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Molecular Probe: Recent Research and Future Challenges

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

Deadline for manuscript submissions: 15 June 2024 | Viewed by 5371

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Special Issue Editor

Dr. Beatriz Salinas Rodríguez

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Guest Editor

1. Unidad de Medicina y Cirugía Experimental, Instituto de Investigación Sanitaria Gregorio Marañón, 28007 Madrid, Spain
2. Departamento de Bioingeniería, Universidad Carlos III de Madrid, 28911 Leganés, Spain
Interests: molecular probes; biomedical imaging; nanomedicine; radiotracers; infectious diseases; cancer; extracellular vesicles; contrast agent

Special Issue Information

Dear Colleagues,

The design and application of new molecular probes is essential for the development of a more specific and selective diagnosis by molecular imaging. The development of new chemical strategies for the labeling of (bio)molecules with radioactive isotopes, the generation of new molecules with optical properties, and the advance of nanotechnology in the creation of new nanoparticles with beneficial physical properties for different imaging techniques have opened a new avenue in the development of non-invasive tools capable of early and specific detection of pathologies as diverse as cancer, neurodegenerative, cardiovascular, and infectious diseases.

In the Special Issue "Molecular Probe: Recent Research and Future Challenges", we welcome your contributions in the form of original research and review articles on all aspects of molecular probes and their biological application through biomedical imaging, as well as articles examining novel chemical methodologies in radioactive or optical labeling, as well as the synthesis of nanoparticles with fluorescent, magnetic or radioactive properties.

Dr. Beatriz Salinas Rodríguez
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

molecular imaging
radiotracer
probes
nanoparticles
diagnosis

Published Papers (4 papers)

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Research

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24 pages, 8102 KiB

Open AccessArticle

Preclinical Evaluation of a Novel High-Affinity Radioligand [^99mTc]Tc-BQ0413 Targeting Prostate-Specific Membrane Antigen (PSMA)

by Ekaterina Bezverkhniaia, Panagiotis Kanellopoulos, Ayman Abouzayed, Mariia Larkina, Maryam Oroujeni, Anzhelika Vorobyeva, Ulrika Rosenström, Vladimir Tolmachev and Anna Orlova

Int. J. Mol. Sci. 2023, 24(24), 17391; https://doi.org/10.3390/ijms242417391 - 12 Dec 2023

Cited by 1 | Viewed by 1454

Abstract

Radionuclide imaging using radiolabeled inhibitors of prostate-specific membrane antigen (PSMA) can be used for the staging of prostate cancer. Previously, we optimized the Glu-urea-Lys binding moiety using a linker structure containing 2-napththyl-L-alanine and L-tyrosine. We have now designed a molecule that contains mercaptoacetyl–triglutamate chelator for labeling with Tc-99m (designated as BQ0413). The purpose of this study was to evaluate the imaging properties of [^99mTc]Tc-BQ0413. PSMA-transfected PC3-pip cells were used to evaluate the specificity and affinity of [^99mTc]Tc-BQ0413 binding in vitro. PC3-pip tumor-bearing BALB/C nu/nu mice were used as an in vivo model. [^99mTc]Tc-BQ0413 bound specifically to PC3-pip cells with an affinity of 33 ± 15 pM. In tumor-bearing mice, the tumor uptake of [^99mTc]Tc-BQ0413 (38 ± 6 %IA/g in PC3-pip 3 h after the injection of 40 pmol) was dependent on PSMA expression (3 ± 2 %IA/g and 0.9 ± 0.3 %IA/g in PSMA-negative PC-3 and SKOV-3 tumors, respectively). We show that both unlabeled BQ0413 and the commonly used binder PSMA-11 enable the blocking of [^99mTc]Tc-BQ0413 uptake in normal PSMA-expressing tissues without blocking the uptake in tumors. This resulted in an appreciable increase in tumor-to-organ ratios. At the same injected mass (5 nmol), the use of BQ0413 was more efficient in suppressing renal uptake than the use of PSMA-11. In conclusion, [^99mTc]Tc-BQ0413 is a promising probe for the visualization of PSMA-positive lesions using single-photon emission computed tomography (SPECT). Full article

(This article belongs to the Special Issue Molecular Probe: Recent Research and Future Challenges)

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10 pages, 1380 KiB

Open AccessArticle

Fully Automated Production of [⁶⁸Ga]GaFAPI-46 with Gallium-68 from Cyclotron Using Liquid Targets

by Alexandra I. Fonseca, Vítor H. Alves, Ivanna Hrynchak, Francisco Alves and Antero J. Abrunhosa

Int. J. Mol. Sci. 2023, 24(20), 15101; https://doi.org/10.3390/ijms242015101 - 12 Oct 2023

Viewed by 894

Abstract

⁶⁸Ga-based radiopharmaceuticals are routinely used for PET imaging of multiple types of tumors. Gallium-68 is commonly obtained from ⁶⁸Ge/⁶⁸Ga generators, which are limited in the quantity of activity produced. Alternatively, gallium-68 can easily be produced on a cyclotron using liquid targets. In this study, we optimized the GMP production of [⁶⁸Ga]GaFAPI-46 using gallium-68 produced via a standard medical cyclotron using liquid targets. Starting from the published synthesis and quality control procedures described for other ⁶⁸Ga-based radiopharmaceuticals, we have validated the synthesis process and the analytical methods to test the quality parameters of the final product to be used for routine clinical studies. [⁶⁸Ga]GaFAPI-46 was successfully produced with high radiochemical purity and yield using an IBA Synthera^® Extension module. Gallium chloride was produced on a medical cyclotron using a liquid target with activity of 4.31 ± 0.36 GBq at the end of purification (EOP). Analytical methods were established and validated, meeting Ph. Eur. standards. Full GMP production was also validated in three consecutive batches, producing 2.50 ± 0.46 GBq of [⁶⁸Ga]GaFAPI-46 at the end of synthesis (EOS), with 98.94 ± 0.72% radiochemical purity measured via radio-HPLC. Quality was maintained for up to 3 h after the EOS. Production of [⁶⁸Ga]GaFAPI-46 was performed and validated using a standard medical cyclotron with liquid targets. The quality control parameters (e.g., sterility, purity, and residual solvents) conformed to Ph. Eur. and a shelf life of 3 h was established. The activity of [⁶⁸Ga]GaFAPI-46 produced was substantially higher than the one obtained with generators, enabling a better response to the clinical need for this radiopharmaceutical. Full article

(This article belongs to the Special Issue Molecular Probe: Recent Research and Future Challenges)

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Review

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37 pages, 6614 KiB

Open AccessReview

Hyperpolarized Xenon-129 Chemical Exchange Saturation Transfer (HyperCEST) Molecular Imaging: Achievements and Future Challenges

by Viktoriia Batarchuk, Yurii Shepelytskyi, Vira Grynko, Antal Halen Kovacs, Aaron Hodgson, Karla Rodriguez, Ruba Aldossary, Tanu Talwar, Carson Hasselbrink, Iulian C. Ruset, Brenton DeBoef and Mitchell S. Albert

Int. J. Mol. Sci. 2024, 25(3), 1939; https://doi.org/10.3390/ijms25031939 - 5 Feb 2024

Cited by 1 | Viewed by 1209

Abstract

Molecular magnetic resonance imaging (MRI) is an emerging field that is set to revolutionize our perspective of disease diagnosis, treatment efficacy monitoring, and precision medicine in full concordance with personalized medicine. A wide range of hyperpolarized (HP) ¹²⁹Xe biosensors have been recently developed, demonstrating their potential applications in molecular settings, and achieving notable success within in vitro studies. The favorable nuclear magnetic resonance properties of ¹²⁹Xe, coupled with its non-toxic nature, high solubility in biological tissues, and capacity to dissolve in blood and diffuse across membranes, highlight its superior role for applications in molecular MRI settings. The incorporation of reporters that combine signal enhancement from both hyperpolarized ¹²⁹Xe and chemical exchange saturation transfer holds the potential to address the primary limitation of low sensitivity observed in conventional MRI. This review provides a summary of the various applications of HP ¹²⁹Xe biosensors developed over the last decade, specifically highlighting their use in MRI. Moreover, this paper addresses the evolution of in vivo applications of HP ¹²⁹Xe, discussing its potential transition into clinical settings. Full article

(This article belongs to the Special Issue Molecular Probe: Recent Research and Future Challenges)

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26 pages, 10135 KiB

Open AccessReview

Bisphosphonates as Radiopharmaceuticals: Spotlight on the Development and Clinical Use of DOTAZOL in Diagnostics and Palliative Radionuclide Therapy

by Céleste Souche, Juliette Fouillet, Léa Rubira, Charlotte Donzé, Emmanuel Deshayes and Cyril Fersing

Int. J. Mol. Sci. 2024, 25(1), 462; https://doi.org/10.3390/ijms25010462 - 29 Dec 2023

Viewed by 1026

Abstract

Bisphosphonates are therapeutic agents that have been used for almost five decades in the treatment of various bone diseases, such as osteoporosis, Paget disease and prevention of osseous complications in cancer patients. In nuclear medicine, simple bisphosphonates such as ^99mTc-radiolabelled oxidronate and medronate remain first-line bone scintigraphic imaging agents for both oncology and non-oncology indications. In line with the growing interest in theranostic molecules, bifunctional bisphosphonates bearing a chelating moiety capable of complexing a variety of radiometals were designed. Among them, DOTA-conjugated zoledronate (DOTAZOL) emerged as an ideal derivative for both PET imaging (when radiolabeled with ⁶⁸Ga) and management of bone metastases from various types of cancer (when radiolabeled with ¹⁷⁷Lu). In this context, this report provides an overview of the main medicinal chemistry aspects concerning bisphosphonates, discussing their roles in molecular oncology imaging and targeted radionuclide therapy with a particular focus on bifunctional bisphosphonates. Particular attention is also paid to the development of DOTAZOL, with emphasis on the radiochemistry and quality control aspects of its preparation, before outlining the preclinical and clinical data obtained so far with this radiopharmaceutical candidate. Full article

(This article belongs to the Special Issue Molecular Probe: Recent Research and Future Challenges)

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