碳酸酐酶Ⅸ在核医学中的研究进展  

Development of Carbonic Anhydrase Ⅸ in the Nuclear Medicine Research

作　　者：李剑波[1,2] 施玲丽[1,2] 王成[1,2] 李潇[1,2] 贾丽娜[1,2] 张岚[1] 漆玉金[1] 

机构地区：[1]中国科学院上海应用物理研究所,上海201800 [2]中国科学院研究生院,北京100049

出　　处：《同位素》2011年第3期140-145,共6页Journal of Isotopes

基　　金：国家自然科学基金资助项目(10875163)

摘　　要：碳酸酐酶Ⅸ(Carbonic anhydrase Ⅸ,CAⅨ)是碳酸酐酶家族(Carbonic anhydrases,CAs)的异构体之一,在许多肿瘤中过量表达,是一种与肿瘤相关的跨膜糖蛋白。它催化CO2水解为碳酸氢根和氢离子,维持肿瘤细胞内的pH,酸化细胞外环境,有利于肿瘤的生长和转移。在核医学的靶向诊断和治疗中,CAⅨ成为一个抗肿瘤药物的靶向目标,也成为病人病情的一个预后因子。CAⅨ抑制剂可以作为一种诊断药物,用于肿瘤的分子影像;也可以作为一种治疗药物,阻断CAⅨ所调控的通路。利用89Zr1、11In1、24I或125I标记靶向CAⅨ的单克隆抗体或其片段进行分子影像,能精确定位CAⅨ的分布,灵敏检测CAⅨ的表达情况;利用90Y1、31I1、77Lu或186Re标记靶向CAⅨ的单克隆抗体,在放免疫治疗中可有效延迟肿瘤的生长。本文对CAⅨ及其在核医学中的研究进展进行了综述。Carbonic anhydrase Ⅸ（CA Ⅸ）,which is one of carbonic anhydrases（CAs）,is a tumor-associated transmembrane protein.CA Ⅸ is detected in various solid tumors,but little or not in the normal tissues;it catalyzes a reversible conversion of carbon dioxide to bicarbonate and proton,controlling pH of intracellular and extracellular space and maintaining the acid-base balance of tissues in favor of tumor growth and invasion.CA Ⅸ is clearly an attractive target for anti-tumor drugs and also as a prognostic factor of patients in the diagnosis and treatment of tumors.CA Ⅸ inhibitors can be used as diagnostic drugs for molecular imaging of tumors and also be used as anti-tumor drugs for blocking the CA Ⅸ mediated pathway.Molecular imaging using 89Zr,111In,124I or 125I labeled monoclonal antibodies targeting CA Ⅸ can precisely position the distribution and sensitively detect expression of CA Ⅸ.In radioimmunotherapy experiments at maximum tolerated dose,tumor growth was effectively delayed by monoclonal antibodies targeting CA Ⅸ labeled with 90Y,131I,177Lu or 186Re.This review focused on the presentation of CA Ⅸ and its applications in the nuclear medicine research.

关 键 词：碳酸酐酶Ⅸ 抑制剂 核医学 研究进展 

分 类 号：R817[医药卫生—影像医学与核医学]