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首页> 外文期刊>Cancer Cell >Tissue-penetrating delivery of compounds and nanoparticles into tumors.
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Tissue-penetrating delivery of compounds and nanoparticles into tumors.

机译：化合物和纳米颗粒进入组织的穿透性肿瘤。

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摘要

Poor penetration of drugs into tumors is a major obstacle in tumor treatment. We describe a strategy for peptide-mediated delivery of compounds deep into the tumor parenchyma that uses a tumor-homing peptide, iRGD (CRGDK/RGPD/EC). Intravenously injected compounds coupled to iRGD bound to tumor vessels and spread into the extravascular tumor parenchyma, whereas conventional RGD peptides only delivered the cargo to the blood vessels. iRGD homes to tumors through a three-step process: the RGD motif mediates binding to alphav integrins on tumor endothelium and a proteolytic cleavage then exposes a binding motif for neuropilin-1, which mediates penetration into tissue and cells. Conjugation to iRGD significantly improved the sensitivity of tumor-imaging agents and enhanced the activity of an antitumor drug.
机译：药物难以渗透到肿瘤中是肿瘤治疗的主要障碍。我们描述了使用肿瘤归巢肽iRGD（CRGDK / RGPD / EC）的肽介导的化合物深入肿瘤实质的策略。与iRGD偶联的静脉注射化合物与肿瘤血管结合并扩散到血管外肿瘤实质中，而常规的RGD肽仅将货物递送至血管。 iRGD通过三步过程将其归巢于肿瘤：RGD基序介导与肿瘤内皮上的alphav整合素的结合，然后蛋白水解酶切揭示Neuropilin-1的结合基序，后者介导渗透到组织和细胞中。与iRGD的​​结合显着提高了肿瘤显像剂的敏感性，并增强了抗肿瘤药的活性。

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