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Radiolabeled Molecules in Medicinal Chemistry
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Radiolabeled Molecules in Medicinal Chemistry

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

Deadline for manuscript submissions: closed (1 April 2022) | Viewed by 13796

Special Issue Editor

Dr. Pierre Bohn

E-Mail Website
Guest Editor
1. Institute for Research and Innovation in Biomedicine (IRIB), University of Rouen Normandy, LITIS-QUANTIF EA4108, 76000 Rouen, France
2. Department of nuclear medicine, Henri Becquerel Centre, Rouen, France
Interests: radiochemistry; radiopharmacy; nuclear medicine

Special Issue Information

Dear Colleagues,

Nuclear medicine is a discipline in the midst of a revolution. The appearance of PET cameras with embedded artificial intelligence on the one hand and the emergence of immunotherapies on the other will profoundly modify clinical practices. Now is the time for radiochemists and pharmacists to bring new tracers to patients to support these changes.The synthesis of new tracers will make it possible to support personalized medicine and ultimately the development of new therapies. Thus, imaging of receptors, enzymes, metabolic chains, etc. will be the key to the development of new therapeutic strategies. In addition, targeted radionuclide therapy (TRNT) is a technology in which peptides, monoclonal antibodies or their fragments, nanobodies, etc. are coupled with therapeutic radionuclides such as lutetium-177, yttrium-90, astatine-211. They can also be coupled with imaging radionuclides such as technetium-99m, indium-111, fluorine-18, gallium-68, zirconium-89, etc. to form a theranostic pair. Furthermore, bimodal tracers are emerging, which can, for instance, detect tumors in vivo by nuclear imaging and ex vivo by fluorescence after tumor removal. All researchers working in this interdisciplinary field are cordially invited to submit their work in the form of original articles or reviews. Research works on tracer synthesis and radiosynthesis, small animal imaging, or the improvement of synthetic pathways are welcome. 

Dr. Pierre Bohn
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. 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

  • radiochemistry
  • lutetium-177
  • yttrium-90
  • astatine-211
  • technetium-99m
  • indium-111
  • fluorine-18
  • gallium-68
  • zirconium-89
  • immunotherapy
  • theranostics
  • targeted radionuclide therapy
  • bimodal tracers
  • cancer

Published Papers (4 papers)

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Research

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22 pages, 3045 KiB  
Article
Novel Radioiodinated and Radiofluorinated Analogues of FT-2102 for SPECT or PET Imaging of mIDH1 Mutant Tumours
by Valérie Weber, Lucie Arnaud, Sladjana Dukic-Stefanovic, Barbara Wenzel, Valérie Roux, Jean-Michel Chezal, Thu-Hang Lai, Rodrigo Teodoro, Klaus Kopka, Elisabeth Miot-Noirault, Winnie Deuther-Conrad and Aurélie Maisonial-Besset
Molecules 2022, 27(12), 3766; https://doi.org/10.3390/molecules27123766 - 11 Jun 2022
Cited by 2 | Viewed by 2302
Abstract
Isocitrate dehydrogenases (IDHs) are metabolic enzymes commonly mutated in human cancers (glioma, acute myeloid leukaemia, chondrosarcoma, and intrahepatic cholangiocarcinoma). These mutated variants of IDH (mIDH) acquire a neomorphic activity, namely, conversion of α-ketoglutarate to the oncometabolite D-2-hydroxyglutarate involved in tumourigenesis. Thus, mIDHs have [...] Read more.
Isocitrate dehydrogenases (IDHs) are metabolic enzymes commonly mutated in human cancers (glioma, acute myeloid leukaemia, chondrosarcoma, and intrahepatic cholangiocarcinoma). These mutated variants of IDH (mIDH) acquire a neomorphic activity, namely, conversion of α-ketoglutarate to the oncometabolite D-2-hydroxyglutarate involved in tumourigenesis. Thus, mIDHs have emerged as highly promising therapeutic targets, and several mIDH specific inhibitors have been developed. However, the evaluation of mIDH status, currently performed by biopsy, is essential for patient stratification and thus treatment and follow-up. We report herein the development of new radioiodinated and radiofluorinated analogues of olutasidenib (FT-2102) as tools for noninvasive single photon emission computed tomography (SPECT) or positron emission tomography (PET) imaging of mIDH1 up- and dysregulation in tumours. Nonradiolabelled derivatives 2 and 3 halogenated at position 6 of the quinolinone scaffold were synthesised and tested in vitro for their inhibitory potencies and selectivities in comparison with the lead compound FT-2102. Using a common organotin precursor, (S)-[125I]2 and (S)-[18F]3 were efficiently synthesised by radio-iododemetallation and copper-mediated radiofluorination, respectively. Both radiotracers were stable at room temperature in saline or DPBS solution and at 37 °C in mouse serum, allowing future planning of their in vitro and in vivo evaluations in glioma and chondrosarcoma models. Full article
(This article belongs to the Special Issue Radiolabeled Molecules in Medicinal Chemistry)
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Review

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25 pages, 8770 KiB  
Review
Advances in [18F]Trifluoromethylation Chemistry for PET Imaging
by Felix Francis and Frank Wuest
Molecules 2021, 26(21), 6478; https://doi.org/10.3390/molecules26216478 - 27 Oct 2021
Cited by 18 | Viewed by 3070
Abstract
Positron emission tomography (PET) is a preclinical and clinical imaging technique extensively used to study and visualize biological and physiological processes in vivo. Fluorine-18 (18F) is the most frequently used positron emitter for PET imaging due to its convenient 109.8 min [...] Read more.
Positron emission tomography (PET) is a preclinical and clinical imaging technique extensively used to study and visualize biological and physiological processes in vivo. Fluorine-18 (18F) is the most frequently used positron emitter for PET imaging due to its convenient 109.8 min half-life, high yield production on small biomedical cyclotrons, and well-established radiofluorination chemistry. The presence of fluorine atoms in many drugs opens new possibilities for developing radioligands labelled with fluorine-18. The trifluoromethyl group (CF3) represents a versatile structural motif in medicinal and pharmaceutical chemistry to design and synthesize drug molecules with favourable pharmacological properties. This fact also makes CF3 groups an exciting synthesis target from a PET tracer discovery perspective. Early attempts to synthesize [18F]CF3-containing radiotracers were mainly hampered by low radiochemical yields and additional challenges such as low radiochemical purity and molar activity. However, recent innovations in [18F]trifluoromethylation chemistry have significantly expanded the chemical toolbox to synthesize fluorine-18-labelled radiotracers. This review presents the development of significant [18F]trifluoromethylation chemistry strategies to apply [18F]CF3-containing radiotracers in preclinical and clinical PET imaging studies. The continuous growth of PET as a crucial functional imaging technique in biomedical and clinical research and the increasing number of CF3-containing drugs will be the primary drivers for developing novel [18F]trifluoromethylation chemistry strategies in the future. Full article
(This article belongs to the Special Issue Radiolabeled Molecules in Medicinal Chemistry)
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22 pages, 3189 KiB  
Review
PET Imaging Radiotracers of Chemokine Receptors
by Santosh R. Alluri, Yusuke Higashi and Kun-Eek Kil
Molecules 2021, 26(17), 5174; https://doi.org/10.3390/molecules26175174 - 26 Aug 2021
Cited by 9 | Viewed by 3439
Abstract
Chemokines and chemokine receptors have been recognized as critical signal components that maintain the physiological functions of various cells, particularly the immune cells. The signals of chemokines/chemokine receptors guide various leukocytes to respond to inflammatory reactions and infectious agents. Many chemokine receptors play [...] Read more.
Chemokines and chemokine receptors have been recognized as critical signal components that maintain the physiological functions of various cells, particularly the immune cells. The signals of chemokines/chemokine receptors guide various leukocytes to respond to inflammatory reactions and infectious agents. Many chemokine receptors play supportive roles in the differentiation, proliferation, angiogenesis, and metastasis of diverse tumor cells. In addition, the signaling functions of a few chemokine receptors are associated with cardiac, pulmonary, and brain disorders. Over the years, numerous promising molecules ranging from small molecules to short peptides and antibodies have been developed to study the role of chemokine receptors in healthy states and diseased states. These drug-like candidates are in turn exploited as radiolabeled probes for the imaging of chemokine receptors using noninvasive in vivo imaging, such as positron emission tomography (PET). Recent advances in the development of radiotracers for various chemokine receptors, particularly of CXCR4, CCR2, and CCR5, shed new light on chemokine-related cancer and cardiovascular research and the subsequent drug development. Here, we present the recent progress in PET radiotracer development for imaging of various chemokine receptors. Full article
(This article belongs to the Special Issue Radiolabeled Molecules in Medicinal Chemistry)
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14 pages, 1707 KiB  
Review
Microspheres Used in Liver Radioembolization: From Conception to Clinical Effects
by Philippe d’Abadie, Michel Hesse, Amandine Louppe, Renaud Lhommel, Stephan Walrand and Francois Jamar
Molecules 2021, 26(13), 3966; https://doi.org/10.3390/molecules26133966 - 29 Jun 2021
Cited by 26 | Viewed by 4258
Abstract
Inert microspheres, labeled with several radionuclides, have been developed during the last two decades for the intra-arterial treatment of liver tumors, generally called Selective Intrahepatic radiotherapy (SIRT). The aim is to embolize microspheres into the hepatic capillaries, accessible through the hepatic artery, to [...] Read more.
Inert microspheres, labeled with several radionuclides, have been developed during the last two decades for the intra-arterial treatment of liver tumors, generally called Selective Intrahepatic radiotherapy (SIRT). The aim is to embolize microspheres into the hepatic capillaries, accessible through the hepatic artery, to deliver high levels of local radiation to primary (such as hepatocarcinoma, HCC) or secondary (metastases from several primary cancers, e.g., colorectal, melanoma, neuro-endocrine tumors) liver tumors. Several types of microspheres were designed as medical devices, using different vehicles (glass, resin, poly-lactic acid) and labeled with different radionuclides, 90Y and 166Ho. The relationship between the microspheres’ properties and the internal dosimetry parameters have been well studied over the last decade. This includes data derived from the clinics, but also computational data with various millimetric dosimetry and radiobiology models. The main purpose of this paper is to define the characteristics of these radiolabeled microspheres and explain their association with the microsphere distribution in the tissues and with the clinical efficacy and toxicity. This review focuses on avenues to follow in the future to optimize such particle therapy and benefit to patients. Full article
(This article belongs to the Special Issue Radiolabeled Molecules in Medicinal Chemistry)
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