NGR(Asn-Gly-Arg)是通过噬菌体展示技术筛选出来的能够和肿瘤新生血管特异结合的三肽模体,可以通过内皮细胞上的氨肽酶N(aminopeptidase N,亦称CD13)与新生血管发生特异性的结合。NGR多肽可以将多种药物分子和病毒载体靶向运输到肿瘤或者进行血管再生的组织中。NGR模体上的天冬酰胺脱酰胺后生成异天冬氨酸-甘氨酸-精氨酸异构体(isoDGR)。isoDGR是整联蛋白αvβ3的配体,可以作为一种新的肿瘤新生血管靶向肽用于肿瘤靶向治疗的研究。本文主要对NGR模体的结构和功能以及其在肿瘤靶向治疗中的应用作一综述。
NGR (Asn-Gly-Arg) motif exploited by phage display can selectively recognize neovasculature by its binding to an endothelium-associated form of aminopeptidase N (CD13). NGR peptides can be used for ligand-directed targeted delivery of various drugs and viral vectors to tumors or to other tissues with an angiogenesis process. NGR can convert to isoaspartate-glycine-arginine (isoDGR) by asparagine deamidation. isoDGR is a ligand for αvβ3 integrin, which could be used as a new targeting peptide of tumor neovasculature for the study of tumor targeted therapy. The paper reviews the structural and functional properties of the NGR motif and its application in tumor targeted therapy.