整合素αⅤβ3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

doi:10.7538/tws.2010.23.04.0247

摘要/Abstract

摘要： 整合素α_Ⅴβ₃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α_Ⅴβ₃的拮抗剂可特异性结合于整合素α_Ⅴβ₃，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α_Ⅴβ₃非肽类小分子拮抗剂设计中的研究现状为重点，对整合素α_Ⅴβ₃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。

关键词: 整合素α_Ⅴβ₃, RGD肽, 小分子拮抗剂, 肿瘤显像

Abstract: Integrin α_Ⅴβ₃ 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 α_Ⅴβ₃ antagonists which have high specificity and affinity to integrin α_Ⅴβ₃. This article will focus on the current researches on nonpeptide small molecular antagonists of integrin α_Ⅴβ₃ by computerassisted drug design(CADD) to review the nonpeptide antagonists of integrin α_Ⅴβ₃ in present progress. Also, it makes an analysis on the applications of radiolabeled small molecular antagonists as probes in tumor imaging.

Key words: integrin α_Ⅴβ₃, RGD peptide, small molecular antagonists, tumor imaging

李玲;张春丽;王荣福. 整合素α_Ⅴβ₃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[J]. 同位素, 2010, 23(4): 247-252.

LI Ling;ZHANG Chun-li;WANG Rong-fu. Design and Development on Tumor Imaging of Nonpeptide Small Molecular Antagonists of Integrin α_Ⅴβ₃[J]. Journal of Isotopes, 2010, 23(4): 247-252.

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整合素α_Ⅴβ₃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 α_Ⅴβ₃

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