整合素αvβ3在肿瘤内皮血管细胞表面特异性表达,是肿瘤靶向的一个重要位点.精氨酸-甘氨酸-天冬氨酸(Arg-Gly-Asp,RGD)三肽序列对αvβ3有很强亲和力,RGD 可以作为αvβ3的受体识别.HPMA具有良好的水溶性、生物相容性,与抗癌药物连接为水溶性高分子聚合物后,利用增强渗透和滞留效应,能改善抗癌药物的体内分布和药代动力学.然而单体 RGD多肽有很多缺陷,需要进一步修饰.将 HPMA-RGD共轭可用于靶向肿瘤血管再生,增加药物在肿瘤的浓度和累积量.核磁共振(MRI)是肿瘤诊断的重要手段,用放射性核素Gd等标记的RGD多肽,可用于肿瘤的无创性检查.%The specific expression of integrin alpha v beta 3 on the surface of tumor vascular endothe-lial cell,is an important site of tumor targeting.three peptide sequences with arginine,glycine,and as-partic acid (Arg-Gly-Asp,RGD)have strong affinity with alpha v beta 3.RGD can be used as receptor recognition of alpha v beta 3.On the other hand,HPMA has good water solubility and biocompatibility when it is connected with anticancer drugs.Then,it may be connected into a water soluble polymer.By utilizing enhanced permeability and retention effect,it can improve the anticancer drug distribution in vivo and pharmacokinetics.However,the monomer of RGD peptide has many defects,which need to be further modified.The HPMA-RGD conj ugate could be used to target tumor angiogenesis and in-crease both drug concentration and accumulation in tumor.Surely,nuclear magnetic resonance (MRI) is an important method for tumor diagnosis.Therefore,RGD peptide and radionuclide with Gd markers can be used noninvasive inspection for tumor.
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