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Radiopharmaceuticals for PET Imaging 2021
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Radiopharmaceuticals for PET Imaging 2021

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 December 2021) | Viewed by 11235

Special Issue Editors

Dr. Aline Nonat

E-Mail Website
Guest Editor
Equipe de Synthèse pour l’Analyse (SynPA), Institut Pluridisciplinaire Hubert Curien, Université de Strasbourg, Strasbourg, France
Interests: chelator synthesis; bispidine; coordination chemistry; PET imaging; MRI; luminescent complexes; bimodal probes; theranostic agents; upconversion
Dr. Ali Ouadi

E-Mail Website
Guest Editor
Groupe Imagerie Moléculaire, Institut Pluridisciplinaire Hubert Curien, Université de Strasbourg, Strasbourg, France
Interests: radioelement production and purification; design and synthesis of novel ligands for SPECT and PET imaging; radiolabeling; antibodies; peptides; Tc-99m; I-123; F-18; Zr-89; Cu-64; Ga-68; Ra-223; Ac-225; radiochemistry; task-specific ionic liquid synthesis

Special Issue Information

Dear Colleagues,

Today, hospitals, pharmaceuticals companies and the entire healthcare industry are turning toward personalized medicine and earlier diagnostics. Positron emission tomography (PET) plays a vital role in achieving these ambitions. PET is able to provide researchers and clinicians with quantitative visual images of organ function; it can also detect disease-related biochemical changes in the tissues before the apparition of structural changes occurs. As a consequence, research around the development and evaluation of radiopharmaceuticals is exploding in recent years (more than 200 articles per year since 2018).

Following the success of the first issue on “Radiopharmaceuticals for PET Imaging” and the strong research activity in the field, we propose here a second issue gathering very recent advances on radiopharmaceuticals design, starting with the production of innovative radioisotopes for diagnosis or therapy. New synthetic strategies are also being developed, including radiosynthesis, the development of new chelators and nanoparticles for PET imaging, as well as new conjugation strategies. Recent trends in biotargeting also contribute to the success of PET imaging. Emphasis of this issue will also be placed on multimodal probes, and theranostic agents and their preclinical and clinical applications, including neuroimaging, will also be encouraged.

You are cordially invited to contribute to this Special Issue on “Radiopharmaceuticals for PET Imaging II” with original articles, perspective papers, and short communications to highlight and review current developments in this field.

Dr. Aline Nonat
Dr. Ali Ouadi
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. Molecules 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 2700 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

  • Innovations in radioisotope production
  • Recent advances in radiosynthesis
  • New chelators and their evaluation as PET imaging agents
  • Nanoparticles for PET imaging
  • Novel conjugation strategies for bio-targeting
  • Recent trends in biotargeting
  • Multimodal probes
  • Theranostic agents
  • Neuroimaging

Published Papers (4 papers)

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Research

14 pages, 1611 KiB  
Article
Automated Synthesis of 68Ga-Labeled DOTA-MGS8 and Preclinical Characterization of Cholecystokinin-2 Receptor Targeting
by Anton Amadeus Hörmann, Elisabeth Plhak, Maximilian Klingler, Christine Rangger, Joachim Pfister, Gert Schwach, Herbert Kvaternik and Elisabeth von Guggenberg
Molecules 2022, 27(6), 2034; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27062034 - 21 Mar 2022
Cited by 4 | Viewed by 2570
Abstract
The new minigastrin analog DOTA-MGS8 targeting the cholecystokinin-2 receptor (CCK2R) used in this study displays the combination of two site-specific modifications within the C-terminal receptor binding sequence together with an additional N-terminal amino acid substitution preventing fast metabolic degradation. Within this study, the [...] Read more.
The new minigastrin analog DOTA-MGS8 targeting the cholecystokinin-2 receptor (CCK2R) used in this study displays the combination of two site-specific modifications within the C-terminal receptor binding sequence together with an additional N-terminal amino acid substitution preventing fast metabolic degradation. Within this study, the preparation of 68Ga-labeled DOTA-MGS8 was validated using an automated synthesis module, describing the specifications and analytical methods for quality control for possible clinical use. In addition, preclinical studies were carried out to characterize the targeting potential. [68Ga]Ga-DOTA-MGS8 showed a high receptor-specific cell internalization into AR42J rat pancreatic cells (~40%) with physiological expression of rat CCK2R as well as A431-CCK2R cells transfected to stably express human CCK2R (~47%). A favorable biodistribution profile was observed in BALB/c nude mice xenografted with A431-CCK2R cells and mock-transfected A431 cells as control. The high tumor uptake of ~27% IA/g together with low background activity and limited uptake in non-target tissue confirms the potential for high-sensitivity positron emission tomography of stabilized MG analogs in patients with MTC and other CCK2R-related malignancies. Full article
(This article belongs to the Special Issue Radiopharmaceuticals for PET Imaging 2021)
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12 pages, 1308 KiB  
Article
New Fully Automated Preparation of High Apparent Molar Activity 68Ga-FAPI-46 on a Trasis AiO Platform
by Chiara Da Pieve, Marta Costa Braga, David R. Turton, Frank A. Valla, Pinar Cakmak, Karl-Heinz Plate and Gabriela Kramer-Marek
Molecules 2022, 27(3), 675; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27030675 - 20 Jan 2022
Cited by 8 | Viewed by 2962
Abstract
A large number of applications for fibroblast activation protein inhibitors (FAPI)-based PET agents have been evaluated in conditions ranging from cancer to non-malignant diseases such as myocardial infarction. In particular, 68Ga-FAPI-46 was reported to have a high specificity and affinity for FAP-expressing [...] Read more.
A large number of applications for fibroblast activation protein inhibitors (FAPI)-based PET agents have been evaluated in conditions ranging from cancer to non-malignant diseases such as myocardial infarction. In particular, 68Ga-FAPI-46 was reported to have a high specificity and affinity for FAP-expressing cells, a fast and high accumulation in tumor lesions/injuries together with a fast body clearance when investigated in vivo. Due to the increasing interest in the use of the agent both preclinically and clinically, we developed an automated synthesis for the production of 68Ga-FAPI-46 on a Trasis AiO platform. The new synthetic procedure, which included the processing of the generator eluate using a strong cation exchange resin and a final purification step through an HLB followed by a QMA cartridge, yielded 68Ga-FAPI-46 with high radiochemical purity (>98%) and apparent molar activity (271.1 ± 105.6 MBq/nmol). Additionally, the in vitro and in vivo properties of the product were assessed on glioblastoma cells and mouse model. Although developed for the preparation of 68Ga-FAPI-46 for preclinical use, our method can be adapted for clinical production as a reliable alternative to the manual (i.e., cold kit) or modular systems preparations already described in the literature. Full article
(This article belongs to the Special Issue Radiopharmaceuticals for PET Imaging 2021)
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22 pages, 5917 KiB  
Article
Separation of 44Sc from 44Ti in the Context of A Generator System for Radiopharmaceutical Purposes with the Example of [44Sc]Sc-PSMA-617 and [44Sc]Sc-PSMA-I&T Synthesis
by Anton A. Larenkov, Artur G. Makichyan and Vladimir N. Iatsenko
Molecules 2021, 26(21), 6371; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26216371 - 21 Oct 2021
Cited by 10 | Viewed by 2219
Abstract
Today, 44Sc is an attractive radionuclide for molecular imaging with PET. In this work, we evaluated a 44Ti/44Sc radionuclide generator based on TEVA resin as a source of 44Sc. The generator prototype (5 MBq) exhibits high 44Ti [...] Read more.
Today, 44Sc is an attractive radionuclide for molecular imaging with PET. In this work, we evaluated a 44Ti/44Sc radionuclide generator based on TEVA resin as a source of 44Sc. The generator prototype (5 MBq) exhibits high 44Ti retention and stable yield of 44Sc (91 ± 6 %) in 1 mL of eluate (20 bed volumes, eluent—0.1 M oxalic acid/0.2 M HCl) during one year of monitoring (more than 120 elutions). The breakthrough of 44Ti did not exceed 1.5 × 10−5% (average value was 6.5 × 10−6%). Post-processing of the eluate for further use in radiopharmaceutical synthesis was proposed. The post-processing procedure using a combination of Presep® PolyChelate and TK221 resins made it possible to obtain 44Sc-radioconjugates with high labeling yield (≥95%) while using small precursor amounts (5 nmol). The proposed method takes no more than 15 min and provides ≥90% yield relative to the 44Sc activity eluted from the generator. The labeling efficiency was demonstrated on the example of [44Sc]Sc-PSMA-617 and [44Sc]Sc-PSMA-I&T synthesis. Some superiority of PSMA-I&T over PSMA-617 in terms of 44Sc labeling efficiency was demonstrated (likely due to presence of DOTAGA chelator in the precursor structure). It was also shown that microwave heating of the reaction mixture considerably shortened the reaction time and improved radiolabeling yield and reproducibility of [44Sc]Sc-PSMA-617 and [44Sc]Sc-PSMA-I&T synthesis. Full article
(This article belongs to the Special Issue Radiopharmaceuticals for PET Imaging 2021)
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18 pages, 3585 KiB  
Article
Hybrid Chelator-Based PSMA Radiopharmaceuticals: Translational Approach
by Hanane Lahnif, Tilmann Grus, Stefanie Pektor, Lukas Greifenstein, Mathias Schreckenberger and Frank Rösch
Molecules 2021, 26(21), 6332; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26216332 - 20 Oct 2021
Cited by 4 | Viewed by 2364
Abstract
(1) Background: Prostate-specific membrane antigen (PSMA) has been extensively studied in the last decade. It became a promising biological target in the diagnosis and therapy of PSMA-expressing cancer diseases. Although there are several radiolabeled PSMA inhibitors available, the search for new compounds with [...] Read more.
(1) Background: Prostate-specific membrane antigen (PSMA) has been extensively studied in the last decade. It became a promising biological target in the diagnosis and therapy of PSMA-expressing cancer diseases. Although there are several radiolabeled PSMA inhibitors available, the search for new compounds with improved pharmacokinetic properties and simplified synthesis is still ongoing. In this study, we developed PSMA ligands with two different hybrid chelators and a modified linker. Both compounds have displayed a promising pharmacokinetic profile. (2) Methods: DATA5m.SA.KuE and AAZTA5.SA.KuE were synthesized. DATA5m.SA.KuE was labeled with gallium-68 and radiochemical yields of various amounts of precursor at different temperatures were determined. Complex stability in phosphate-buffered saline (PBS) and human serum (HS) was examined at 37 °C. Binding affinity and internalization ratio were determined in in vitro assays using PSMA-positive LNCaP cells. Tumor accumulation and biodistribution were evaluated in vivo and ex vivo using an LNCaP Balb/c nude mouse model. All experiments were conducted with PSMA-11 as reference. (3) Results: DATA5m.SA.KuE was synthesized successfully. AAZTA5.SA.KuE was synthesized and labeled according to the literature. Radiolabeling of DATA5m.SA.KuE with gallium-68 was performed in ammonium acetate buffer (1 M, pH 5.5). High radiochemical yields (>98%) were obtained with 5 nmol at 70 °C, 15 nmol at 50 °C, and 60 nmol (50 µg) at room temperature. [68Ga]Ga-DATA5m.SA.KuE was stable in human serum as well as in PBS after 120 min. PSMA binding affinities of AAZTA5.SA.KuE and DATA5m.SA.KuE were in the nanomolar range. PSMA-specific internalization ratio was comparable to PSMA-11. In vivo and ex vivo studies of [177Lu]Lu-AAZTA5.SA.KuE, [44Sc]Sc-AAZTA5.SA.KuE and [68Ga]Ga-DATA5m.SA.KuE displayed specific accumulation in the tumor along with fast clearance and reduced off-target uptake. (4) Conclusions: Both KuE-conjugates showed promising properties especially in vivo allowing for translational theranostic use. Full article
(This article belongs to the Special Issue Radiopharmaceuticals for PET Imaging 2021)
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