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靶向纤溶酶原激活物抑制剂1的肿瘤治疗研究进展
引用本文:刘吉昊,唐述志,胡立宏,黄明东,陈卓.靶向纤溶酶原激活物抑制剂1的肿瘤治疗研究进展[J].生物化学与生物物理进展,2019,46(7):663-672.
作者姓名:刘吉昊  唐述志  胡立宏  黄明东  陈卓
作者单位:中国科学院福建物质结构研究所结构化学国家重点实验室,福州 350002;中国科学院大学,北京 100049,中国科学院福建物质结构研究所结构化学国家重点实验室,福州 350002;中国科学院大学,北京 100049,中国科学院上海药物研究所,上海 201203,福州大学化学学院,福州 350116,中国科学院福建物质结构研究所结构化学国家重点实验室,福州 350002;中国科学院大学,北京 100049
基金项目:科技部重点专项(2017YFE0103200),国家自然科学基金(31370737, 81572944),中国科学院国家外国专家局创新国际团队项目和福建省引进高层次创业创新人才项目(闽委人才[2018]8-1)资助.
摘    要:肿瘤是严重危害人类健康的疾病.研究表明,实体瘤周围环境中的胞外基质蛋白、浸润性免疫细胞和间充质细胞分泌的蛋白质组等均与肿瘤的发生、发展以及肿瘤治疗的耐受性等密切相关.肿瘤微环境中一个重要调控因子,纤溶酶原激活物抑制剂1 (plasminogen activator inhibitor-1,PAI-1),不仅与组织型纤溶酶原激活物(tissue-type plasminogen activators,tPA)构成调节纤溶活性的一对关键物质,而且参与肿瘤的侵袭、浸润和转移等多个环节并扮演重要角色.本文针对近年来PAI-1的结构和功能方面研究新进展及其与肿瘤微环境的相关性进行综述,并提出PAI-1可作为抗肿瘤治疗的重要靶点.同时,本文也分析了PAI-1抑制剂对肿瘤干预的研究现状,指出PAI-1抑制剂对肿瘤治疗的潜在应用价值.

关 键 词:肿瘤治疗  纤溶酶原激活物抑制剂1  肿瘤微环境
收稿时间:2019/1/17 0:00:00
修稿时间:2019/5/21 0:00:00

Research Progress in Tumor Therapy Targeting Plasminogen Activator Inhibitor-1
LIU Ji-Hao,TANG Shu-Zhi,HU Li-Hong,HUANG Ming-Dong and CHEN Zhuo.Research Progress in Tumor Therapy Targeting Plasminogen Activator Inhibitor-1[J].Progress In Biochemistry and Biophysics,2019,46(7):663-672.
Authors:LIU Ji-Hao  TANG Shu-Zhi  HU Li-Hong  HUANG Ming-Dong and CHEN Zhuo
Institution:State Key Laboratory of Structural Chemistry, Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences, Fuzhou 350002, China; University of Chinese Academy of Sciences, Beijing 100049, China,State Key Laboratory of Structural Chemistry, Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences, Fuzhou 350002, China; University of Chinese Academy of Sciences, Beijing 100049, China,Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China,College of Chemistry, Fuzhou University, Fuzhou 350116, China,State Key Laboratory of Structural Chemistry, Fujian Institute of Research on the Structure of Matter, Chinese Academy of Sciences, Fuzhou 350002, China; University of Chinese Academy of Sciences, Beijing 100049, China
Abstract:Cancer is a serious disease that endangers human health. Solid tumors are surrounded by extracellular matrix, infiltrated immune cells, and the secretum of surrounding mesenchymal cells. The tumor microenvironment plays a key role in tumorigenesis, tumor growth, and resistance to antineoplastic therapy. Plasminogen activator inhibitor-1 (PAI-1) is an important regulatory factor in tumor microenvironment. PAI-1 not only functions as a key constitution with tissue-type plasminogen activators (tPA) in regulating fibrinolytic activity, but also participates in invasion, infiltration and migration of tumor. In this paper, the structure and function of PAI-1 and its significance in tumor microenvironment in recent years are reviewed. It is considered that PAI-1 may be an important target for anti-cancer therapy. At the same time, the latest research results of PAI-1 inhibitors in the field of anticancer were analyzed, and the potential application value of PAI-1 inhibitors was demonstrated.
Keywords:tumor therapy  plasminogen activator inhibitor -1  tumor microenvironment
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