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Cancers
Special Issues
Radioprobes and Other Bioconjugates for Cancer Theranostics
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Radioprobes and Other Bioconjugates for Cancer Theranostics

A special issue of Cancers (ISSN 2072-6694). This special issue belongs to the section "Methods and Technologies Development".

Deadline for manuscript submissions: closed (31 March 2023) | Viewed by 12753

Special Issue Editor

Prof. Dr. Yasushi Arano

E-Mail Website
Guest Editor
Professor Emeritus, Chiba University, Chiba, Japan
Interests: nuclear medicine; molecular imaging; targeted radionuclide therapy; radiopharmaceuticals; radiochemistry; radiopharmacy

Special Issue Information

Dear Colleagues,

Theranostics is the systematic integration of targeted diagnostics and therapeutics, which promotes precise and personalized cancer treatment. A variety of theranostic pairs have been proposed and evaluated so far, including SPECT/PET imaging and targeted radionuclide therapy, fluorescent/photoacoustic imaging and photodynamic/chemodynamic/thermodynamic  therapy. The diagnostic imaging before treatment allows the selection of patients who would benefit from the treatment. The diagnostic imaging post-therapy provides the efficacy of the treatment. The Special Issue of Cancers calls for manuscripts that describe a new chemical/biological approach that significantly boosts the clinical application of theranostic pharmaceutics, including the improvement of pharmacokinetics/pharmacodynamics, therapeutic efficacy, or safety of theranostic pairs. A proposal of a new targeting device, a new class of theranostic pair, and a labeling reagent of improved stability of the resulting label is also appreciated.

Prof. Dr. Yasushi Arano
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. 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

  • Cancer
  • Theranostics
  • Targeted Imaging
  • Targeted Therapy
  • Radionuclide
  • Fluorescent
  • Photoacoustic
  • Photodynamic
  • Chemodynamic
  • Thermodynamic
  • Magnetic Resonance.

Published Papers (6 papers)

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Editorial

Jump to: Research, Other

2 pages, 142 KiB  
Editorial
Editorial for the Specific Issue of Radioprobes and Other Bioconjugates for Cancer Theranostics
by Yasushi Arano
Cancers 2024, 16(3), 541; https://0-doi-org.brum.beds.ac.uk/10.3390/cancers16030541 - 26 Jan 2024
Viewed by 520
Abstract
Theranostics refers to the systematic integration of targeted diagnostics and therapeutics, which promotes precise and personalized cancer treatment [...] Full article
(This article belongs to the Special Issue Radioprobes and Other Bioconjugates for Cancer Theranostics)

Research

Jump to: Editorial, Other

11 pages, 2622 KiB  
Article
Enhancing the Therapeutic Effect of 2-211At-astato-α-methyl-L-phenylalanine with Probenecid Loading
by Hirofumi Hanaoka, Yasuhiro Ohshima, Hiroyuki Suzuki, Ichiro Sasaki, Tadashi Watabe, Kazuhiro Ooe, Shigeki Watanabe and Noriko S. Ishioka
Cancers 2021, 13(21), 5514; https://0-doi-org.brum.beds.ac.uk/10.3390/cancers13215514 - 03 Nov 2021
Cited by 2 | Viewed by 2848
Abstract
L-type amino acid transporter 1 (LAT1) might be a useful target for tumor therapy since it is highly expressed in various types of cancers. We previously developed an astatine-211 (211At)-labeled amino acid derivative, 2-211At-astato-α-methyl-L-phenylalanine (2-211At-AAMP), and demonstrated [...] Read more.
L-type amino acid transporter 1 (LAT1) might be a useful target for tumor therapy since it is highly expressed in various types of cancers. We previously developed an astatine-211 (211At)-labeled amino acid derivative, 2-211At-astato-α-methyl-L-phenylalanine (2-211At-AAMP), and demonstrated its therapeutic potential for LAT1-positive cancers. However, the therapeutic effect of 2-211At-AAMP was insufficient, probably due to its low tumor retention. The preloading of probenecid, an organic anion transporter inhibitor, can delay the clearance of some amino acid tracers from the blood and consequently increase their accumulation in tumors. In this study, we evaluated the effect of probenecid preloading on the biodistribution and therapeutic effect of 2-211At-AAMP in mice. In biodistribution studies, the blood radioactivity of 2-211At-AAMP significantly increased with probenecid preloading. Consequently, the accumulation of 2-211At-AAMP in tumors was significantly higher with probenecid than without probenecid loading. In a therapeutic study, tumor growth was suppressed by 2-211At-AAMP with probenecid, and the tumor volume was significantly lower in the treatment group than in the untreated control group from day 2 to day 30 (end of the follow-up period) after treatment. These results indicate that probenecid loading could improve the therapeutic effect of 2-211At-AAMP by increasing its accumulation in tumors. Full article
(This article belongs to the Special Issue Radioprobes and Other Bioconjugates for Cancer Theranostics)
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10 pages, 1879 KiB  
Article
Enhanced Delivery of Thermoresponsive Polymer-Based Medicine into Tumors by Using Heat Produced from Gold Nanorods Irradiated with Near-Infrared Light
by Kohei Sano, Yumi Ishida, Toshie Tanaka, Tatsuya Mizukami, Tomono Nagayama, Yoshie Haratake, Masayuki Munekane, Toshihide Yamasaki and Takahiro Mukai
Cancers 2021, 13(19), 5005; https://0-doi-org.brum.beds.ac.uk/10.3390/cancers13195005 - 06 Oct 2021
Cited by 4 | Viewed by 1574
Abstract
The aim of this study was to establish a drug delivery system (DDS) for marked therapy of tumors using a thermoresponsive polymer, polyoxazoline (POZ). The effectiveness of the following was investigated: (i) the delivery of gold nanorods (GNRs) to tumor tissues, (ii) heat [...] Read more.
The aim of this study was to establish a drug delivery system (DDS) for marked therapy of tumors using a thermoresponsive polymer, polyoxazoline (POZ). The effectiveness of the following was investigated: (i) the delivery of gold nanorods (GNRs) to tumor tissues, (ii) heat production of GNR upon irradiation with near-infrared (NIR) light, and (iii) high accumulation of an intravenously injected radiolabeled POZ as a drug carrier in tumors by sensing heat produced by GNRs. When the GNR solution was irradiated with NIR light (808 nm), the solution temperature was increased both in a GNR-concentration-dependent manner and in a light-dose-dependent manner. POZ, with a lower critical solution temperature of 38 °C, was aggregated depending on the heat produced by the GNR irradiated by NIR light. When it was intratumorally pre-injected into colon26-tumor-bearing mice, followed by NIR light irradiation (GNR+/Light+ group), the tumor surface temperature increased to approximately 42 °C within 5 min. Fifteen minutes after irradiation with NIR light, indium-111 (111In)-labeled POZ was intravenously injected into tumor-bearing mice, and the radioactivity distribution was evaluated. The accumulation of POZ in the tumor was significantly (approximately 4-fold) higher than that in the control groups (GNR+/without NIR light irradiation (Light–), without injection of GNR (GNR–)/Light+, and GNR–/Light– groups). Furthermore, an in vivo confocal fluorescence microscopy study, using fluorescence-labeled POZ, revealed that uptake of POZ by the tumor could be attributed to the heat produced by GNR. In conclusion, we successfully established a novel DDS in which POZ could be efficiently delivered into tumors by using the heat produced by GNR irradiated with NIR light. Full article
(This article belongs to the Special Issue Radioprobes and Other Bioconjugates for Cancer Theranostics)
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17 pages, 2231 KiB  
Article
Synthesis and Characterization of Radiogallium-Labeled Cationic Amphiphilic Peptides as Tumor Imaging Agents
by Takeshi Fuchigami, Takeshi Chiga, Sakura Yoshida, Makoto Oba, Yu Fukushima, Hiromi Inoue, Akari Matsuura, Akira Toriba and Morio Nakayama
Cancers 2021, 13(10), 2388; https://0-doi-org.brum.beds.ac.uk/10.3390/cancers13102388 - 14 May 2021
Cited by 3 | Viewed by 1977
Abstract
SVS-1 is a cationic amphiphilic peptide (CAP) that exhibits a preferential cytotoxicity towards cancer cells over normal cells. In this study, we developed radiogallium-labeled SVS-1 (67Ga-NOTA-KV6), as well as two SVS-1 derivatives, with the repeating KV residues replaced by RV or [...] Read more.
SVS-1 is a cationic amphiphilic peptide (CAP) that exhibits a preferential cytotoxicity towards cancer cells over normal cells. In this study, we developed radiogallium-labeled SVS-1 (67Ga-NOTA-KV6), as well as two SVS-1 derivatives, with the repeating KV residues replaced by RV or HV (67Ga-NOTA-RV6 and 67Ga-NOTA-HV6). All three peptides showed high accumulation in epidermoid carcinoma KB cells (53–143% uptake/mg protein). Though 67Ga-NOTA-RV6 showed the highest uptake among the three CAPs, its uptake in 3T3-L1 fibroblasts was just as high, indicating a low selectivity. In contrast, the uptake of 67Ga-NOTA-KV6 and 67Ga-NOTA-HV6 into 3T3-L1 cells was significantly lower than that in KB cells. An endocytosis inhibition study suggested that the three 67Ga-NOTA-CAPs follow distinct pathways for internalization. In the biodistribution study, the tumor uptakes were found to be 4.46%, 4.76%, and 3.18% injected dose/g of tissue (% ID/g) for 67Ga-NOTA-KV6, 67Ga-NOTA-RV6, and 67Ga-NOTA-HV6, respectively, 30 min after administration. Though the radioactivity of these peptides in tumor tissue decreased gradually, 67Ga-NOTA-KV6, 67Ga-NOTA-RV6, and 67Ga-NOTA-HV6 reached high tumor/blood ratios (7.7, 8.0, and 3.8, respectively) and tumor/muscle ratios (5.0, 3.3, and 4.0, respectively) 120 min after administration. 67Ga-NOTA-HV6 showed a lower tumor uptake than the two other tracers, but it exhibited very low levels of uptake into peripheral organs. Overall, the replacement of lysine in SVS-1 with other basic amino acids significantly influenced its binding and internalization into cancer cells, as well as its in vivo pharmacokinetic profile. The high accessibility of these peptides to tumors and their ability to target the surface membranes of cancer cells make radiolabeled CAPs excellent candidates for use in tumor theranostics. Full article
(This article belongs to the Special Issue Radioprobes and Other Bioconjugates for Cancer Theranostics)
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Graphical abstract

13 pages, 5511 KiB  
Article
In Vitro and In Vivo Cell Uptake of a Cell-Penetrating Peptide Conjugated with Fluorescent Dyes Having Different Chemical Properties
by Hideo Takakura, Honoka Sato, Kohei Nakajima, Motofumi Suzuki and Mikako Ogawa
Cancers 2021, 13(9), 2245; https://0-doi-org.brum.beds.ac.uk/10.3390/cancers13092245 - 07 May 2021
Cited by 9 | Viewed by 3980 | Correction
Abstract
In molecular imaging, a targeting strategy with ligands is widely used because specificity can be significantly improved. In fluorescence imaging based on a targeting strategy, the fluorescent dyes conjugated with ligands may affect the targeting efficiency depending on the chemical properties. Herein, we [...] Read more.
In molecular imaging, a targeting strategy with ligands is widely used because specificity can be significantly improved. In fluorescence imaging based on a targeting strategy, the fluorescent dyes conjugated with ligands may affect the targeting efficiency depending on the chemical properties. Herein, we used a cell-penetrating peptide (CPP) as a ligand with a variety of fluorescent cyanine dye. We investigated in vitro and in vivo cell uptake of the dye-CPP conjugates when cyanine dyes with differing charge and hydrophilicity/lipophilicity were used. The results showed that the conjugates with positively charged and lipophilic cyanine dyes accumulated in cancer cells in vitro, but there was almost no accumulation in tumors in vivo. On the other hand, the conjugates with negatively charged and hydrophilic cyanine dyes did not accumulate in cancer cells in vitro, but fluorescence was observed in tumors in vivo. These results show that there are some cases in which the cell uptake of the dye-peptide conjugates may differ significantly between in vitro and in vivo experiments due to the chemical properties of the fluorescent dyes. This suggests that attention should be paid to the chemical properties of fluorescent dyes in fluorescence imaging based on a targeting strategy. Full article
(This article belongs to the Special Issue Radioprobes and Other Bioconjugates for Cancer Theranostics)
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Other

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7 pages, 4868 KiB  
Correction
Correction: Takakura et al. In Vitro and In Vivo Cell Uptake of a Cell-Penetrating Peptide Conjugated with Fluorescent Dyes Having Different Chemical Properties. Cancers 2021, 13, 2245
by Hideo Takakura, Honoka Sato, Kohei Nakajima, Motofumi Suzuki and Mikako Ogawa
Cancers 2022, 14(8), 1880; https://0-doi-org.brum.beds.ac.uk/10.3390/cancers14081880 - 08 Apr 2022
Viewed by 986
Abstract
There was an error in the description in the original publication, and it contained information that should not have been disclosed [...] Full article
(This article belongs to the Special Issue Radioprobes and Other Bioconjugates for Cancer Theranostics)
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