Fluorine-18-Labeled PET Radiotracers for Imaging Tryptophan Uptake and Metabolism: a Systematic Review

John, Flóra; Muzik, Otto; Mittal, Sandeep; Juhász, Csaba

doi:10.1007/s11307-019-01430-6

Cited by 25 publications

(15 citation statements)

References 67 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Imaging of tryptophan metabolism and presence of IDO in the tumor metabolism is performed by using the clinical available a-[ 11 C]methyl-L-tryptophan (AMT) PET tracer (262), in the context of breast, lung cancer and gliomas (263). One phase II study is enlisted on clinicaltrials.gov to investigate [ 11 C]AMT as a predictive imaging biomarker response to immunotherapy with the PD-1 inhibitor Pembrolizumab in melanoma patients (NCT03089606), but this study is not yet recruiting.…”

Section: Tryptophan Metabolismmentioning

confidence: 99%

Imaging the Rewired Metabolism in Lung Cancer in Relation to Immune Therapy

et al. 2022

View full text Add to dashboard Cite

Metabolic reprogramming is recognized as one of the hallmarks of cancer. Alterations in the micro-environmental metabolic characteristics are recognized as important tools for cancer cells to interact with the resident and infiltrating T-cells within this tumor microenvironment. Cancer-induced metabolic changes in the micro-environment also affect treatment outcomes. In particular, immune therapy efficacy might be blunted because of somatic mutation-driven metabolic determinants of lung cancer such as acidity and oxygenation status. Based on these observations, new onco-immunological treatment strategies increasingly include drugs that interfere with metabolic pathways that consequently affect the composition of the lung cancer tumor microenvironment (TME). Positron emission tomography (PET) imaging has developed a wide array of tracers targeting metabolic pathways, originally intended to improve cancer detection and staging. Paralleling the developments in understanding metabolic reprogramming in cancer cells, as well as its effects on stromal, immune, and endothelial cells, a wave of studies with additional imaging tracers has been published. These tracers are yet underexploited in the perspective of immune therapy. In this review, we provide an overview of currently available PET tracers for clinical studies and discuss their potential roles in the development of effective immune therapeutic strategies, with a focus on lung cancer. We report on ongoing efforts that include PET/CT to understand the outcomes of interactions between cancer cells and T-cells in the lung cancer microenvironment, and we identify areas of research which are yet unchartered. Thereby, we aim to provide a starting point for molecular imaging driven studies to understand and exploit metabolic features of lung cancer to optimize immune therapy.

show abstract

Section: Tryptophan Metabolismmentioning

confidence: 99%

Imaging the Rewired Metabolism in Lung Cancer in Relation to Immune Therapy

et al. 2022

View full text Add to dashboard Cite

show abstract

“…Imaging of tryptophan metabolism and presence of IDO in the tumor metabolism is performed by using the clinical available a-[ 11 C]methyl-L-tryptophan (AMT) PET tracer (262), in the context of breast, lung cancer and gliomas (263). One phase II study is enlisted on clinicaltrials.gov to investigate [ 11 C]AMT as a predictive imaging biomarker of response to immunotherapy with the PD-1 inhibitor Pembrolizumab in melanoma patients (NCT03089606), but this study is not yet recruiting.…”

Section: Tryptophan Metabolismmentioning

confidence: 99%

Understanding the Interplay Between the Tumor Immune Microenvironment and Genetic Alterations in Thoracic Malignancies

2022

Frontiers Research Topics

View full text Add to dashboard Cite

Frontiers is more than just an open-access publisher of scholarly articles: it is a pioneering approach to the world of academia, radically improving the way scholarly research is managed. The grand vision of Frontiers is a world where all people have an equal opportunity to seek, share and generate knowledge. Frontiers provides immediate and permanent online open access to all its publications, but this alone is not enough to realize our grand goals. Frontiers Journal SeriesThe Frontiers Journal Series is a multi-tier and interdisciplinary set of open-access, online journals, promising a paradigm shift from the current review, selection and dissemination processes in academic publishing. All Frontiers journals are driven by researchers for researchers; therefore, they constitute a service to the scholarly community. At the same time, the Frontiers Journal Series operates on a revolutionary invention, the tiered publishing system, initially addressing specific communities of scholars, and gradually climbing up to broader public understanding, thus serving the interests of the lay society, too. Dedication to QualityEach Frontiers article is a landmark of the highest quality, thanks to genuinely collaborative interactions between authors and review editors, who include some of the world's best academicians. Research must be certified by peers before entering a stream of knowledge that may eventually reach the public -and shape society; therefore, Frontiers only applies the most rigorous and unbiased reviews. Frontiers revolutionizes research publishing by freely delivering the most outstanding research, evaluated with no bias from both the academic and social point of view. By applying the most advanced information technologies, Frontiers is catapulting scholarly publishing into a new generation.

show abstract

“…However, challenges remain regarding metabolic pathway specificity, 14 synthesis feasibility, and in vivo stability. 12,14,15 Our lab demonstrated that the PET imaging outcomes for B16F10 tumor-bearing mice could be improved by fluorine substitution of the hydrogen atom at the 5-position of AMT, resulting 5-[ 18 F]F-AMT. 16 However, as a multistep synthesis starting with L-Trp, the production of the precursor was complicated.…”

Section: ■ Introductionmentioning

confidence: 99%

Development of [¹⁸F]F-5-OMe-Tryptophans through Photoredox Radiofluorination: A New Method to Access Tryptophan-Based PET Agents

Zhong

et al. 2023

J. Med. Chem.

View full text Add to dashboard Cite

Although various radiolabeled tryptophan analogs have been developed to monitor tryptophan metabolism using positron emission tomography (PET) for various human diseases including melanoma and other cancers, their application can be limited due to the complicated synthesis process. In this study, we demonstrated that photoredox radiofluorination represents a simple method to access novel tryptophan-based PET agents. In brief, 4-F-5-OMe-tryptophans (L/D-T13) and 6-F-5-OMe-tryptophans (L/D-T18) were easily synthesized. The 18 F-labeled analogs were produced by photoredox radiofluorination with radiochemical yields ranging from 2.6 ± 0.5% to 32.4 ± 4.1% (3 ≤ n ≤ 5, enantiomeric excess ≥ 99.0%) and over 98.0% radiochemical purity. Small animal imaging showed that L-[ 18 F]T13 achieved 9.58 ± 0.26%ID/g tumor uptake and good contrast in B16F10 tumor-bearing mice (n = 3). Clearly, L-[ 18 F]T13 exhibited prominent tumor uptake, warranting future evaluations of its potential usage in precise immunotherapy monitoring.

show abstract

Fluorine-18-Labeled PET Radiotracers for Imaging Tryptophan Uptake and Metabolism: a Systematic Review

Cited by 25 publications

References 67 publications

Imaging the Rewired Metabolism in Lung Cancer in Relation to Immune Therapy

Imaging the Rewired Metabolism in Lung Cancer in Relation to Immune Therapy

Understanding the Interplay Between the Tumor Immune Microenvironment and Genetic Alterations in Thoracic Malignancies

Development of [¹⁸F]F-5-OMe-Tryptophans through Photoredox Radiofluorination: A New Method to Access Tryptophan-Based PET Agents

Contact Info

Product

Resources

About

Fluorine-18-Labeled PET Radiotracers for Imaging Tryptophan Uptake and Metabolism: a Systematic Review

Cited by 25 publications

References 67 publications

Imaging the Rewired Metabolism in Lung Cancer in Relation to Immune Therapy

Imaging the Rewired Metabolism in Lung Cancer in Relation to Immune Therapy

Understanding the Interplay Between the Tumor Immune Microenvironment and Genetic Alterations in Thoracic Malignancies

Development of [18F]F-5-OMe-Tryptophans through Photoredox Radiofluorination: A New Method to Access Tryptophan-Based PET Agents

Contact Info

Product

Resources

About

Development of [¹⁸F]F-5-OMe-Tryptophans through Photoredox Radiofluorination: A New Method to Access Tryptophan-Based PET Agents