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Metabolic Imaging Detects Resistance to PI3Kα Inhibition Mediated by Persistent FOXM1 Expression in ER+ Breast Cancer.

Accepted version
Peer-reviewed

Type

Article

Change log

Authors

Ros, Susana 
Wright, Alan J 
D'Santos, Paula 
Hu, De-En 
Hesketh, Richard L 

Abstract

PIK3CA, encoding the PI3Kα isoform, is the most frequently mutated oncogene in estrogen receptor (ER)-positive breast cancer. Isoform-selective PI3K inhibitors are used clinically but intrinsic and acquired resistance limits their utility. Improved selection of patients that will benefit from these drugs requires predictive biomarkers. We show here that persistent FOXM1 expression following drug treatment is a biomarker of resistance to PI3Kα inhibition in ER+ breast cancer. FOXM1 drives expression of lactate dehydrogenase (LDH) but not hexokinase 2 (HK-II). The downstream metabolic changes can therefore be detected using MRI of LDH-catalyzed hyperpolarized 13C label exchange between pyruvate and lactate but not by positron emission tomography measurements of HK-II-mediated trapping of the glucose analog 2-deoxy-2-[18F]fluorodeoxyglucose. Rapid assessment of treatment response in breast cancer using this imaging method could help identify patients that benefit from PI3Kα inhibition and design drug combinations to counteract the emergence of resistance.

Description

Keywords

FDG-PET, FOXM1, MRI, PI3K alpha inhibition, biomarker, breast cancer, hexokinase 2, hyperpolarized [1-(13)C]pyruvate, lactate dehydrogenase, treatment response, Animals, Antineoplastic Combined Chemotherapy Protocols, Breast Neoplasms, Cell Line, Tumor, Class I Phosphatidylinositol 3-Kinases, Drug Resistance, Neoplasm, Female, Forkhead Box Protein M1, Fulvestrant, Humans, Imidazoles, MCF-7 Cells, Magnetic Resonance Imaging, Mice, Inbred NOD, Mice, Knockout, Mice, SCID, Oxazepines, Protein Kinase Inhibitors, Receptors, Estrogen, Tamoxifen, Xenograft Model Antitumor Assays

Journal Title

Cancer Cell

Conference Name

Journal ISSN

1535-6108
1878-3686

Volume Title

38

Publisher

Elsevier BV
Sponsorship
Cancer Research UK (CB4100)
Cancer Research UK (C14303/A17197)
Cancer Research Uk (None)
Cancer Research UK (C37096/A16673)
Cancer Research UK NIH
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