同位素2025，Vol.38Issue(3)：239-246,8.DOI:10.7538/tws.2024.youxian.042
L-赖氨酸降低放射性标记多肽异二聚体探针68Ga/177Lu-FAP-RGD肾摄取的实验研究
Renal Uptake Blocking Study of Radiolabeled Peptidic Heterodimer 68Ga/177Lu-FAP-RGD by L-lysine
摘要
Abstract
To explore possible mechanisms that might explain the high uptake of peptidic heterodimer 68Ga/177Lu-FAP-RGD in kidneys,we constructed U87MG glioma xenograft models and evaluate the impact of L-lysine on biodistribution of 68Ga/177Lu-FAP-RGD by small animal PET/CT or biodistribution studies.68Ga/177Lu-FAP-RGD demonstrated high radiochemical labeling yield and radiochemical purity,with good stability in saline.The results of PET/CT imaging showed that pre-injection of 20 mg lysine could significantly inhibit the uptake of 68Ga-FAP-RGD in mouse kidneys,in contrast to the control group((9.77±0.94)vs.(6.78±0.77)%ID/g,P<0.05),whereas both groups exhibited similar tumor uptake((5.64±0.60)vs.(6.78±0.77)%ID/g,P=0.38).The biodistribution results indicated that compared with the control group,177Lu-FAP-RGD radioactivity was significantly reduced in mouse kidneys of the lysine injection group((11.15±1.33)vs.(6.44±1.42)%ID/g,P<0.01),while other tissues or organs including the tumor((6.27±1.04)vs.(6.00±0.63)%ID/g,P=0.65)showed insignificant changes.Thus,L-lysine is expected to improve the detection sensitivity of renal lesions by reducing the accumulation of 68Ga-FAP-RGD in the kidneys and serve as a potent agent for renal protection against 177Lu-FAP-RGD induced nephrotoxicity in radionuclide therapy.关键词
放射性标记肽/L-赖氨酸/PET/CT/生物分布Key words
radiolabeled peptide/L-lysine/PET/CT/biodistribution分类
核科学引用本文复制引用
刘克皝,陈蓓,蒋涛,胡硕..L-赖氨酸降低放射性标记多肽异二聚体探针68Ga/177Lu-FAP-RGD肾摄取的实验研究[J].同位素,2025,38(3):239-246,8.基金项目
湖南省科技创新计划项目(2021RC4056) （2021RC4056）
