【摘 要】
:
In recent years,fibroblast activation protein(FAP)has emerged as an attractive target for the diag-nosis and radiotherapy of cancers using FAP-specific radioligands.Herein,we aimed to design a novel 18F-labeled FAP tracer([18F]A1F-P-FAPI)for FAP imaging a
【机 构】
:
Department of Nuclear Medicine,Nanfang Hospital,Southern Medical University,Guangzhou 510515,China;S
论文部分内容阅读
In recent years,fibroblast activation protein(FAP)has emerged as an attractive target for the diag-nosis and radiotherapy of cancers using FAP-specific radioligands.Herein,we aimed to design a novel 18F-labeled FAP tracer([18F]A1F-P-FAPI)for FAP imaging and evaluated its potential for clinical application.The[18F]A1F-P-FAPI novel tracer was prepared in an automated manner within 42 min with a non-decay cor-rected radiochemical yield of 32±6%(n=8).Among A549-FAP cells,[1 8F]A1F-P-FAPI demonstrated spe-cific uptake,rapid internalization,and low cellular efflux.Compared to the patent tracer[18F]FAPI-42,[18F]A1F-P-FAPI exhibited lower levels of cellular efflux in the A549-FAP cells and higher stability in vivo.Micro-PET imaging in the A549-FAP tumor model indicated higher specific tumor uptake of[18F]A1F-P-FAPI(7.0±1.0%ID/g)compared to patent tracers[18F]FAPI-42(3.2±0.6%ID/g)and[68Ga]Ga-FAPI-04(2.7±0.5%ID/g).Furthermore,in an initial diagnostic application in a patient with nasopharyngeal cancer,[18F]A1F-P-FAPI and[18F]FDG PET/CT showed comparable results for both primary tumors and lymph node metastases.These results suggest that[18F]A1F-P-FAPI can be conveniently prepared,with promising charac-teristics in the preclinical evaluation.The feasibility of FAP imaging was demonstrated using PET studies.
其他文献
Tyrosine-decahydrofluorene derivatives feature a fused[6.5.6]tricarbocyclic core and a 13-membered para-cyclophane ether.Herein,we identified new xenoacremones A,B,and C(1-3)from the fungal strain Xenoacremonium sinensis ML-31 and elucidated their biosynt
Heart aging is characterized by structural and diastolic dysfunction of the heart.However,there is still no effective drug to prevent and treat the abnormal changes in cardiac function caused by aging.Here,we present the preventive effects of emodin and i
Panax notoginseng,a traditional Chinese medicine,exerts beneficial effect on diabetic kidney disease(DKD),but its mechanism is not well clarified.In this study we investigated the effects of ginsenoside Rb1(Rb1),the main active ingredients of Panax notogi
Acute lung injury(ALI)and its severe form acute respiratory distress syndrome(ARDS)are known as the common causes of respiratory failure in critically ill patients.Myeloid differentiation 2(MD2),a co-receptor of toll like receptor 4(TLR4),plays an importa
目的:观察荭草苷通过Notch通路对心律失常大鼠的改善作用及对心电图(ECG)的影响.方法:采用舌下注射乌头碱方式建立心律失常大鼠模型,随机分为模型组、荭草苷低剂量组(0.75 mg· kg-1)、荭草苷中剂量组(1.5 mg·kg-1)、荭草苷高剂量组(3 mg·kg-1),另设对照组.干预后监测ECG,比较心率(HR)、Q-T间期、P-R间期、QRS波群时间及室性早搏(PVC)、室性心动过速(VT)、心室颤动(VF)发生时间;HE染色观察心肌组织病理学变化;TUNEL染色观察心肌细胞凋亡情况;比较心肌
Emerging evidence shows that chronic inflammation mediated by toll-like receptors(TLRs)contributes to diabetic nephropathy.Myeloid differentiation primary-response protein-88(MyD88)is an essential adapter protein of all TLRs except TLR3 in innate immunity
Vascular calcification(VC)is characterized by pathological depositions of calcium and phosphate in the arteries and veins via an active cell-regulated process,in which vascular smooth muscle cells(VSMCs)transform into osteoblast/chondrocyte-like cells as
目的:建立以土大黄苷为标志性成分的保健食品中非法添加伪品大黄及其提取物的UPLC-QTRAP-MS/MS的分析方法.方法:样品用甲醇经超声提取,经Agilent InfinityLab Poroshell 120 SB-Cl8色谱柱(100mm×2.1 mm,2.7μm)分离,以5 mmol·L-1甲酸铵水溶液和乙腈作为流动相,进行梯度洗脱,在负离子扫描模式下,采用MRM-IDA-EPI模式检测.结果:土大黄苷质量浓度在5~100 ng·mL-1范围内线性均良好.相关系数(r2)为0.9987.土大黄苷在
Accumulating evidence indicates that mitochondrial dysfunction and oxidative stress play a pivotal role in the initiation and progression of nonalcoholic fatty liver disease(NAFLD).In this study,we found that blueberry-derived exosomes-like nanoparticles(
Transforming growth factor β(TGF-β)is a multifunctional polypeptide that plays critical roles in regulating a broad range of cellular functions and physiological processes.TGF-β signalling dysfunction contributes to many disorders,such as cardiovascular d