| CXCR4拮抗剂在肿瘤治疗中的应用 |
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| 引用本文： | 罗竞红,郭芝刚,曾军.CXCR4拮抗剂在肿瘤治疗中的应用[J].成都大学学报(自然科学版),2012,31(4):309-315. |
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| 作者姓名： | 罗竞红 郭芝刚 曾军 |
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| 作者单位： | 1. 成都大学城乡建设学院,四川成都,610106
2. 广州医学院基础学院,广东广州,510182 |
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| 摘 要： | G蛋白偶联趋化因子受体CXCR4在癌细胞表面广泛表达,癌细胞易转移部位的基质细胞组成型分泌CXCR4的配体——基质细胞衍生因子-1(SDF-1/CXCL12),表达CXCR4的癌细胞在CXCR4/CXCL12轴的调控下沿CXCL12浓度梯度进行转运和归巢,转移的癌细胞在CXCL12作用下与基质细胞紧密联系而获得药物抗性.CXCR4的拮抗剂,比如AMD3100,T140类似物和本课题组开发的SDF-1βP2G,能打断癌细胞与基质细胞的相互作用,动员癌细胞离开对其具保护作用的微环境从而进入血液循环系统,使癌细胞对传统药物的敏感性增加.因此,靶向CXCR4/CXCL12轴的CXCR4拮抗剂联合化疗在探索肿瘤患者治疗方面是一个新颖的,富有吸引力的方法.
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| 关 键 词： | CXCR 拮抗剂 肿瘤治疗 |
Application of CXCR4 Antagonists in Oncotherapy |
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| LUO Jinghong,GUO Zhigang,ZENG Jun.Application of CXCR4 Antagonists in Oncotherapy[J].Journal of Chengdu University (Natural Science),2012,31(4):309-315. |
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| Authors: | LUO Jinghong GUO Zhigang ZENG Jun |
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| Institution: | 1.School of Industrial Manufacturing,Chengdu University,Chengdu 610106,China;2.School of Basic Medicine,Guangzhou Medical College,Guangzhou 510182,China) |
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| Abstract: | CXCR4,a seven-transmembrane G-protein-coupled chemokine receptor,is expressed heavily in cancer cells.Stromal cells in which cancer cell metastasizes keep releasing a ligand for CXCR4,stromal cell-derived factor-1(SDF-1/CXCL12).Cancer cells expressing CXCR4 transfer and home along a gradient of the CXCL12.CXCL12 facilitates tight adhesion of cancer cells with stromal cells,which leads to drug resistance.CXCR4 antagonists,such as SDF-1βP2G developed by this lab,Plerixafor(AMD3100) and T140 analogs alike,can disrupt adhesive tumor-stroma interactions and mobilize cancer cells from their protective stromal microenvironment,making them more exposed to conventional anti-cancer drugs.Therefore,targeting the CXCR4-CXCL12 axis may be a novel and potential therapeutic approach in current clinical trials for tumor patients. |
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| Keywords: | CXCR4 antagonist oncotherapy |
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