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( Sajid Mushtaq ),전종호 한국공업화학회 2016 한국공업화학회 연구논문 초록집 Vol.2016 No.0
The purpose of this study was to synthesize (125)I-labeled 2-(4-iodophenethyl)-2-methylmalonic acid ([(125)I]IMA) and its biodistribution study for the development of new apoptosis imaging tracer. The optimized radiolabeling procedure provided [(125)I]IMA with high radiochemical yield (75.5 ± 5.2%) and excellent radiochemical purity (>99%) within 100 min. Specific radioactivity of [(125)I]IMA was observed to be 31.0 MBq/mol. Ex vivo biodistribution study of [(125)I]IMA was carried out using male ICR mouse and the result showed the uptake values in apoptotic cells of the testes of the male mice were more than 1.7 fold higher than those of leg muscle. Those results demonstrated that [(125)I]IMA will be a potentially useful radiotracer for in vivo imaging of apoptotic cell and tissue.
PSMA Inhibitors for Nuclear Imaging and Radiotherapy of Prostate Cancer
Sajid Mushtaq,Tugsuu Uyanga,박지애,김정영 대한방사성의약품학회 2023 Journal of radiopharmaceuticals and molecular prob Vol.9 No.1
Prostate cancer ranks as the world's second most frequently diagnosed cancer among men, and is responsible for the fifth highest number of cancer-related deaths in this population. The development of effective diagnostic and therapeutic approaches for prostate cancer remains a major challenge in the field of oncology. Over the past few years, the prostate-specific membrane antigen (PSMA) has raised as a hopeful tracer for the diagnosis and treatment of prostate cancer.Various radioisotopes, such as 131I, 99mTc, 68Ga, and 177Lu, have been used to label PSMA analogues, with varying degrees of success. Among these, 68Ga-PSMA-11 and 177Lu-PSMA-617 have emerged as the most promising radioligands for clinical use. Recently, researchers have been exploring the use of other radioisotopes, such as 211At, 89Zr, 64/67Cu, and 203/212Pb, for the labeling of PSMA-targeted radioligands. These radioisotopes have unique properties that may offer advantages over existing radioligands, such as longer half-lives, higher specific activities, and different emission profiles. Efforts are currently underway to develop these radiopharmaceuticals and make them more widely available for clinical use. These exciting developments highlight the potential of PSMA-targeted radioligands for the diagnosis and treatment of prostate cancer, and provided significant implications for the management of this disease in the future. The current study aims to provide a comprehensive summary of the latest research and clinical applications of radiolabeled PSMA inhibitors for diagnoses and therapy of prostate cancer, emphasizing the exciting developments in the field and their potential impact on clinical practice
Sajid Mushtaq,Jung Eun Park,Ha Eun Shim,Chang Heon Lee,Hee Soon Shin,So-Young Lee,Jongho Jeon 대한환경공학회 2022 Environmental Engineering Research Vol.27 No.5
A lot of people in Korea have suffered from severe toxicity of PHMG, a humidifier disinfectant. To assess the risk and in-depth mechanistic understanding of toxicity posed by a hazardous substance, it is essential to determine its biological uptake in organs. In this study, we investigate the biodistribution of PHMG using radioanalytical techniques. By labeling PHMG with radioactive indium (<SUP>111</SUP>In), the uptake values of PHMG in organs can be measured after intravenous injection in Sprague–Dawley rats for up to 168 h. The results indicate that PHMG is distributed in the liver (28.63% injected dose (%ID)) and lungs (12.44%ID) at 30 min post administration. In addition, the clearance rate of PHMG distributed in the internal organs is slow, with approximately 65% of injected PHMG remaining in the lungs after 1 week. Moreover, we quantified biodistribution of the radiolabeled PHMG exposed through intratracheal instillation and oral administration routes, and the observed data were compared to each other to understand in vivo behavior of PHMG. In addition, radiolabeled PHMG in an animal model can be visualized using SPECT/CT. The obtained results indicate that repetitive exposure to PHMG results in damage to lungs, as well as extrapulmonary organs.
Inverse Electron-demand Diels-Alder 반응을 이용한 핵의학 영상 프로브의 합성 및 활용
( Sajid Mushtaq ),전종호 ( Jongho Jeon ) 한국공업화학회 2017 공업화학 Vol.28 No.2
1,2,4,5-테트라진 유도체를 이용한 inverse electron-demand Diels-Alder (IEDDA) 반응은 다양한 생체물질, 고분자, 나노물질 복합체의 효율적인 합성에 폭넓게 활용되고 있다. IEDDA는 유기용매에서뿐만 아니라 생리학적 조건 하에서도 우 특이적이며 빠른 반응속도를 가지고 있는 것으로 알려져 있다. 이러한 특성으로 인해 본 반응은 다양한 생물학적 활성을 가지는 물질의 방사성동위원소 표지와 분자영상 및 질병 치료를 위한 방사성의약품 개발에도 활발히 응용되고 있다. 본 리뷰 논문은 IEDDA 반응을 방사화학 및 핵의학 분야에서 이용한 최근 연구 동향 및 연구 결과 그리고 향후 전망에 대해 소개하고자 한다. Inverse electron-demand Diels-Alder reactions (IEDDA) between tetrazine derivatives and strained dienophiles have attracted a lot of attention for the efficient conjugation of biomolecules, polymers, and nanomaterials. Excellent specificity, exceptionally fast reaction rate, and biocompatibility are key features of IEDDA. Therefore, it has also been applied to the development of new labeling methods using several radioisotopes and development of radiotracers to carry out various nuclear imaging as well as therapeutic studies. The purpose of this review is to introduce the reader to the recent advances and applications of IEDDA in the fields of radiochemistry and nuclear medicine.
Sajid Mushtaq,최대성,전종호 대한방사성의약품학회 2017 Journal of radiopharmaceuticals and molecular prob Vol.3 No.1
Herein we report an efficient radiolabeling method based on a rapid condensation reaction between N-terminal cysteine and 2-cyanobenzothiazole (CBT). Radioiodination of 2-cyano-6-hydroxybenzothiazole 2 was carried out using chloramine-T to give 125I-labeled CBT ([125I]1) with a high radiochemical yield (90±6% isolated yield, n=3) and radiochemical purity (>99%). To evaluate the radiolabeling efficiency of 125I-labeled CBT, model compounds, L-cysteine and N-terminal cysteine conjugated cRGD peptide were reacted with [125I]1 under mild conditions. The radiolabeling reactions rapidly provided the 125I-labeled products [125I]5 and [125I]6 with excellent radiochemical yields and radiochemical purity. Therefore, we demonstrate that [125I]1 will be a useful prosthetic group for radioactive iodine labeling of N-terminal cysteine bearing biomolecules. J Radiopharm Mol Probes 3(1):44-51, 2017
Mushtaq, Sajid,Choi, Dae Seong,Jeon, Jongho Korean Society of Radiopharmaceuticals and Molecul 2017 Journal of radiopharmaceuticals and molecular prob Vol.3 No.1
Herein we report an efficient radiolabeling method based on a rapid condensation reaction between N-terminal cysteine and 2-cyanobenzothiazole (CBT). Radioiodination of 2-cyano-6-hydroxybenzothiazole 2 was carried out using chloramine-T to give $^{125}I$-labeled CBT ([$^{125}I$]1) with a high radiochemical yield ($90{\pm}6%$ isolated yield, n=3) and radiochemical purity (>99%). To evaluate the radiolabeling efficiency of $^{125}I$-labeled CBT, model compounds, L-cysteine and N-terminal cysteine conjugated cRGD peptide were reacted with [$^{125}I$]1 under mild conditions. The radiolabeling reactions rapidly provided the $^{125}I$-labeled products [$^{125}I$]5 and [$^{125}I$]6 with excellent radiochemical yields and radiochemical purity. Therefore, we demonstrate that [$^{125}I$]1 will be a useful prosthetic group for radioactive iodine labeling of N-terminal cysteine bearing biomolecules.
박상현,( Sajid Mushtaq ),심하은,전종호,최대성 한국공업화학회 2018 한국공업화학회 연구논문 초록집 Vol.2018 No.0
Synthsis of <sup>99m</sup>Tc-based radiotracer and its biological evaluation were accomplished for an apoptosis imaging used for the efficacy evaluation of drugs as well as the early detection of cancer. In this study <sup>99m</sup>Tc-ML-10 derivative was designed and synthesized with high radiochemical yield (84%) and radiochemical purity (>99%). The radiotracer showed excellent in vitro stability for more than 12 h in mouse serum under ambient conditions. And it was intravenously injected to healthy ICR male mice for the bioditritibtion study and apoptosis was detected in the testes of the mice. The biodistribution study revealed that the radiotracer was accumlated in the testes three times higher than muscle tissue. And it showed fast blood clearance via kidneys.