https://scholars.lib.ntu.edu.tw/handle/123456789/611888
標題: | Rational Design, Pharmacomodulation, and Synthesis of [68Ga]Ga-Alb-FAPtp-01, a Selective Tumor-Associated Fibroblast Activation Protein Tracer for PET Imaging of Glioma | 作者: | Lin, Jia-Jia Chuang, Chia-Pao Lin, Jia-Yu FENG-TING HUANG Huang, Chiun-Wei |
關鍵字: | FAP;FAPI-04;gallium-68;glioblastoma;PET/CT imaging | 公開日期: | 24-九月-2021 | 出版社: | American Chemical Society | 卷: | 6 | 期: | 9 | 起(迄)頁: | 3424-3435 | 來源出版物: | ACS Sensors | 摘要: | Dynamic changes in the tumor-associated fibroblast activation protein (FAP) expression in tumors of different stages may be helpful for prognostic evaluation and treatment response monitoring, making this protein a promising surveillance biomarker for timely diagnosis of malignant tumors and effective planning of patient care. To prospectively verify the diagnostic efficacy value of the developed FAP tracers, [68Ga]Ga-FAPtp and [68Ga]Ga-Alb-FAPtp-01, dynamic/static positron emission tomography (PET)/computed tomography scans were acquired for tumor-targeting studiesin vivoand in comparison with the well-established clinically used tracer [68Ga]Ga-FAPI-04. The optimized rationally designed FAP-targeting PET tracer, [68Ga]Ga-Alb-FAPtp-01, with albumin-binding capability demonstrated prominent tumor uptake over time. The mean standard uptake value (SUV) and the tumor/muscle (T/M) ratio were as high as 1.775 ± 0.179 SUV and T/M = 5.9, 1.533 ± 0.222 SUV and T/M = 6.7, and 1.425 ± 0.204 SUV and T/M = 9.5, respectively, at 1, 2, and 3 h. Its improved tumor uptake and pharmacokinetics suggest that the [68Ga]Ga-Alb-FAPtp-01 tracer can noninvasively detect FAP activationin vivo, permitting a precise definition of its roles in tumors of different stages and yielding insights regarding FAP-targeted radiotherapeutic strategies at the molecular level. |
URI: | https://scholars.lib.ntu.edu.tw/handle/123456789/611888 | ISSN: | 23793694 | DOI: | 10.1021/acssensors.1c01316 |
顯示於: | 生化科技學系 |
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