]
Whole-organism lineage tracing by combinatorial and cumulative genome editing.

Science. 2016-7-29

[9]
NRF2 Intensifies Host Defense Systems to Prevent Lung Carcinogenesis, but After Tumor Initiation Accelerates Malignant Cell Growth.

Cancer Res. 2016-3-28

[10]
Multiplexed pancreatic genome engineering and cancer induction by transfection-based CRISPR/Cas9 delivery in mice.

Nat Commun. 2016-2-26

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