Cancer Molecular Imaging

A special issue of Cancers (ISSN 2072-6694).

Deadline for manuscript submissions: closed (30 April 2020) | Viewed by 54234

Special Issue Editors


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Guest Editor
Cancer Imaging Centre, Department of Surgery and Cancer, Faculty of Medicine, Imperial College London, London W12 0HS, UK
Interests: discovery and development of new methods for experimental; clinical cancer molecular imaging

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Guest Editor
Department of Biomedical Sciences, University of Hull, Cottingham Road, Kingston upon Hull HU6 7RX, UK
Interests: PET radiochemistry; drug and radiopharmaceutical discovery; clinical translation
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Molecular imaging in oncology forms the keystone of personalised medicine and allows the interrogation of cancer pharmacology from a minimally invasive scan. The development of new functional imaging radiopharmaceuticals and their rapid implementation in phase I clinical trials is a facet of molecular imaging that has resulted in many promising radiopharmaceuticals that are likely to bring tremendous benefits to patients.

This Special Issue aims to consolidate the bench-to-bedside journey for developing radiopharmaceuticals. We welcome submissions that contribute to the field of Cancer Molecular Imaging, with focus towards selecting lead candidates from compound libraries, implementing radiochemistry, GMP manufacture and clinical translation. The field of molecular imaging is diverse, spanning from small molecule compounds to large biomolecule targeting vectors and from receptor-based radioligands to metabolism tracers; therefore, we hope to reflect the diversity of our field in this Special Issue.

Prof. Dr. Eric O. Aboagye
Dr. Louis Allott
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Cancers is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Radiopharmaceutical development
  • Radioligand screening
  • Radiolabeled biomolecules
  • Cancer pharmacology
  • Imaging metabolism
  • Receptor imaging
  • PET radiochemistry
  • GMP manufacture
  • Clinical translation

Published Papers (13 papers)

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Research

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14 pages, 11815 KiB  
Article
Tracing Nutrient Flux Following Monocarboxylate Transporter-1 Inhibition with AZD3965
by Marta Braga, Maciej Kaliszczak, Laurence Carroll, Zachary T. Schug, Kathrin Heinzmann, Nicoleta Baxan, Adrian Benito, Gabriel N. Valbuena, Stephen Stribbling, Alice Beckley, Gillian Mackay, Francesco Mauri, John Latigo, Chris Barnes, Hector Keun, Eyal Gottlieb and Eric O. Aboagye
Cancers 2020, 12(6), 1703; https://doi.org/10.3390/cancers12061703 - 26 Jun 2020
Cited by 8 | Viewed by 4121
Abstract
The monocarboxylate transporter 1 (MCT1) is a key element in tumor cell metabolism and inhibition of MCT1 with AZD3965 is undergoing clinical trials. We aimed to investigate nutrient fluxes associated with MCT1 inhibition by AZD3965 to identify possible biomarkers of drug action. We [...] Read more.
The monocarboxylate transporter 1 (MCT1) is a key element in tumor cell metabolism and inhibition of MCT1 with AZD3965 is undergoing clinical trials. We aimed to investigate nutrient fluxes associated with MCT1 inhibition by AZD3965 to identify possible biomarkers of drug action. We synthesized an 18F-labeled lactate analogue, [18F]-S-fluorolactate ([18F]-S-FL), that was used alongside [18F]fluorodeoxyglucose ([18F]FDG), and 13C-labeled glucose and lactate, to investigate the modulation of metabolism with AZD3965 in diffuse large B-cell lymphoma models in NOD/SCID mice. Comparative analysis of glucose and lactate-based probes showed a preference for glycolytic metabolism in vitro, whereas in vivo, both glucose and lactate were used as metabolic fuel. While intratumoral L-[1-13C]lactate and [18F]-S-FL were unchanged or lower at early (5 or 30 min) timepoints, these variables were higher compared to vehicle controls at 4 h following treatment with AZD3965, which indicates that inhibition of MCT1-mediated lactate import is reversed over time. Nonetheless, AZD3965 treatment impaired DLBCL tumor growth in mice. This was hypothesized to be a consequence of metabolic strain, as AZD3965 treatment showed a reduction in glycolytic intermediates and inhibition of the TCA cycle likely due to downregulated PDH activity. Glucose ([18F]FDG and D-[13C6]glucose) and lactate-based probes ([18F]-S-FL and L-[1-13C]lactate) can be successfully used as biomarkers for AZD3965 treatment. Full article
(This article belongs to the Special Issue Cancer Molecular Imaging)
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12 pages, 12893 KiB  
Article
Relationships and Qualitative Evaluation between Diffusion-Weighted Imaging and Pathologic Findings of Resected Lung Cancers
by Katsuo Usuda, Shun Iwai, Aika Yamagata, Atsushi Sekimura, Nozomu Motono, Munetaka Matoba, Mariko Doai, Sohsuke Yamada, Yoshimichi Ueda, Keiya Hirata and Hidetaka Uramoto
Cancers 2020, 12(5), 1194; https://doi.org/10.3390/cancers12051194 - 08 May 2020
Cited by 8 | Viewed by 2440
Abstract
For detecting malignant tumors, diffusion-weighted magnetic resonance imaging (DWI) as well as fluoro-2-deoxy-glucose positron emission tomography/computed tomography (FDG-PET/CT) are available. It is not definitive how DWI correlates the pathological findings of lung cancer. The aim of this study is to evaluate the relationships [...] Read more.
For detecting malignant tumors, diffusion-weighted magnetic resonance imaging (DWI) as well as fluoro-2-deoxy-glucose positron emission tomography/computed tomography (FDG-PET/CT) are available. It is not definitive how DWI correlates the pathological findings of lung cancer. The aim of this study is to evaluate the relationships between DWI findings and pathologic findings. In this study, 226 patients with resected lung cancers were enrolled. DWI was performed on each patient before surgery. There were 167 patients with adenocarcinoma, 44 patients with squamous cell carcinoma, and 15 patients with other cell types. Relationships between the apparent diffusion coefficient (ADC) of DWI and the pathology were analyzed. When the optimal cutoff value (OCV) of ADC for diagnosing malignancy was 1.70 × 10−3 mm2/s, the sensitivity of DWI was 92.0% (208/226). The sensitivity was 33.3% (3/9) in mucinous adenocarcinoma. The ADC value (1.31 ± 0.32 × 10−3 mm2/s) of adenocarcinoma was significantly higher than that (1.17 ± 0.29 × 10−3 mm2/s) of squamous cell carcinoma (p = 0.012), or (0.93 ± 0.14 × 10−3 mm2/s) of small cell carcinoma (p = 0.0095). The ADC value (1.91 ± 0.36 × 10−3 mm2/s) of mucinous adenocarcinoma was significantly higher than that (1.25 ± 0.25 × 10−3 mm2/s) of adenocarcinoma with mucin and that (1.24 ± 0.30 × 10−3 mm2/s) of other cell types. The ADC (1.11 ± 0.26 × 10−3 mm2/s) of lung cancer with necrosis was significantly lower than that (1.32 ± 0.33 × 10−3 mm2/s) of lung cancer without necrosis. The ADC of mucinous adenocarcinoma was significantly higher than those of adenocarcinoma of other cell types. The ADC of lung cancer was likely to decrease according to cell differentiation decreasing. The sensitivity of DWI for lung cancer was 92% and this result shows that DWI is valuable for the evaluation of lung cancer. Lung cancer could be evaluated qualitatively using DWI. Full article
(This article belongs to the Special Issue Cancer Molecular Imaging)
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Review

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26 pages, 3012 KiB  
Review
Quantifying PD-L1 Expression to Monitor Immune Checkpoint Therapy: Opportunities and Challenges
by Sridhar Nimmagadda
Cancers 2020, 12(11), 3173; https://doi.org/10.3390/cancers12113173 - 29 Oct 2020
Cited by 34 | Viewed by 3125
Abstract
Therapeutics targeting programmed death ligand 1 (PD-L1) protein and its receptor PD-1 are now dominant players in restoring anti-tumor immune responses. PD-L1 detection by immunohistochemistry (IHC) is emerging as a reproducible biomarker for guiding patient stratification for those therapies in some cancers. However, [...] Read more.
Therapeutics targeting programmed death ligand 1 (PD-L1) protein and its receptor PD-1 are now dominant players in restoring anti-tumor immune responses. PD-L1 detection by immunohistochemistry (IHC) is emerging as a reproducible biomarker for guiding patient stratification for those therapies in some cancers. However, PD-L1 expression in the tumor microenvironment is highly complex. It is upregulated by aberrant genetic alterations, and is highly regulated at the transcriptional, posttranscriptional, and protein levels. Thus, PD-L1 IHC is inadequate to fully understand the relevance of PD-L1 levels in the whole body and their dynamics to improve therapeutic outcomes. Imaging technologies could potentially assist in meeting that need. Early clinical investigations show promising results in quantifying PD-L1 expression in the whole body by positron emission tomography (PET). Within this context, this review summarizes advancements in regulation of PD-L1 expression and imaging agents, and in PD-L1 PET for drug development, and discusses opportunities and challenges presented by these innovations for guiding immune checkpoint therapy (ICT). Full article
(This article belongs to the Special Issue Cancer Molecular Imaging)
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16 pages, 1304 KiB  
Review
The Unique Pharmacometrics of Small Molecule Therapeutic Drug Tracer Imaging for Clinical Oncology
by Mark P. S. Dunphy and Nagavarakishore Pillarsetty
Cancers 2020, 12(9), 2712; https://doi.org/10.3390/cancers12092712 - 22 Sep 2020
Cited by 5 | Viewed by 2608
Abstract
Translational development of radiolabeled analogues or isotopologues of small molecule therapeutic drugs as clinical imaging biomarkers for optimizing patient outcomes in targeted cancer therapy aims to address an urgent and recurring clinical need in therapeutic cancer drug development: drug- and target-specific biomarker assays [...] Read more.
Translational development of radiolabeled analogues or isotopologues of small molecule therapeutic drugs as clinical imaging biomarkers for optimizing patient outcomes in targeted cancer therapy aims to address an urgent and recurring clinical need in therapeutic cancer drug development: drug- and target-specific biomarker assays that can optimize patient selection, dosing strategy, and response assessment. Imaging the in vivo tumor pharmacokinetics and biomolecular pharmacodynamics of small molecule cancer drugs offers patient- and tumor-specific data which are not available from other pharmacometric modalities. This review article examines clinical research with a growing pharmacopoeia of investigational small molecule cancer drug tracers. Full article
(This article belongs to the Special Issue Cancer Molecular Imaging)
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16 pages, 5239 KiB  
Review
Development of [18F]ICMT-11 for Imaging Caspase-3/7 Activity during Therapy-Induced Apoptosis
by Segundo Francisco García-Argüello, Beatriz Lopez-Lorenzo, Bart Cornelissen and Graham Smith
Cancers 2020, 12(8), 2191; https://doi.org/10.3390/cancers12082191 - 06 Aug 2020
Cited by 8 | Viewed by 2294
Abstract
Insufficient apoptosis is a recognised hallmark of cancer. A strategy to quantitatively measure apoptosis in vivo would be of immense value in both drug discovery and routine patient management. The first irreversible step in the apoptosis cascade is activation of the “executioner” caspase-3 [...] Read more.
Insufficient apoptosis is a recognised hallmark of cancer. A strategy to quantitatively measure apoptosis in vivo would be of immense value in both drug discovery and routine patient management. The first irreversible step in the apoptosis cascade is activation of the “executioner” caspase-3 enzyme to commence cleavage of key structural proteins. One strategy to measure caspase-3 activity is Positron Emission Tomography using isatin-5-sulfonamide radiotracers. One such radiotracer is [18F]ICMT-11, which has progressed to clinical application. This review summarises the design and development process for [18F]ICMT-11, suggesting potential avenues for further innovation. Full article
(This article belongs to the Special Issue Cancer Molecular Imaging)
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32 pages, 4449 KiB  
Review
PET Imaging Agents (FES, FFNP, and FDHT) for Estrogen, Androgen, and Progesterone Receptors to Improve Management of Breast and Prostate Cancers by Functional Imaging
by John A. Katzenellenbogen
Cancers 2020, 12(8), 2020; https://doi.org/10.3390/cancers12082020 - 23 Jul 2020
Cited by 19 | Viewed by 4127
Abstract
Many breast and prostate cancers are driven by the action of steroid hormones on their cognate receptors in primary tumors and in metastases, and endocrine therapies that inhibit hormone production or block the action of these receptors provide clinical benefit to many but [...] Read more.
Many breast and prostate cancers are driven by the action of steroid hormones on their cognate receptors in primary tumors and in metastases, and endocrine therapies that inhibit hormone production or block the action of these receptors provide clinical benefit to many but not all of these cancer patients. Because it is difficult to predict which individuals will be helped by endocrine therapies and which will not, positron emission tomography (PET) imaging of estrogen receptor (ER) and progesterone receptor (PgR) in breast cancer, and androgen receptor (AR) in prostate cancer can provide useful, often functional, information on the likelihood of endocrine therapy response in individual patients. This review covers our development of three PET imaging agents, 16α-[18F]fluoroestradiol (FES) for ER, 21-[18F]fluoro-furanyl-nor-progesterone (FFNP) for PgR, and 16β-[18F]fluoro-5α-dihydrotestosterone (FDHT) for AR, and the evolution of their clinical use. For these agents, the pathway from concept through development tracks with an emerging understanding of critical performance criteria that is needed for successful PET imaging of these low-abundance receptor targets. Progress in the ongoing evaluation of what they can add to the clinical management of breast and prostate cancers reflects our increased understanding of these diseases and of optimal strategies for predicting the success of clinical endocrine therapies. Full article
(This article belongs to the Special Issue Cancer Molecular Imaging)
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13 pages, 1352 KiB  
Review
The Biological Function of Sigma-2 Receptor/TMEM97 and Its Utility in PET Imaging Studies in Cancer
by Chenbo Zeng, Aladdin Riad and Robert H. Mach
Cancers 2020, 12(7), 1877; https://doi.org/10.3390/cancers12071877 - 13 Jul 2020
Cited by 31 | Viewed by 4416
Abstract
The sigma-2 receptor was originally defined pharmacologically and recently identified as TMEM97. TMEM97 has been validated as a biomarker of proliferative status and the radioligand of TMEM97, [18F]ISO-1, has been developed and validated as a PET imaging biomarker of proliferative status [...] Read more.
The sigma-2 receptor was originally defined pharmacologically and recently identified as TMEM97. TMEM97 has been validated as a biomarker of proliferative status and the radioligand of TMEM97, [18F]ISO-1, has been developed and validated as a PET imaging biomarker of proliferative status of tumors and as a predictor of the cancer therapy response. [18F]ISO-1 PET imaging should be useful to guide treatment for cancer patients. TMEM97 is a membrane-bound protein and localizes in multiple subcellular organelles including endoplasmic reticulum and lysosomes. TMEM97 plays distinct roles in cancer. It is reported that TMEM97 is upregulated in some tumors but downregulated in other tumors and it is required for cell proliferation in certain tumor cells. TMEM97 plays important roles in cholesterol homeostasis. TMEM97 expression is regulated by cholesterol-regulating signals such as sterol depletion and SREBP expression levels. TMEM97 regulates cholesterol trafficking processes such as low density lipoprotein (LDL) uptake by forming complexes with PGRMC1 and low density lipoprotein receptor (LDLR), as well as cholesterol transport out of lysosome by interacting with and regulating NPC1 protein. Understanding molecular functions of TMEM97 in proliferation and cholesterol metabolism will be important to develop strategies to diagnose and treat cancer and cholesterol disorders using a rich collection of TMEM97 radiotracers and ligands. Full article
(This article belongs to the Special Issue Cancer Molecular Imaging)
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20 pages, 2655 KiB  
Review
Development of Folate Receptor−Targeted PET Radiopharmaceuticals for Tumor Imaging—A Bench-to-Bedside Journey
by Silvan D. Boss and Simon Mensah Ametamey
Cancers 2020, 12(6), 1508; https://doi.org/10.3390/cancers12061508 - 09 Jun 2020
Cited by 27 | Viewed by 3999
Abstract
The folate receptor-α (FR-α) is overexpressed in many epithelial cancers, including ovary, uterus, kidneys, breast, lung, colon and prostate carcinomas, but shows limited expression in normal tissues such as kidneys, salivary glands, choroid plexus and placenta. FR-α has therefore emerged as a promising [...] Read more.
The folate receptor-α (FR-α) is overexpressed in many epithelial cancers, including ovary, uterus, kidneys, breast, lung, colon and prostate carcinomas, but shows limited expression in normal tissues such as kidneys, salivary glands, choroid plexus and placenta. FR-α has therefore emerged as a promising target for the delivery of therapeutic and imaging agents to FR-positive tumors. A series of folate-based PET (positron emission tomography) radiopharmaceuticals have been developed for the selective targeting of FR-positive malignancies. This review provides an overview on the research progress made so far regarding the design, radiosynthesis and the utility of the folate-derived PET radioconjugates for targeting FR-positive tumors. For the most part, results from folate radioconjugates labeled with fluorine-18 (t1/2 = 109.8 min) and gallium-68 (t1/2 = 67.7 min) have been presented but folates labeled with “exotic” and new PET radionuclides such as copper-64 (t1/2 = 12.7 h), terbium-152 (t1/2 = 17.5 h), scandium-44 (t1/2 = 3.97 h), cobalt-55 (t1/2 = 17.5 h) and zirconium-89 (t1/2 = 78.4 h) are also discussed. For tumor imaging, none of the reported PET radiolabeled folates reported to date has made the complete bench-to-bedside journey except [18F]AzaFol, which made it to patients with metastatic ovarian and lung cancers in a multicenter first-in-human trial. In the near future, however, we expect more clinical trials with folate-based PET radiopharmaceuticals given the increasing clinical interest in imaging and the treatment of FR-related malignancies. Full article
(This article belongs to the Special Issue Cancer Molecular Imaging)
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16 pages, 3391 KiB  
Review
Hypoxia PET Imaging with [18F]-HX4—A Promising Next-Generation Tracer
by Sebastian Sanduleanu, Alexander M.A. van der Wiel, Relinde I.Y. Lieverse, Damiënne Marcus, Abdalla Ibrahim, Sergey Primakov, Guangyao Wu, Jan Theys, Ala Yaromina, Ludwig J. Dubois and Philippe Lambin
Cancers 2020, 12(5), 1322; https://doi.org/10.3390/cancers12051322 - 22 May 2020
Cited by 31 | Viewed by 4239
Abstract
Hypoxia—a common feature of the majority of solid tumors—is a negative prognostic factor, as it is associated with invasion, metastasis and therapy resistance. To date, a variety of methods are available for the assessment of tumor hypoxia, including the use of positron emission [...] Read more.
Hypoxia—a common feature of the majority of solid tumors—is a negative prognostic factor, as it is associated with invasion, metastasis and therapy resistance. To date, a variety of methods are available for the assessment of tumor hypoxia, including the use of positron emission tomography (PET). A plethora of hypoxia PET tracers, each with its own strengths and limitations, has been developed and successfully validated, thereby providing useful prognostic or predictive information. The current review focusses on [18F]-HX4, a promising next-generation hypoxia PET tracer. After a brief history of its development, we discuss and compare its characteristics with other hypoxia PET tracers and provide an update on its progression into the clinic. Lastly, we address the potential applications of assessing tumor hypoxia using [18F]-HX4, with a focus on improving patient-tailored therapies. Full article
(This article belongs to the Special Issue Cancer Molecular Imaging)
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34 pages, 4755 KiB  
Review
Insight into the Development of PET Radiopharmaceuticals for Oncology
by Joseph Lau, Etienne Rousseau, Daniel Kwon, Kuo-Shyan Lin, François Bénard and Xiaoyuan Chen
Cancers 2020, 12(5), 1312; https://doi.org/10.3390/cancers12051312 - 21 May 2020
Cited by 47 | Viewed by 6775
Abstract
While the development of positron emission tomography (PET) radiopharmaceuticals closely follows that of traditional drug development, there are several key considerations in the chemical and radiochemical synthesis, preclinical assessment, and clinical translation of PET radiotracers. As such, we outline the fundamentals of radiotracer [...] Read more.
While the development of positron emission tomography (PET) radiopharmaceuticals closely follows that of traditional drug development, there are several key considerations in the chemical and radiochemical synthesis, preclinical assessment, and clinical translation of PET radiotracers. As such, we outline the fundamentals of radiotracer design, with respect to the selection of an appropriate pharmacophore. These concepts will be reinforced by exemplary cases of PET radiotracer development, both with respect to their preclinical and clinical evaluation. We also provide a guideline for the proper selection of a radionuclide and the appropriate labeling strategy to access a tracer with optimal imaging qualities. Finally, we summarize the methodology of their evaluation in in vitro and animal models and the road to clinical translation. This review is intended to be a primer for newcomers to the field and give insight into the workflow of developing radiopharmaceuticals. Full article
(This article belongs to the Special Issue Cancer Molecular Imaging)
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18 pages, 2284 KiB  
Review
[18F]FET-βAG-TOCA: The Design, Evaluation and Clinical Translation of a Fluorinated Octreotide
by Louis Allott, Suraiya Dubash and Eric O. Aboagye
Cancers 2020, 12(4), 865; https://doi.org/10.3390/cancers12040865 - 02 Apr 2020
Cited by 14 | Viewed by 3618
Abstract
The success of Lutathera™ ([177Lu]Lu-DOTA-TATE) in the NETTER-1 clinical trial as a peptide receptor radionuclide therapy (PRRT) for somatostatin receptor expressing (SSTR) neuroendocrine tumours (NET) is likely to increase the demand for patient stratification by positron emission tomography (PET). The current [...] Read more.
The success of Lutathera™ ([177Lu]Lu-DOTA-TATE) in the NETTER-1 clinical trial as a peptide receptor radionuclide therapy (PRRT) for somatostatin receptor expressing (SSTR) neuroendocrine tumours (NET) is likely to increase the demand for patient stratification by positron emission tomography (PET). The current gold standard of gallium-68 radiolabelled somatostatin analogues (e.g., [68Ga]Ga-DOTA-TATE) works effectively, but access is constrained by the limited availability and scalability of gallium-68 radiopharmaceutical production. The aim of this review is three-fold: firstly, we discuss the peptide library design, biological evaluation and clinical translation of [18F]fluoroethyltriazole-βAG-TOCA ([18F]FET-βAG-TOCA), our fluorine-18 radiolabelled octreotide; secondly, to exemplify the potential of the 2-[18F]fluoroethylazide prosthetic group and copper-catalysed azide-alkyne cycloaddition (CuAAC) chemistry in accessing good manufacturing practice (GMP) compatible radiopharmaceuticals; thirdly, we aim to illustrate a framework for the translation of similarly radiolabelled peptides, in which in vivo pharmacokinetics drives candidate selection, supported by robust radiochemistry methodology and a route to GMP production. It is hoped that this review will continue to inspire the development and translation of fluorine-18 radiolabelled peptides into clinical studies for the benefit of patients. Full article
(This article belongs to the Special Issue Cancer Molecular Imaging)
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12 pages, 517 KiB  
Review
Metastatic Heterogeneity of Breast Cancer: Companion and Theranostic Approach in Nuclear Medicine
by Christopher Montemagno and Gilles Pagès
Cancers 2020, 12(4), 821; https://doi.org/10.3390/cancers12040821 - 29 Mar 2020
Cited by 9 | Viewed by 4691
Abstract
Breast cancer is the most common malignancy in women throughout the world. Metastatic dissemination to vital organs is the leading cause of breast cancer-related deaths. The treatment of metastases is mainly based on the primary tumor characteristics. However, breast cancer metastases exhibit high [...] Read more.
Breast cancer is the most common malignancy in women throughout the world. Metastatic dissemination to vital organs is the leading cause of breast cancer-related deaths. The treatment of metastases is mainly based on the primary tumor characteristics. However, breast cancer metastases exhibit high heterogeneity leading to different prognosis and therapeutic responses. Getting access to phenotype of metastases would allow better management of patients. The advent of theranostics in nuclear medicine has opened new opportunities for the diagnosis and treatment of cancer patients. The aim of this review is to provide an overview of current knowledge and future directions in nuclear medicine for therapeutic management of metastatic breast cancer patients. Full article
(This article belongs to the Special Issue Cancer Molecular Imaging)
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21 pages, 4412 KiB  
Review
Affibody Molecules as Targeting Vectors for PET Imaging
by Vladimir Tolmachev and Anna Orlova
Cancers 2020, 12(3), 651; https://doi.org/10.3390/cancers12030651 - 11 Mar 2020
Cited by 57 | Viewed by 6865
Abstract
Affibody molecules are small (58 amino acids) engineered scaffold proteins that can be selected to bind to a large variety of proteins with a high affinity. Their small size and high affinity make them attractive as targeting vectors for molecular imaging. High-affinity affibody [...] Read more.
Affibody molecules are small (58 amino acids) engineered scaffold proteins that can be selected to bind to a large variety of proteins with a high affinity. Their small size and high affinity make them attractive as targeting vectors for molecular imaging. High-affinity affibody binders have been selected for several cancer-associated molecular targets. Preclinical studies have shown that radiolabeled affibody molecules can provide highly specific and sensitive imaging on the day of injection; however, for a few targets, imaging on the next day further increased the imaging sensitivity. A phase I/II clinical trial showed that 68Ga-labeled affibody molecules permit an accurate and specific measurement of HER2 expression in breast cancer metastases. This paper provides an overview of the factors influencing the biodistribution and targeting properties of affibody molecules and the chemistry of their labeling using positron emitters. Full article
(This article belongs to the Special Issue Cancer Molecular Imaging)
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