Yin Hong, Yang Jie, Zhang Qing, Yang Jie, Wang Haiyu, Xu Jinjing, Zheng Junnian
Cancer Institute, Xuzhou Medical University, Xuzhou, Jiangsu 221002, P.R. China.
Mol Med Rep. 2017 May;15(5):2925-2930. doi: 10.3892/mmr.2017.6419. Epub 2017 Mar 30.
As a tumor-targeting and ‑penetrating peptide, iRGD binds to αv integrins and neuropilin‑1 receptors, which are expressed at high levels on tumor cells and the surfaces of vasculature. Subsequently, iRGD penetrates deep into the tumor parenchyma with antitumor drugs, imaging agents, immune modulators and biological products. These substances are either chemically linked to the peptide or co‑injected with the peptide. The iRGD peptide can be readily synthesized, exhibits significantly improved penetration, compared with traditional peptides, and can effectively inhibit tumor metastasis. Therefore, the peptide is now used widely for the diagnosis and treatment of cancer. However, whether the peptide is able to promote the entry of drugs into non‑targeted cells remains to be fully elucidated. In this review, an overview of iRGD is presented, focusing on its identification, mechanism of action and previous studies on its roles in various types of cancer. Studies in previous years have demonstrated the potential of the iRGD protein for tumors diagnosis and targeted treatment, which warrants further investigation.
作为一种肿瘤靶向和穿透肽,iRGD可与αv整合素和神经纤毛蛋白-1受体结合,这些受体在肿瘤细胞和脉管系统表面高水平表达。随后,iRGD与抗肿瘤药物、成像剂、免疫调节剂和生物制品一起深入渗透到肿瘤实质中。这些物质要么与该肽化学连接,要么与该肽共同注射。iRGD肽易于合成,与传统肽相比,其穿透性显著提高,并且能够有效抑制肿瘤转移。因此,该肽目前被广泛用于癌症的诊断和治疗。然而,该肽是否能够促进药物进入非靶向细胞仍有待充分阐明。在本综述中,对iRGD进行了概述,重点介绍了其鉴定、作用机制以及此前关于其在各类癌症中作用的研究。过去几年的研究已经证明了iRGD蛋白在肿瘤诊断和靶向治疗方面的潜力,这值得进一步研究。