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肿瘤微环境响应性小分子诊断治疗抗肿瘤前药研究进展
引用本文:卢晓林,郑莹,邱洋,周湘,陆涛. 肿瘤微环境响应性小分子诊断治疗抗肿瘤前药研究进展[J]. 中国药科大学学报, 2016, 47(6): 629-638
作者姓名:卢晓林  郑莹  邱洋  周湘  陆涛
作者单位:中国药科大学有机化学教研室,中国药科大学有机化学教研室,中国药科大学有机化学教研室,中国药科大学有机化学教研室,中国药科大学有机化学教研室
基金项目:国家自然科学青年基金资助项目(No.81102318/H3001)
摘    要:诊断治疗学(theranostics)是把诊断和治疗结合起来,同时实现影像诊断与治疗的效果。为了提高抗肿瘤药物的安全性及靶向性,诊断治疗药物作为一种新型的治疗策略,具有良好的应用前景,该策略能有效提高药物的生物利用度及靶向性从而提高抗肿瘤活性并降低其毒性。在诊断治疗学中,诊断的作用在于收集治疗前后疾病状态的信息并指导进一步用药。肿瘤组织微环境相对于正常组织存在着很大的差异,主要包括微酸性、过度表达的各种酶、低氧等。本文对利用荧光成像技术进行诊断治疗的肿瘤微环境响应性的小分子抗肿瘤药物的研究进展进行综述。

关 键 词:肿瘤;诊断治疗;荧光;小分子前药

Small conjugate-based theranostic agents:a tumour microenvironment responsive approach for cancer therapy
LU Xiaolin,ZHENG Ying,QIU Yang,ZHOU Xiang and LU Tao. Small conjugate-based theranostic agents:a tumour microenvironment responsive approach for cancer therapy[J]. Journal of China Pharmaceutical University, 2016, 47(6): 629-638
Authors:LU Xiaolin  ZHENG Ying  QIU Yang  ZHOU Xiang  LU Tao
Abstract:Theranostics, combining therapy and diagnosis, is an appealing approach for chemotherapy in medicine which exhibits improved biodistribution, selective cancer targeting ability, reduced toxicity, masked drug efficacy, and minimum side effects. The role of diagnosis tools in theranostics is to collect the information of the disease state before and after specific treatment. Currently, small conjugate-based systems have received much attention for cancer treatment and diagnosis. Relative to the normal tissues, tumor microenvironment shows great difference, including acidic excessive expression of various enzymes as well as low oxygen. In this review, the latest developments on small conjugate based theranostic agents for tumor treatment and diagnosis using fluorescence were summarized.
Keywords:tumour   theranostic agents   fluorescence   small-conjugate prodrug
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