• Journal of Radiation Industry
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• v.9 no.4
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• pp.193-198
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• 2015

Most of targeted therapies block the action of certain enzymes, proteins, or other molecules involved in the growth and spread of cancer cells to produce its cytotoxic effect. Either small molecule drugs or monoclonal antibodies are mostly used in targeted therapies. Unfortunately, targeted therapy has a certain degree of unwanted side effect like other cytotoxicity inducing chemotherapies. To overcome and to reduce unwanted side effects during a cancer therapy, recently radiopeptide therapies has got the worlds' attraction for the tumor targeting modalities due to its beneficial effect on less side effect compared to cytotoxic chemotherapies. Among radiopeptide therapies, $^{177}Lu$-DOTATATE is a major modality as an effective one invented so far in treating neuroendocrine tumor (NET) and it has been in clinical trials at least one decade. Although it does have rather effective therapeutic effect on NET, it has less effective in rather large solid tumor. There are many ways to improve or increase therapeutic effect of radiopeptide are a finding the potent small molecules to target the tumor site selectively, or a labeling with radioisotope of emitting high energy, or an improving its biological half-life by introducing different moieties to increase lipophilicity. Present study was focus to increase a biological half-life of radio somatostatin which will target the somatostatin receptor by altering the bifunctional chelator (BFCA) by introducing lipophilic moiety to the somatostatin, which would make the labeled peptide stay longer in the tumor site and thus it can intensify the therapeutic effect on tumor cell itself and around tissues.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.1 no.1
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• pp.23-30
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• 2015

Radioisotopes emitting low-range highly ionizing radiation such as ${\beta}$-particles are of increasing significance in internal radiotherapy. Among the ${\beta}$-particle emitting radioisotopes, $^{67}Cu$ is an attractive radioisotope for various nuclear medicine applications due to its medium energy ${\beta}$-particle, gamma emissions, and 61.83-hour half-life, which can also be used with $^{64}Cu$ for PET imaging. The production and application of the ${\beta}$-emitting radioisotope $^{67}Cu$ for therapeutic radiopharmaceutical are outlined, and different production routes are discussed. A survey of copper chelators used for antibody labeling is provided. It has been produced via proton, alpha, neutron, and gamma irradiations followed by solvent extraction, ion exchange, electrodeposition. Clinical studies using $^{67}Cu$-labelled antibodies in lymphoma, colon carcinoma and bladder cancer patients are reviewed. Widespread use of this isotope for clinical studies and preliminary treatments has been limited by unreliable supplies, cost, and difficulty in obtaining therapeutic quantities.

• Journal of Radiation Industry
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• v.7 no.2_3
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• pp.191-200
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• 2013

In this study, a novel bombesin (BBN) analogues, DOTA-Ala($SO_3H$)-4 aminobenzoyl-Gln-Trp-Ala-Val-Gly-His-Leu-Met-$NH_2$ (DOTA-sBBN) and DOTA-Lys(glucose)-4 aminobenzoyl-Gln-Trp-Ala-Val-Gly-His-Leu-Met-$NH_2$ (DOTA-gluBBN), were synthesized and radiolabeled, and their binding affinities were evaluated. Peptides were prepared by a solid phase synthesis method and their purities were over 98%. DOTA is the chelating agent for $^{177}Lu$-labeling, and the DOTA-conjugated peptides were radiolabeled with $^{177}Lu$ by a high radiolabeling yield (>98%). The Log P values of DOTA-sBBN and DOTA-gluBBN were -2.20 and -2.79, respectively. 50.41% of $^{177}Lu$-DOTA-sBBN and 72.97% of $^{177}Lu$-DOTA-gluBBN were left undegraded by the serum incubation at $37^{\circ}C$ for 48 hr. A competitive displacement of $^{125}I-[Tyr^4]$-BBN on the PC-3 human prostate carcinoma cells revealed that 50% inhibitory concentration ($IC_{50}$) were 1.46 nM of DOTA-sBBN and 4.67 nM of DOTA-gluBBN indicating a highly nanomolar binding affinity for GRPR. Therefore, it is concluded that $^{177}Lu$-DOTA-sBBN and $^{177}Lu$-DOTA-gluBBN can be potential candidates as a targeting modality for the Gastrin-releasing peptide receptor (GRPR)-over-expressing tumors, and further studies to evaluate their biological and pharmacological characteristics are needed.

• Nuclear Engineering and Technology
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• v.50 no.8
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• pp.1355-1363
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• 2018

Many radionuclides exist in normal environment and artificial radionuclides also can be detected. The radionuclides ($^{131}I$) are widely used for labeling compounds and radiation therapy. In Korea, the radionuclide ($^{131}I$) is produced at the Radioisotope Production Facility (RIPF) at the Korea Atomic Energy Research Institute in Daejeon. The residents around the RIPF assume that $^{131}I$ detected in environmental samples is produced from RIPF. To ensure the safety of the residents, the radioactive concentration of $^{131}I$ near the RIPF was investigated by monitoring environmental samples along the Gap River. The selected geographical places are near the nuclear installation, another possible location for $^{131}I$ detection, and downstream of the Gap River. The first selected places are the "front gate of KAERI", and the "Donghwa bridge". The second selected place is the sewage treatment plant. Therefore, the Wonchon bridge is selected for the upstream of the plant and the sewage treatment plant is selected for the downstream of the plant. The last selected places are the downstream where the two paths converged, which is Yongshin bridge (in front of the cogeneration plant). In these places, environmental samples, including sediment, fish, surface water, and aquatic plants, were collected. In this study, the radioactive iodine ($^{131}I$) detection along the Gap River will be investigated.

• Biotechnology and Bioprocess Engineering:BBE
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• v.5 no.3
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• pp.191-195
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• 2000

Quantitation of N7-methyldeoxyguanosine (N7-MedG) produced in the in vitro N-methly-N-nitrosuourea (NMU) action on thymus DNA has been achieved by enzymatic degradation, liquid chromatoraphic separaphic separation and desorption chemical ionization tandem mass spectrometry. In conjunction with the resolving power HPLC in the separation of isomers, desorprion chemical ionization tandem mass spectrometry has utilized in determining modified nucleosides at low levels using a stable-isotope labled compound as an internal reforence. The quantitative estimation of N7-methyldeoxyguanosine was previously established by an independent HPLC analysis of methylated calf thymus DNA. A sensitive and specific methodogy for the quantitation of N7-MedG at the picomole level using HPLC combined with tandem mass spectrometry without radioisotope labeling process is presented. The potential of the liquid chromatoraphic tandem mass exposure to methlation agents in vitro.

• Journal of the korean society of oceanography
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• v.31 no.2
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• pp.97-106
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• 1996

Advantages and disadvantages of four radioisotopic methods, $^{3}H$-thymidine, $^{3}H$-adenine, $^{3}H$-leucine, and $^{35}S$-sulfate, for measuring bacterial production were reviewed. The maior issues discussed in production methods were: (1) whether all the actively growing bacteria take up the radiolabeled (organic) tracers; (2) how each target molecule should be purified (nonspecific labeling); and (3) how important the determination of the precursor pool specific activity is (internal isotope dilution). Since all the radioisotoic methods have their own advantages and disadvantages, careful consideration must be paid in choosing the radioisotope according to the conditions of each environment investigated.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.7 no.2
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• pp.133-140
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• 2021

Various iron oxide nanoparticle-based radiomaterials(IO-NRM) can be used for multimodal imaging of magnetic resonance imaging and molecular imaging, can be easily sized, can be easily functionalized, and have biocompatibility, making them a very good platform for molecular imaging. Based on the previously revealed molecular imaging technology of iron oxide nanoparticles, this paper introduces the in vivo distribution and use in various diseases through iron oxide nanoparticles-based radiolabeled compounds for diagnosis and treatment of iron oxide nanoparticles-based molecular imaging platforms. We would like to look forward to its potential as a radiopharmaceutical.

• Journal of Microbiology and Biotechnology
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• v.16 no.10
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• pp.1491-1498
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• 2006

The feasibility of pullulan acetate nanoparticles (PAN) with ionic strength (IS) sensitivity as a radioisotope carrier to inhibit tumor growth is demonstrated. PAN was radiolabeled with rhenium 188 (Re-188) without any chelating agents. The labeling efficiency of Re-188 into PAN (Re-188PAN) was $49.3{\pm}4.0%$ as determined by TLC. The tumor volumes of mice treated with 0.45 mCi of Re-188-PAN were measured and compared with that of free Re-188 after 5 days of intratumoral injection. For the histological evaluation of apoptotic nuclei of tumor cells, hematoxylin and eosin (H&E), and terminal deoxynucleotidyl transferase biotinylated deoxyuridine triphosphate nick end labeling (TUNEL) staining were performed. The mean tumor volume of the Re-188-PAN-treated group was decreased by 36% after 5 days, whereas that the free Re-188-treated group was decreased by only 15% (P<0.05). The mean number of TUNEL-positive cells in Re-188-PAN-treated tumors at $144.3{\pm}79.9$ cells/section was significantly greater than the control ($26.7{\pm}7.9$ cells/section, P=0.03). The numbers of leukocyte and lymphocyte were decreased in both free Re-188- and Re-188-PAN-treated mice. These results indicated that the intratumoral injection of Re-188-PAN effectively inhibits the tumor growth by prolonging Re-188 retention time in tumor site induced by the IS sensitivity.

• Journal of Radiopharmaceuticals and Molecular Probes
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• v.8 no.1
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• pp.45-49
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• 2022

With the development of monoclonal antibodies, therapeutic or diagnostic radioisotope has been successfully delivered at tumor sites with high selectivity for antigens. Different approaches have been applied to improve the tumor-to-normal ratio by considering the in vivo stability of radioimmunoconjugates as a prerequisite. Various stable and inert antibody radiolabeling techniques for radioimmunoconjugate preparation have been extensively evaluated to enhance in vivo stability. Antibody radiolabeling techniques should be rapid and easy; they should not disrupt the immunoreactivity and in vivo behavior of antibodies, which are coupled with a bifunctional chelator (BFC) to stably coordinate with a radiometal. For the design of BFCs, radiometal coordination properties must be considered. However, various diagnostic radionuclides, such as ⁸⁹Zr, ⁶⁴Cu, ⁶⁸Ga, ¹¹¹ln, and ^99mTc, or therapeutic radionuclides, such as ¹⁷⁷Lu, ⁶⁷Cu, ⁹⁰Y, and ²²⁵Ac, have been increasingly used for antibody radiolabeling. In addition to useful radionuclides, ⁶⁴Cu and ¹⁷⁷Lu with the most accessible or the highest production rates in many countries should be considered. In this review, we mainly discussed antibody radiolabeling techniques and conditions that involve ⁶⁴Cu and ¹⁷⁷Lu radiometals.

• The Korean Journal of Nuclear Medicine
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• v.34 no.4
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• pp.344-352
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• 2000

Purpose: Re-188-Hydroxyethylidene diphosphonate (HEDP) is a new cost-effective agent for systemic radioisotope therapy of metastatic bone pain. We investigated the influence of carrier for labeling and biodistribution of Re-188-HEDP using HEDP kit with or without carrier ($KReO_4$). Materials and Methods: The kits (HEDP 15 mg, gentisic acid 4 mg and $SnCl_2.2H_2O_2$ 4.5 mg) with or without carrier ($KReO_4$ 0.1 mg) were labeled with Re-188 solution, made available from an in-house generator by boiling for 15 min. We compared the labeling efficiency and stability of carrier-added and carrier-free preparations of Re-188-HEDP Biodistribution and imaging studies of each preparation were performed in ICR mice ($1.85{\sim}3.7MBq/0.1ml$) and SD rats ($74.1{\sim}85.2MBq/0.5ml$). Results: The carrier-added preparation showed high labeling efficiency (95% at pH 5) and high stability in serum (88%, 3 hr). However, the carrier-free preparation showed low labeling efficiency (59% at pH 5) and low stability (43%, 3 hr). The carrier-added preparation showed high uptake in bone and low uptake in stomach and kidneys. However, the carrier-free preparation showed lower uptake in bone and higher uptake in both stomach and kidneys, which is supposed to be due to released perrhenate. The carrier-added preparation also showed better images with higher skeletal accumulation, lower uptake in other organs and lower soft tissue uptake than the carrier-free preparation. Conclusion: The results of these studies clearly demonstrate that addition of carrier perrhenate is required for high labeling efficiency, stability, bone uptake and good image quality of Re-188-HEDP.