整合素αⅤβ_3非肽类小分子拮抗剂的设计及其在肿瘤显像中的研究进展  

Design and Development on Tumor Imaging of Nonpeptide Small Molecular Antagonists of Integrin αⅤβ_3

作　　者：李玲[1] 张春丽[1] 王荣福[1] 

机构地区：[1]北京大学第一医院核医学科,北京100034

出　　处：《同位素》2010年第4期247-252,共6页Journal of Isotopes

基　　金：国家重点基础研究发展计划基金-973计划(2006CB705705);国家自然科学基金(30870729;30900374)资助;北京大学985II期基金(985-2-056)

摘　　要：整合素αⅤβ3在肿瘤血管生成中发挥着重要的作用,肿瘤血管生成又是肿瘤生长和转移的重要环节,由于整合素αⅤβ3的拮抗剂可特异性结合于整合素αⅤβ3,因此用放射性核素对其拮抗剂进行标记并将其应用于肿瘤的显像和靶向治疗,可达到早期发现和抑制肿瘤转移的作用。本文以计算机辅助药物设计在整合素αⅤβ3非肽类小分子拮抗剂设计中的研究现状为重点,对整合素αⅤβ3非肽类小分子拮抗剂的当前研究进展进行综述,展望小分子拮抗剂在未来肿瘤显像中的应用。Integrin αⅤβ3 is significant to tumor angiogenesis,which is necessary for tumor growth and metastasis.So,it＇s beneficial for us to make noninvasive visualizations and targeted treatments in tumor patients to detect malignant tumors and inhabit tumor metastasis early by using radiolabeled integrin αⅤβ3 antagonists which have high specificity and affinity to integrin αⅤβ3.This article will focus on the current researches on nonpeptide small molecular antagonists of integrin αⅤβ3 by computer-assisted drug design（CADD） to review the nonpeptide antagonists of integrin αⅤβ3 in present progress.Also,it makes an analysis on the applications of radiolabeled small molecular antagonists as probes in tumor imaging.

关 键 词：整合素αⅤβ3 RGD肽 小分子拮抗剂 肿瘤显像 

分 类 号：R817[医药卫生—影像医学与核医学]