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本文引用的文献

1
The "specific" P-glycoprotein inhibitor Tariquidar is also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2).“特异性”P-糖蛋白抑制剂 Tariquidar 也是乳腺癌耐药蛋白（BCRP/ABCG2）的底物和抑制剂。
ACS Chem Neurosci. 2011 Feb 16;2(2):82-9. doi: 10.1021/cn100078a. Epub 2010 Oct 21.
2
Lysosomal trapping of a radiolabeled substrate of P-glycoprotein as a mechanism for signal amplification in PET.作为 PET 信号放大机制的 P-糖蛋白放射性标记底物的溶酶体捕获。
Proc Natl Acad Sci U S A. 2011 Feb 8;108(6):2593-8. doi: 10.1073/pnas.1014641108. Epub 2011 Jan 24.
3
Revisiting the ABCs of multidrug resistance in cancer chemotherapy.重新审视癌症化疗中多药耐药性的 ABC 问题。
Curr Pharm Biotechnol. 2011 Apr;12(4):570-94. doi: 10.2174/138920111795164048.
4
A pharmacodynamic study of docetaxel in combination with the P-glycoprotein antagonist tariquidar (XR9576) in patients with lung, ovarian, and cervical cancer.多西他赛联合 P-糖蛋白拮抗剂 XR9576 治疗肺癌、卵巢癌和宫颈癌患者的药效学研究。
Clin Cancer Res. 2011 Feb 1;17(3):569-80. doi: 10.1158/1078-0432.CCR-10-1725. Epub 2010 Nov 16.
5
Synthesis and in vivo evaluation of [11C]tariquidar, a positron emission tomography radiotracer based on a third-generation P-glycoprotein inhibitor.基于第三代 P-糖蛋白抑制剂的正电子发射断层扫描放射性示踪剂[11C]tariquidar 的合成及体内评价。
Bioorg Med Chem. 2010 Aug 1;18(15):5489-97. doi: 10.1016/j.bmc.2010.06.057. Epub 2010 Jun 22.
6
Evaluation of limiting brain penetration related to P-glycoprotein and breast cancer resistance protein using [(11)C]GF120918 by PET in mice.采用 [(11)C]GF120918 通过 PET 评估与 P-糖蛋白和乳腺癌耐药蛋白相关的脑穿透限制在小鼠中的作用。
Mol Imaging Biol. 2011 Feb;13(1):152-60. doi: 10.1007/s11307-010-0313-1.
7
Synthesis and evaluation of [11C]XR9576 to assess the function of drug efflux transporters using PET.合成并评估 [11C]XR9576 以使用 PET 评估药物外排转运体的功能。
Ann Nucl Med. 2010 Jun;24(5):403-12. doi: 10.1007/s12149-010-0373-y. Epub 2010 Apr 2.
8
Dose-response assessment of tariquidar and elacridar and regional quantification of P-glycoprotein inhibition at the rat blood-brain barrier using (R)-[(11)C]verapamil PET.利用（R）-[(11)C]维拉帕米 PET 评估 tariquidar 和 elacridar 的剂量反应及对大鼠血脑屏障 P-糖蛋白抑制的区域定量。
Eur J Nucl Med Mol Imaging. 2010 May;37(5):942-53. doi: 10.1007/s00259-009-1332-5. Epub 2009 Dec 17.
9
Synthesis and small-animal positron emission tomography evaluation of [11C]-elacridar as a radiotracer to assess the distribution of P-glycoprotein at the blood-brain barrier.[11C]依拉曲沙作为一种放射性示踪剂用于评估血脑屏障处P-糖蛋白分布的合成及小动物正电子发射断层扫描评估
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10
Imaging the function of P-glycoprotein with radiotracers: pharmacokinetics and in vivo applications.用放射性示踪剂成像P-糖蛋白的功能：药代动力学及体内应用
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一种用于检测表达 P-糖蛋白的鼠乳腺癌的 [11C]tariquidar、[11C]elacridar 和 (R)-[11C]verapamil 的小动物 PET 比较评估。

A comparative small-animal PET evaluation of [11C]tariquidar, [11C]elacridar and (R)-[11C]verapamil for detection of P-glycoprotein-expressing murine breast cancer.

机构信息

Health & Environment Department, Molecular Medicine, AIT Austrian Institute of Technology GmbH, Seibersdorf, Austria.

出版信息

Eur J Nucl Med Mol Imaging. 2012 Jan;39(1):149-59. doi: 10.1007/s00259-011-1941-7. Epub 2011 Oct 8.

DOI:10.1007/s00259-011-1941-7
PMID:21983837
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3684861/
Abstract

PURPOSE

One important mechanism for chemoresistance of tumours is overexpression of the adenosine triphosphate-binding cassette transporter P-glycoprotein (Pgp). Pgp reduces intracellular concentrations of chemotherapeutic drugs. The aim of this study was to compare the suitability of the radiolabelled Pgp inhibitors [(11)C]tariquidar and [(11)C]elacridar with the Pgp substrate radiotracer (R)-[(11)C]verapamil for discriminating tumours expressing low and high levels of Pgp using small-animal PET imaging in a murine breast cancer model.

METHODS

Murine mammary carcinoma cells (EMT6) were continuously exposed to doxorubicin to generate a Pgp-overexpressing, doxorubicin-resistant cell line (EMT6AR1.0 cells). Both cell lines were subcutaneously injected into female athymic nude mice. One week after implantation, animals underwent PET scans with [(11)C]tariquidar (n = 7), [(11)C]elacridar (n = 6) and (R)-[(11)C]verapamil (n = 7), before and after administration of unlabelled tariquidar (15 mg/kg). Pgp expression in tumour grafts was evaluated by Western blotting.

RESULTS

[(11)C]Tariquidar showed significantly higher retention in Pgp-overexpressing EMT6AR1.0 compared with EMT6 tumours: the mean ± SD areas under the time-activity curves in scan 1 from time 0 to 60 min (AUC(0-60)) were 38.8 ± 2.2 min and 25.0 ± 5.3 min (p = 0.016, Wilcoxon matched pairs test). [(11)C]Elacridar and (R)-[(11)C]verapamil were not able to discriminate Pgp expression in tumour models. Following administration of unlabelled tariquidar, both EMT6Ar1.0 and EMT6 tumours showed increases in uptake of [(11)C]tariquidar, [(11)C]elacridar and (R)-[(11)C]verapamil.

CONCLUSION

Among the tested radiotracers, [(11)C]tariquidar performed best in discriminating tumours expressing high and low levels of Pgp. Therefore [(11)C]tariquidar merits further investigation as a PET tracer to assess Pgp expression levels in solid tumours.

摘要

目的

肿瘤产生化学抗性的一个重要机制是过度表达三磷酸腺苷结合盒转运蛋白 P-糖蛋白（Pgp）。Pgp 降低了细胞内化疗药物的浓度。本研究的目的是比较放射性标记的 Pgp 抑制剂 [(11)C]tariquidar 和 [(11)C]elacridar 与 Pgp 底物放射性示踪剂 [(R)-[(11)C]verapamil 的适用性，以使用小动物 PET 成像在鼠乳腺癌模型中区分表达低水平和高水平 Pgp 的肿瘤。

方法

将鼠乳腺癌细胞（EMT6）连续暴露于多柔比星中，以产生 Pgp 过表达、多柔比星耐药细胞系（EMT6AR1.0 细胞）。将这两种细胞系均皮下注射到雌性无胸腺裸鼠体内。在植入后 1 周，动物接受 [(11)C]tariquidar（n = 7）、[(11)C]elacridar（n = 6）和 (R)-[(11)C]verapamil（n = 7）的 PET 扫描，在给予未标记的 tariquidar（15 mg/kg）前后进行。通过 Western 印迹评估肿瘤移植物中的 Pgp 表达。

结果

与 EMT6 肿瘤相比，[(11)C]tariquidar 在过表达 Pgp 的 EMT6AR1.0 中显示出明显更高的保留率：扫描 1 中从时间 0 到 60 分钟的时间-活性曲线下面积（AUC(0-60)）分别为 38.8 ± 2.2 min 和 25.0 ± 5.3 min（p = 0.016，Wilcoxon 配对检验）。[(11)C]elacridar 和 (R)-[(11)C]verapamil 均不能区分肿瘤模型中的 Pgp 表达。给予未标记的 tariquidar 后，EMT6Ar1.0 和 EMT6 肿瘤均显示 [(11)C]tariquidar、[(11)C]elacridar 和 (R)-[(11)C]verapamil 的摄取增加。

结论

在测试的示踪剂中，[(11)C]tariquidar 在区分表达高低水平 Pgp 的肿瘤方面表现最佳。因此，[(11)C]tariquidar 值得进一步研究作为 PET 示踪剂来评估实体瘤中的 Pgp 表达水平。