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임재청,최상무,조은하,김진주 한국방사선산업학회 2013 방사선산업학회지 Vol.7 No.2
Bombesin receptors are overexpressed in many kinds of human tumors. In particular,the gastrin releasing peptide receptor (GRPR) which is also called bombesin receptor subtype 2,has been identified in prostate cancer. In the present study, we developed a bombesin antagonistbased177Lu-labeled peptide, 177Lu-DOTA-Ala(SO3H)-Aminooctanoyl-Gln-Trp-Ala-Val-N methylGly-His-Statine-Leu-NH2(DOTA-sBBNA). DOTA-sBBNA was prepared using a solid phase synthesismethod. It was labeled with 177Lu by a high radiolabeling yield (¤98%), and its Log P valuewas - 2.05. The radiolabeled peptide was highly stable in serum incubation at 37 C for 48 hr. Acompetitive displacement of 125I-[Tyr4]-Bombesin on the PC-3 human prostate carcinoma cellsrevealed that the IC50 value of the peptide was 6.76 nM indicating a highly nanomolar bindingaffinity for GRPR. These results suggest that 177Lu-DOTA-sBBNA can be a potential candidatefor targeting prostate cancer, and further studies to evaluate its biological characteristics areneeded.
임재청,김다미,남성수,조은하,이소영,정혜경,이인기 충북대학교 동물의학연구소 2022 Journal of Biomedical and Translational Research Vol.23 No.4
Following the previous study, the toxicity of a single subcutaneous administration of the Thyrokitty injection (I-131) and the side effects that may occur at therapeutic doses were confirmed. The Thyrokitty injection (I-131) was administered subcutaneously once at a dose of 0, 2.0, 6.0, and 18.0 mCi/kg, 5 male and female rats per group, and mortality, general symptom observation, and weight measurement were performed for 2 weeks, followed by observation of autopsy findings. There were no deaths, and no statistically significant weight change was observed. Mild hair loss, fissures, and crusting were observed by general symptom observation, but it was not a toxic change related to the Thyrokitty injection (I-131). Gastric atrophy and a decrease in the size of the spleen were observed by the autopsy. As a results of single subcutaneous administration of the Thyrokitty Injection (I-131) to rats at a maximum dose of 18.0 mCi/kg, a decrease in the size of the spleen and gastric atrophy were observed as the dose of the Thyrokitty Injection (I-131) increased, which may be related to the test substance. No abnormal findings related to the Thyrokitty injection (I-131) were observed. Therefore, the approximate lethal dose of the Thyrokitty injection (I-131) was 18.0 mCi/kg or more. In addition, as reported for the treatment of feline hyperthyroidism with radioiodine (131I), side effects of the Thyrokitty injection (I-131) are expected to be extremely rare. Temporary dysphagia and fever may occur, but it will recover naturally. It should be administered with caution in cats with diseases such as urinary system, cardiovascular system, gastrointestinal system and endocrine system, especially with kidney disease. And it should not be used in cats who are pregnant, lactating, or likely. It is expected that the Thyrokitty injection (I-131) can be used for clinical treatment in Korea as a veterinary drug.
Development of Freeze-Dried DOTMP Kits for Labeling with 68Ga
임재청,최상무,조은하,이소영,도소희,김수영 한국방사선산업학회 2015 방사선산업학회지 Vol.9 No.2
Lyophilized DOTMP kits were prepared using DOTMP, ammonium acetate, andascorbic acid. The 68Ga-DOT MP was prepared by incubating the kit dissolved in 0.5 ml ofconcentrated 68Ga using NaCl method and 0.5 ml of DDW, at 100°C for 7 min. The labeling yieldwas evaluated by two solvent systems of TLC. 1 MBq of concentrated 68Ga was labeled with 0.8μg of DOTMP by high radiolabeling yield (>98%), which was determined by two TLC methods. The composition of the prepared freeze-dried vial is 400 μg of DOTMP, 19.27 mg of ammoniumacetate and 17.62 mg of ascorbic acid. ~555 MBq of 68Ga-DOT MP was prepared with excellentradiochemical purity (>98%) and it was stable for 4 hr at room temperature. In conclusion,Freeze-dried DOTMP kits for the convenient preparation of 68Ga-DOTMP have been developed. Availability of this kit is expected to stimulate the widespread use of 68Ga-DOTMP in the fields ofnuclear medicine.
임재청,최상무,조은하,김진주 한국방사선산업학회 2013 방사선산업학회지 Vol.7 No.2
In this study, a novel bombesin (BBN) analogues, DOTA-Ala(SO3H)-4 aminobenzoyl-Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH2 (DOTA-sBBN) and DOTA-Lys(glucose)-4 aminobenzoyl-Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH2 (DOTA-gluBBN), were synthesized and radiolabeled,and their binding affinities were evaluated. Peptides were prepared by a solid phase synthesismethod and their purities were over 98%. DOTA is the chelating agent for 177Lu-labeling, and theDOTA-conjugated peptides were radiolabeled with 177Lu 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 177Lu-DOTA-sBBN and 72.97% of 177Lu-DOTA-gluBBN were left undegraded by the serumincubation at 37 C for 48 hr. A competitive displacement of 125I-[Tyr4]-BBN on the PC-3 humanprostate carcinoma cells revealed that 50% inhibitory concentration (IC50) were 1.46 nM ofDOTA-sBBN and 4.67 nM of DOTA-gluBBN indicating a highly nanomolar binding affinity forGRPR. Therefore, it is concluded that 177Lu-DOTA-sBBN and 177Lu-DOTA-gluBBN can bepotential candidates as a targeting modality for the Gastrin-releasing peptide receptor (GRPR)-over-expressing tumors, and further studies to evaluate their biological and pharmacological characteristicsare needed.
임재청,김다미,남성수,조은하,이소영,정혜경,Inki Lee 충북대학교 동물의학연구소 2022 Journal of Biomedical and Translational Research Vol.23 No.4
Radioiodine (131I) has been used for the treatment of feline hyperthyroidism since the 1990s in the USA and Europe, and it is recommended as the most effective treatment for feline hyperthyroidism because it has a high therapeutic effect, small side effects, and does not require anesthesia. In this study, the pharmacological properties of the Thyrokitty injection (I-131), which is being developed as a treatment for feline hyperthyroidism, using radioiodine (131I) as an active ingredient, was tested. The %cell uptake of the Thyrokitty injection (I-131) in FRTL5 thyroid cells was 0.410 ± 0.016%, which was about 18 times higher compared to Clone 9 hepatocytes, and it was decreased by 30.7% due to the competitive reaction with iodine (sodium iodide). In addition, the %cell growth of the FRTL-5 thyroid cells was reduced by 25.0% by treatment with the Thyrokitty injection (I-131). As a result of the tissue distribution test, the Thyrokitty injection (I-131) was distributed at the highest concentration at 0.083 hours (5 minutes) after subcutaneous administration to animals in most organs except the stomach, small intestine, large intestine, muscle and thyroid gland, and it was excreted mainly through the kidneys. The stomach and thyroid gland showed a typical distribution pattern observed when radioiodine (131I) was administered. In addition, about 78.45% of the total amount of excretion was excreted within 48 hours, of which more than 85% was excreted in urine. In conclusion, the Thyrokitty injection (I-131) has the same mechanism of action, potency, absorption, distribution, metabolism and excretion characteristics as radioiodine (131I) reported in connection with the treatment of feline hyperthyroidism. In the future, using the results of this study, it is expected that the Thyrokitty (I-131) could be safely used in the clinical treatment of feline hyperthyroidism
임재청,이정락,정연모 경희-다반 ASIC 설계교육센터 2003 경희-다반 ASIC센터 논문집 Vol.4 No.-
암호화 해쉬 알고리즘은 인터넷 보안 및 인증에 널리 사용되는 알고리즘으로서 하드웨어로 구현함으로서 빠르고 신뢰성 있는 동작을 보장할 수 있다. 본 논문에서는 여러 해쉬 알고리즘 중에서 SHA-1을 VHDL로 모델링 하였으며 단계연산에 필요한 연산들의 최적화된 스케줄링으로 동작속도를 증가 시켰다.
임재청,조은하,이소영,도소희,김수용,정성희 한국공업화학회 2016 한국공업화학회 연구논문 초록집 Vol.2016 No.1
Radiation therapy which utilizes radiation to induce cell death is an effective cancer therapeutic option in conjunction with chemotherapy and surgery. In particular, tumor cell-targeting peptides have been successfully used in peptide receptor radionuclide therapy (PRRT). PRRT is a tumor-directed systemic treatment, and <sup>68</sup>Ga/<sup>177</sup>Lu-octreatate for the treatment of neuroendocrine tumor has shown the therapeutic effect of PRRT. In this study, a series of DOTA chelator-conjugated peptides were synthesized, and radiolabeled with 68Ga and <sup>177</sup>Lu. The pharmacokinetic characteristics, imaging diagnosis and therapeutic efficacy of the radiolabeled peptides were investigated using PC-3 human prostate carcinoma xenograft model in vivo.