Integrin targeted delivery of chemotherapeutics.
Integrin targeted delivery of chemotherapeutics.
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DOI：
10.7150/thno/v01p0189
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发表时间：
2011-02-17
期刊：
影响因子：
12.4
通讯作者：
Chen X
中科院分区：
文献类型：
--
作者：
Chen K;Chen X
化学治疗剂的靶向递送定义为通过将其药理学活性严格定位于作用部位或组织来使化学治疗剂的治疗指数最大化。整合素是一个异二聚体跨膜糖蛋白家族，参与广泛的细胞-细胞外基质（ECM）和细胞-细胞相互作用。整合素作为细胞表面受体，与细胞外配体相互作用，在血管生成、白细胞功能和肿瘤发生发展中起重要作用，是化疗的理想靶点。含有精氨酸-甘氨酸-天冬氨酸（RGD）的肽配体显示出对整合素（特别是整合素αvβ3）的强结合亲和力和选择性，已经开发用于与各种常规化疗剂缀合，例如小分子、肽和蛋白质以及纳米颗粒携带的药物，用于整合素靶向治疗研究。本文综述了近年来整合素靶向化疗药物的研究进展，重点介绍了整合素αvβ3的靶点，并介绍了不同的RGD肽-化疗药物偶联物的设计思路及其主要应用。
Targeted delivery of chemotherapeutics is defined in the sense, that is, to maximize the therapeutic index of a chemotherapeutic agent by strictly localizing its pharmacological activity to the site or tissue of action. Integrins are a family of heterodimeric transmembrane glycoproteins involved in a wide range of cell-to-extracellular matrix (ECM) and cell-to-cell interactions. As cell surface receptors, integrins readily interact with extracellular ligands and play a vital role in angiogenesis, leukocytes function and tumor development, which sets up integrins as an excellent target for chemotherapy treatment. The peptide ligands containing the arginine-glycine-aspartic acid (RGD), which displays a strong binding affinity and selectivity to integrins, particularly to integrin αvβ3, have been developed to conjugate with various conventional chemotherapeutic agents, such as small molecules, peptides and proteins, and nanoparticle-carried drugs for integtrin targeted therapeutic studies. This review highlights the recent advances in integrin targeted delivery of chemotherapeutic agents with emphasis on target of integrin αvβ3, and describes the considerations for the design of the diverse RGD peptide-chemotherapeutics conjugates and their major applications.
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