Imaging NRF2 activation in non-small cell lung cancer with positron emission tomography

Abstract Mutations in the NRF2-KEAP1 pathway are common in non-small cell lung cancer (NSCLC) and confer broad-spectrum therapeutic resistance, leading to poor outcomes. Currently, there is no means to non-invasively identify NRF2 activation in living subjects. Here, we show that positron emission t...

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Main Authors: Hannah E. Greenwood, Abigail R. Barber, Richard S. Edwards, Will E. Tyrrell, Madeleine E. George, Sofia N. dos Santos, Friedrich Baark, Muhammet Tanc, Eman Khalil, Aimee Falzone, Nathan P. Ward, Janine M. DeBlasi, Laura Torrente, Pritin N. Soni, David R. Pearce, George Firth, Lydia M. Smith, Oskar Vilhelmsson Timmermand, Ariana Huebner, Charles Swanton, Robert E. Hynds, Gina M. DeNicola, Timothy H. Witney
Format: Article
Language:English
Published: Nature Portfolio 2024-12-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-024-54852-4
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author Hannah E. Greenwood
Abigail R. Barber
Richard S. Edwards
Will E. Tyrrell
Madeleine E. George
Sofia N. dos Santos
Friedrich Baark
Muhammet Tanc
Eman Khalil
Aimee Falzone
Nathan P. Ward
Janine M. DeBlasi
Laura Torrente
Pritin N. Soni
David R. Pearce
George Firth
Lydia M. Smith
Oskar Vilhelmsson Timmermand
Ariana Huebner
Charles Swanton
Robert E. Hynds
Gina M. DeNicola
Timothy H. Witney
author_facet Hannah E. Greenwood
Abigail R. Barber
Richard S. Edwards
Will E. Tyrrell
Madeleine E. George
Sofia N. dos Santos
Friedrich Baark
Muhammet Tanc
Eman Khalil
Aimee Falzone
Nathan P. Ward
Janine M. DeBlasi
Laura Torrente
Pritin N. Soni
David R. Pearce
George Firth
Lydia M. Smith
Oskar Vilhelmsson Timmermand
Ariana Huebner
Charles Swanton
Robert E. Hynds
Gina M. DeNicola
Timothy H. Witney
author_sort Hannah E. Greenwood
collection DOAJ
description Abstract Mutations in the NRF2-KEAP1 pathway are common in non-small cell lung cancer (NSCLC) and confer broad-spectrum therapeutic resistance, leading to poor outcomes. Currently, there is no means to non-invasively identify NRF2 activation in living subjects. Here, we show that positron emission tomography imaging with the system xc − radiotracer, [18F]FSPG, provides a sensitive and specific marker of NRF2 activation in orthotopic, patient-derived, and genetically engineered mouse models of NSCLC. We found a NRF2-related gene expression signature in a large cohort of NSCLC patients, suggesting an opportunity to preselect patients prior to [18F]FSPG imaging. Furthermore, we reveal that system xc − is a metabolic vulnerability that can be therapeutically targeted with an antibody-drug conjugate for sustained tumour growth suppression. Overall, our results establish [18F]FSPG as a predictive marker of therapy resistance in NSCLC and provide the basis for the clinical evaluation of both imaging and therapeutic agents that target this important antioxidant pathway.
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spelling doaj-art-3dcf089945564aceb0bdbed94a00b1bb2024-12-22T12:36:13ZengNature PortfolioNature Communications2041-17232024-12-0115111410.1038/s41467-024-54852-4Imaging NRF2 activation in non-small cell lung cancer with positron emission tomographyHannah E. Greenwood0Abigail R. Barber1Richard S. Edwards2Will E. Tyrrell3Madeleine E. George4Sofia N. dos Santos5Friedrich Baark6Muhammet Tanc7Eman Khalil8Aimee Falzone9Nathan P. Ward10Janine M. DeBlasi11Laura Torrente12Pritin N. Soni13David R. Pearce14George Firth15Lydia M. Smith16Oskar Vilhelmsson Timmermand17Ariana Huebner18Charles Swanton19Robert E. Hynds20Gina M. DeNicola21Timothy H. Witney22School of Biomedical Engineering & Imaging Sciences, King’s College London, St Thomas’ HospitalSchool of Biomedical Engineering & Imaging Sciences, King’s College London, St Thomas’ HospitalSchool of Biomedical Engineering & Imaging Sciences, King’s College London, St Thomas’ HospitalSchool of Biomedical Engineering & Imaging Sciences, King’s College London, St Thomas’ HospitalSchool of Biomedical Engineering & Imaging Sciences, King’s College London, St Thomas’ HospitalSchool of Biomedical Engineering & Imaging Sciences, King’s College London, St Thomas’ HospitalSchool of Biomedical Engineering & Imaging Sciences, King’s College London, St Thomas’ HospitalSchool of Biomedical Engineering & Imaging Sciences, King’s College London, St Thomas’ HospitalSchool of Biomedical Engineering & Imaging Sciences, King’s College London, St Thomas’ HospitalDepartment of Metabolism and Physiology, H. Lee Moffitt Cancer CenterDepartment of Metabolism and Physiology, H. Lee Moffitt Cancer CenterDepartment of Metabolism and Physiology, H. Lee Moffitt Cancer CenterDepartment of Metabolism and Physiology, H. Lee Moffitt Cancer CenterDepartment of Metabolism and Physiology, H. Lee Moffitt Cancer CenterCRUK Lung Cancer Centre of Excellence, UCL Cancer Institute, University College LondonSchool of Biomedical Engineering & Imaging Sciences, King’s College London, St Thomas’ HospitalSchool of Biomedical Engineering & Imaging Sciences, King’s College London, St Thomas’ HospitalSchool of Biomedical Engineering & Imaging Sciences, King’s College London, St Thomas’ HospitalCRUK Lung Cancer Centre of Excellence, UCL Cancer Institute, University College LondonCRUK Lung Cancer Centre of Excellence, UCL Cancer Institute, University College LondonCRUK Lung Cancer Centre of Excellence, UCL Cancer Institute, University College LondonDepartment of Metabolism and Physiology, H. Lee Moffitt Cancer CenterSchool of Biomedical Engineering & Imaging Sciences, King’s College London, St Thomas’ HospitalAbstract Mutations in the NRF2-KEAP1 pathway are common in non-small cell lung cancer (NSCLC) and confer broad-spectrum therapeutic resistance, leading to poor outcomes. Currently, there is no means to non-invasively identify NRF2 activation in living subjects. Here, we show that positron emission tomography imaging with the system xc − radiotracer, [18F]FSPG, provides a sensitive and specific marker of NRF2 activation in orthotopic, patient-derived, and genetically engineered mouse models of NSCLC. We found a NRF2-related gene expression signature in a large cohort of NSCLC patients, suggesting an opportunity to preselect patients prior to [18F]FSPG imaging. Furthermore, we reveal that system xc − is a metabolic vulnerability that can be therapeutically targeted with an antibody-drug conjugate for sustained tumour growth suppression. Overall, our results establish [18F]FSPG as a predictive marker of therapy resistance in NSCLC and provide the basis for the clinical evaluation of both imaging and therapeutic agents that target this important antioxidant pathway.https://doi.org/10.1038/s41467-024-54852-4
spellingShingle Hannah E. Greenwood
Abigail R. Barber
Richard S. Edwards
Will E. Tyrrell
Madeleine E. George
Sofia N. dos Santos
Friedrich Baark
Muhammet Tanc
Eman Khalil
Aimee Falzone
Nathan P. Ward
Janine M. DeBlasi
Laura Torrente
Pritin N. Soni
David R. Pearce
George Firth
Lydia M. Smith
Oskar Vilhelmsson Timmermand
Ariana Huebner
Charles Swanton
Robert E. Hynds
Gina M. DeNicola
Timothy H. Witney
Imaging NRF2 activation in non-small cell lung cancer with positron emission tomography
Nature Communications
title Imaging NRF2 activation in non-small cell lung cancer with positron emission tomography
title_full Imaging NRF2 activation in non-small cell lung cancer with positron emission tomography
title_fullStr Imaging NRF2 activation in non-small cell lung cancer with positron emission tomography
title_full_unstemmed Imaging NRF2 activation in non-small cell lung cancer with positron emission tomography
title_short Imaging NRF2 activation in non-small cell lung cancer with positron emission tomography
title_sort imaging nrf2 activation in non small cell lung cancer with positron emission tomography
url https://doi.org/10.1038/s41467-024-54852-4
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