Cancer cells reprogram their gene expression to promote growth,survival,proliferation,and invasiveness.The unique expression of certain uptake transporters in cancers and their innate function to concentrate small mol...Cancer cells reprogram their gene expression to promote growth,survival,proliferation,and invasiveness.The unique expression of certain uptake transporters in cancers and their innate function to concentrate small molecular substrates in cells make them ideal targets for selective delivering imaging and therapeutic agents into cancer cells.In this review,we focus on several solute carrier(SLC)transporters known to be involved in transporting clinically used radiopharmaceutical agents into cancer cells,including the sodium/iodine symporter(NIS),norepinephrine transporter(NET),glucose transporter 1(GLUT1),and monocarboxylate transporters(MCTs).The molecular and functional characteristics of these transporters are reviewed with special emphasis on their specific expressions in cancers and interaction with imaging or theranostic agents[e.g.,Ⅰ-123,Ⅰ-131,123Ⅰ-iobenguane(mIBG),18F-fluorodeoxyglucose(18F-FDG)and 13C pyruvate].Current clinical applications and research areas of these transporters in cancer diagnosis and treatment are discussed.Finally,we offer our views on emerging opportunities and challenges in targeting transporters for cancer imaging and treatment.By analyzing the few clinically successful examples,we hope much interest can be garnered in cancer research towards uptake transporters and their potential applications in cancer diagnosis and treatment.展开更多
BACKGROUND Incidentally found thyroid tumor(thyroid incidentaloma,TI)on F-18 fluorodeoxyglucose(FDG)positron emission tomography-computed tomography(PETCT)is reported in 2.5%-5%of patients being investigated for non-t...BACKGROUND Incidentally found thyroid tumor(thyroid incidentaloma,TI)on F-18 fluorodeoxyglucose(FDG)positron emission tomography-computed tomography(PETCT)is reported in 2.5%-5%of patients being investigated for non-thyroid purposes.Up to 50%of these cases have been diagnosed to be malignant by cytological/histological results.Ultrasonography(US)and fine-needle aspiration cytology are recommended for thyroid nodules with high FDG uptake(hypermetabolism)that are 1 cm or greater in size.It is important to accurately determine whether a suspicious hypermetabolic TI is malignant or benign.AIM To distinguish malignant hypermetabolic TIs from benign disease by analyzing F-18 FDG PET-CT parameters and to identify a cut-off value.METHODS Totally,12761 images of patients who underwent F-18 FDG PET-CT for nonthyroid purposes at our hospital between January 2016 and December 2020 were retrospectively reviewed,and 339 patients[185 men(mean age:68±11.2)and 154 women(mean age:63±15.0)]were found to have abnormal,either focal or diffuse,thyroid FDG uptake.After a thorough review of their medical records,US,and cytological/histological reports,46 eligible patients with focal hypermetabolic TI were included in this study.The TIs were categorized as malignant and benign according to the cytological/histological reports,and four PET parameters[standardized uptake value(SUV)max,SUV_(peak),SUV_(mean),and metabolic tumor volume(MTV)]were measured on FDG PET-CT.Total lesion glycolysis(TLG)was calculated by multiplying the SUV_(mean) by MTV.Both parametric and non-parametric methods were used to compare the five parameters between malignant and benign lesions.Receiver operating characteristic(ROC)curve analysis was performed to identify a cut-off value.RESULTS Each of the 46 patients[12 men(26.1%;mean age:62±13.1 years)and 34 women(73.9%;mean age:60±12.0 years)]with focal hypermetabolic TIs had one focal hypermetabolic TI.Among them,26(56.5%)were malignant and 20(43.5%)were benign.SUV_(max),SUV_(peak),SUV_(mean),and TLG were all hig展开更多
目的探讨甲状腺功能减退(甲减)和甲状腺功能亢进(甲亢)患者治疗前后摄碘率(RAIU)与甲状腺钠/碘同向转运体抗原(NIS-Ag)、甲状腺过氧化物酶(TPO)含量变化的相关性。方法选取2015年2月—2016年8月濮阳市安阳地区医院36例健康体检人员和10...目的探讨甲状腺功能减退(甲减)和甲状腺功能亢进(甲亢)患者治疗前后摄碘率(RAIU)与甲状腺钠/碘同向转运体抗原(NIS-Ag)、甲状腺过氧化物酶(TPO)含量变化的相关性。方法选取2015年2月—2016年8月濮阳市安阳地区医院36例健康体检人员和108例甲状腺疾病就诊患者做为研究对象。电化学发光法检测血清中游离三碘甲状腺素原氨酸(FT3)、游离甲状腺素原氨酸(FT4)和促甲状腺激素(TSH)含量。用甲状腺摄碘功能仪分别检测各组的3 h RAIU、24 h RAIU,用酶联免疫吸附试验测定血浆中NIS-Ag、TPO含量,比较各组别RAIU、NIS-Ag、TPO含量,并分析患者药物治疗前后RAIU与NIS-Ag、TPO相关性。结果FT3、FT4、TSH含量,除甲减摄碘率增高组和减低组之间比较无差异外,其余各组含量比较,差异有统计学意义(均P<0.05)。甲减摄碘率增高组和减低组FT3、FT4含量最低,TSH最高;甲亢组FT3、FT4含量最高,TSH最低。各组治疗前3 h RAIU、24 h RAIU、NIS-Ag及TPO含量比较,差异有统计学意义(P<0.05)。24 h RAIU、3 h RAIU、NIS-Ag及TPO在甲减甲状腺摄碘率减低组中最低,而在甲亢组中最高。各患病组3 h RAIU、24 hRAIU与NIS-Ag、TPO均呈正相关,差异有统计学意义(P<0.05),但在正常组该指标间无相关性(P>0.05)。各组治疗后24 h RAIU、3 h RAIU、NIS-Ag及TPO值均较治疗前降低,差异有统计学意义(P<0.05)。各患病组治疗后3 h RAIU、24 h RAIU与NIS-Ag、TPO均呈正相关,差异有统计学意义(P<0.05)。结论甲减患者和甲亢患者RAIU与NIS-Ag、TPO存在正相关性;药物治疗能降低RAIU、NIS-Ag及TPO。展开更多
基金supported by the National Institutes of Health(NIH)National Institute of General Medical Sciences(Grant R01 GM066233,USA).
文摘Cancer cells reprogram their gene expression to promote growth,survival,proliferation,and invasiveness.The unique expression of certain uptake transporters in cancers and their innate function to concentrate small molecular substrates in cells make them ideal targets for selective delivering imaging and therapeutic agents into cancer cells.In this review,we focus on several solute carrier(SLC)transporters known to be involved in transporting clinically used radiopharmaceutical agents into cancer cells,including the sodium/iodine symporter(NIS),norepinephrine transporter(NET),glucose transporter 1(GLUT1),and monocarboxylate transporters(MCTs).The molecular and functional characteristics of these transporters are reviewed with special emphasis on their specific expressions in cancers and interaction with imaging or theranostic agents[e.g.,Ⅰ-123,Ⅰ-131,123Ⅰ-iobenguane(mIBG),18F-fluorodeoxyglucose(18F-FDG)and 13C pyruvate].Current clinical applications and research areas of these transporters in cancer diagnosis and treatment are discussed.Finally,we offer our views on emerging opportunities and challenges in targeting transporters for cancer imaging and treatment.By analyzing the few clinically successful examples,we hope much interest can be garnered in cancer research towards uptake transporters and their potential applications in cancer diagnosis and treatment.
文摘BACKGROUND Incidentally found thyroid tumor(thyroid incidentaloma,TI)on F-18 fluorodeoxyglucose(FDG)positron emission tomography-computed tomography(PETCT)is reported in 2.5%-5%of patients being investigated for non-thyroid purposes.Up to 50%of these cases have been diagnosed to be malignant by cytological/histological results.Ultrasonography(US)and fine-needle aspiration cytology are recommended for thyroid nodules with high FDG uptake(hypermetabolism)that are 1 cm or greater in size.It is important to accurately determine whether a suspicious hypermetabolic TI is malignant or benign.AIM To distinguish malignant hypermetabolic TIs from benign disease by analyzing F-18 FDG PET-CT parameters and to identify a cut-off value.METHODS Totally,12761 images of patients who underwent F-18 FDG PET-CT for nonthyroid purposes at our hospital between January 2016 and December 2020 were retrospectively reviewed,and 339 patients[185 men(mean age:68±11.2)and 154 women(mean age:63±15.0)]were found to have abnormal,either focal or diffuse,thyroid FDG uptake.After a thorough review of their medical records,US,and cytological/histological reports,46 eligible patients with focal hypermetabolic TI were included in this study.The TIs were categorized as malignant and benign according to the cytological/histological reports,and four PET parameters[standardized uptake value(SUV)max,SUV_(peak),SUV_(mean),and metabolic tumor volume(MTV)]were measured on FDG PET-CT.Total lesion glycolysis(TLG)was calculated by multiplying the SUV_(mean) by MTV.Both parametric and non-parametric methods were used to compare the five parameters between malignant and benign lesions.Receiver operating characteristic(ROC)curve analysis was performed to identify a cut-off value.RESULTS Each of the 46 patients[12 men(26.1%;mean age:62±13.1 years)and 34 women(73.9%;mean age:60±12.0 years)]with focal hypermetabolic TIs had one focal hypermetabolic TI.Among them,26(56.5%)were malignant and 20(43.5%)were benign.SUV_(max),SUV_(peak),SUV_(mean),and TLG were all hig
文摘目的探讨甲状腺功能减退(甲减)和甲状腺功能亢进(甲亢)患者治疗前后摄碘率(RAIU)与甲状腺钠/碘同向转运体抗原(NIS-Ag)、甲状腺过氧化物酶(TPO)含量变化的相关性。方法选取2015年2月—2016年8月濮阳市安阳地区医院36例健康体检人员和108例甲状腺疾病就诊患者做为研究对象。电化学发光法检测血清中游离三碘甲状腺素原氨酸(FT3)、游离甲状腺素原氨酸(FT4)和促甲状腺激素(TSH)含量。用甲状腺摄碘功能仪分别检测各组的3 h RAIU、24 h RAIU,用酶联免疫吸附试验测定血浆中NIS-Ag、TPO含量,比较各组别RAIU、NIS-Ag、TPO含量,并分析患者药物治疗前后RAIU与NIS-Ag、TPO相关性。结果FT3、FT4、TSH含量,除甲减摄碘率增高组和减低组之间比较无差异外,其余各组含量比较,差异有统计学意义(均P<0.05)。甲减摄碘率增高组和减低组FT3、FT4含量最低,TSH最高;甲亢组FT3、FT4含量最高,TSH最低。各组治疗前3 h RAIU、24 h RAIU、NIS-Ag及TPO含量比较,差异有统计学意义(P<0.05)。24 h RAIU、3 h RAIU、NIS-Ag及TPO在甲减甲状腺摄碘率减低组中最低,而在甲亢组中最高。各患病组3 h RAIU、24 hRAIU与NIS-Ag、TPO均呈正相关,差异有统计学意义(P<0.05),但在正常组该指标间无相关性(P>0.05)。各组治疗后24 h RAIU、3 h RAIU、NIS-Ag及TPO值均较治疗前降低,差异有统计学意义(P<0.05)。各患病组治疗后3 h RAIU、24 h RAIU与NIS-Ag、TPO均呈正相关,差异有统计学意义(P<0.05)。结论甲减患者和甲亢患者RAIU与NIS-Ag、TPO存在正相关性;药物治疗能降低RAIU、NIS-Ag及TPO。