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肿瘤的发病率和病死率呈逐年上升趋势,近30年来尽管肿瘤的治疗方案有很大改进,但肿瘤的长期生存率仍然很低,其中多药耐药(multidrug resistance,MDR)是导致化疗失败的主要原因之一。MDR的发生与多种因素有关,目前研究较多的是ATP结合盒(ATP-binding cassette,ABC)转运蛋白,其中已经明确的ABC转运蛋白有48种,这些转运蛋白具有共同的ATP结合域,水解ATP释放能量将药物泵出细胞。活体、无创性观察肿瘤多药耐药成为亟待解决的问题,一些针对P-糖蛋白(P-glycoprotein,P-gp)底物及抑制剂的正电子显像剂不断涌现,成为肿瘤多药耐药研究的热点。
P-gp功能的PET显像剂的研究进展
Progress in PET imaging evaluating of P-gp function
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摘要: 肿瘤对化疗药物产生耐药性是肿瘤治疗失败的主要原因,引起肿瘤对化疗药物耐药的重要机制是ATP结合盒(ABC)转运蛋白的过度表达。P-糖蛋白(P-gp)是ABC转运蛋白超家族中研究最广、最深入的一类转运蛋白,目前检测P-gp主要依赖于组织活检或术后病理组织在体外进行定性、定量分析,这些检测方法受取材技术、肿瘤标本差异等因素的限制,因此,寻找一种无创性、可以动态检测肿瘤多药耐药的方法就显得尤为重要。目前许多18F、11C标记的P-gp底物及抑制剂的正电子显像剂已经进行基础研究,部分进入了临床试验阶段。该文对P-gp的PET显像剂现状进行综述。
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关键词:
- P-糖蛋白 /
- 正电子发射断层显像术 /
- 放射性示踪剂
Abstract: The resistance of malignant tumors to chemotherapy is a major cause of treatment failure. One important mechanism in this resistance is the overexpression of adenosine triphosphate-binding cassette transporters. The best-characterize member of this superfamily of transporters is P-glycoprotein(P-gp). The qualitative and quantitative ananlysis of P-gp mainly depends on the tissue biopsy or postoperative pathologic tissue in vitro. It is important to find a method of noninvasive and dynamic monitoring tumor multidrug resistance. Many positron imaging agent of P-gp substrates and inhibitors have been researched, and part of them have been researched in clinic. In this review, the current status is summarized on PET imaging and P-gp function.-
Key words:
- P-glycoprotein /
- Positron emission tomography /
- Radiotracer
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