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Novel PET Radiopharmaceuticals: Molecular Probes for Personalized Imaging 2.0
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Novel PET Radiopharmaceuticals: Molecular Probes for Personalized Imaging 2.0

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: 30 July 2024 | Viewed by 2058

Special Issue Editor

Dr. Ferdinando F. Calabria

E-Mail Website
Guest Editor
Department of Nuclear Medicine and Theragnostics, “Mariano Santo” Hospital, 87100 Cosenza, Italy
Interests: hybrid imaging; PET/CT; PET/MRI; prostate cancer; brain tumors; molecular imaging; infectious diseases
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We are glad to share with you that Volume I of this Special Issue (https://www.mdpi.com/journal/ijms/special_issues/molecular_probes) was a success, so we reopened this Special Issue as “Novel PET Radiopharmaceuticals: Molecular Probes for Personalized Imaging 2.0”:

The emerging role of novel radiopharmaceuticals for PET imaging allows for the opportunity to investigate and depict many diseases, enlarge the fields of application of PET/CT and PET/MRI from oncology to infectious diseases and neuro-oncology, and to evaluate neurodegenerative diseases.

For this reason, the accurate knowledge of the synthesis, availability, and in vivo biodistribution of these novel molecular probes is of utmost importance for physicians and professionals.

Beyond scientific papers focused on specific clinical settings, an accurate collection of PET tracers in a single volume is still missing; it is necessary to cover all aspects of these tracers in order to assess their biochemical peculiarities, diagnostic overlapping, and efficacy.

For these reasons, a monography with several chapters on the peculiar aspects of these molecular probes is needed.

Suitable topics include, but are not limited to, the synthesis, kinetics, biodistribution of PET radiopharmaceuticals, and their current applications.

Dr. Ferdinando F. Calabria
Guest Editor

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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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

  • synthesis
  • kinetics
  • biodistribution
  • PET
  • radiopharmaceuticals
  • molecular probes
  • PET/CT
  • PET/MRI
  • hybrid imaging
  • molecular imaging

Published Papers (2 papers)

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18 pages, 10425 KiB  
Article
Evaluation of Chelator-to-Antibody Ratio on Development of 89Zr-iPET Tracer for Imaging of PD-L1 Expression on Tumor
by Shih-Chuan Tsai, Shiou-Shiow Farn, Wei-Lin Lo, Fang-Yu Ou Yang, Yong-Ching Kang, Liang-Cheng Chen, Kuo-Ting Chen, Jiunn-Wang Liao, Jui-Yin Kung, Jenn-Tzong Chen and Feng-Yun J. Huang
Int. J. Mol. Sci. 2023, 24(24), 17132; https://doi.org/10.3390/ijms242417132 - 5 Dec 2023
Cited by 1 | Viewed by 1006
Abstract
89Zr-iPET has been widely used for preclinical and clinical immunotherapy studies to predict patient stratification or evaluate therapeutic efficacy. In this study, we prepared and evaluated 89Zr-DFO-anti-PD-L1-mAb tracers with varying chelator-to-antibody ratios (CARs), including 89Zr-DFO-anti-PD-L1-mAb_3X (tracer_3X), 89Zr-DFO-anti-PD-L1-mAb_10X [...] Read more.
89Zr-iPET has been widely used for preclinical and clinical immunotherapy studies to predict patient stratification or evaluate therapeutic efficacy. In this study, we prepared and evaluated 89Zr-DFO-anti-PD-L1-mAb tracers with varying chelator-to-antibody ratios (CARs), including 89Zr-DFO-anti-PD-L1-mAb_3X (tracer_3X), 89Zr-DFO-anti-PD-L1-mAb_10X (tracer_10X), and 89Zr-DFO-anti-PD-L1-mAb_20X (tracer_20X). The DFO-anti-PD-L1-mAb conjugates with varying CARs were prepared using a random conjugation method and then subjected to quality control. The conjugates were radiolabeled with 89Zr and evaluated in a PD-L1-expressing CT26 tumor-bearing mouse model. Next, iPET imaging, biodistribution, pharmacokinetics, and ex vivo pathological and immunohistochemical examinations were conducted. LC–MS analysis revealed that DFO-anti-PD-L1-mAb conjugates were prepared with CARs ranging from 0.4 to 2.0. Radiochemical purity for all tracer groups was >99% after purification. The specific activity levels of tracer_3X, tracer_10X, and tracer_20X were 2.2 ± 0.6, 8.2 ± 0.6, and 10.5 ± 1.6 μCi/μg, respectively. 89Zr-iPET imaging showed evident tumor uptake in all tracer groups and reached the maximum uptake value at 24 h postinjection (p.i.). Biodistribution data at 168 h p.i. revealed that the tumor-to-liver, tumor-to-muscle, and tumor-to-blood uptake ratios for tracer_3X, tracer_10X, and tracer_20X were 0.46 ± 0.14, 0.58 ± 0.33, and 1.54 ± 0.51; 4.7 ± 1.3, 7.1 ± 3.9, and 14.7 ± 1.1; and 13.1 ± 5.8, 19.4 ± 13.8, and 41.3 ± 10.6, respectively. Significant differences were observed between tracer_3X and tracer_20X in the aforementioned uptake ratios at 168 h p.i. The mean residence time and elimination half-life for tracer_3X, tracer_10X, and tracer_20X were 25.4 ± 4.9, 24.2 ± 6.1, and 25.8 ± 3.3 h and 11.8 ± 0.5, 11.1 ± 0.7, and 11.7 ± 0.6 h, respectively. No statistical differences were found between-tracer in the aforementioned pharmacokinetic parameters. In conclusion, 89Zr-DFO-anti-PD-L1-mAb tracers with a CAR of 1.4–2.0 may be better at imaging PD-L1 expression in tumors than are traditional low-CAR 89Zr-iPET tracers. Full article
(This article belongs to the Special Issue Novel PET Radiopharmaceuticals: Molecular Probes for Personalized Imaging 2.0)
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22 pages, 2321 KiB  
Article
Preparation of NIn-Methyl-6-[18F]fluoro- and 5-Hydroxy-7-[18F]fluorotryptophans as Candidate PET-Tracers for Pathway-Specific Visualization of Tryptophan Metabolism
by Niklas Kolks, Felix Neumaier, Bernd Neumaier and Boris D. Zlatopolskiy
Int. J. Mol. Sci. 2023, 24(20), 15251; https://doi.org/10.3390/ijms242015251 - 17 Oct 2023
Viewed by 820
Abstract
Tryptophan (Trp) is an essential proteinogenic amino acid and metabolic precursor for several signaling molecules that has been implicated in many physiological and pathological processes. Since the two main branches of Trp metabolism—serotonin biosynthesis and kynurenine pathway—are differently affected by a variety of [...] Read more.
Tryptophan (Trp) is an essential proteinogenic amino acid and metabolic precursor for several signaling molecules that has been implicated in many physiological and pathological processes. Since the two main branches of Trp metabolism—serotonin biosynthesis and kynurenine pathway—are differently affected by a variety of neurological and neoplastic diseases, selective visualization of these pathways is of high clinical relevance. However, while positron emission tomography (PET) with existing probes can be used for non-invasive assessment of total Trp metabolism, optimal imaging agents for pathway-specific PET imaging are still lacking. In this work, we describe the preparation of two 18F-labeled Trp derivatives, NIn-methyl-6-[18F]fluorotryptophan (NIn-Me-6-[18F]FTrp) and 5-hydroxy-7-[18F]fluorotryptophan (5-HO-7-[18F]FTrp). We also report feasible synthetic routes for the preparation of the hitherto unknown boronate radiolabeling precursors and non-radioactive reference compounds. Under optimized conditions, alcohol-enhanced Cu-mediated radiofluorination of the respective precursors afforded NIn-Me-6-[18F]FTrp and 5-HO-7-[18F]FTrp as application-ready solutions in radiochemical yields of 45 ± 7% and 29 ± 4%, respectively. As such, our work provides access to two promising candidate probes for pathway-specific visualization of Trp metabolism in amounts sufficient for their preclinical evaluation. Full article
(This article belongs to the Special Issue Novel PET Radiopharmaceuticals: Molecular Probes for Personalized Imaging 2.0)
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