NRP1 transport of cancer therapeutics mediated by tumor-penetrating peptides.
NRP1 transport of cancer therapeutics mediated by tumor-penetrating peptides.
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DOI：
10.1358/dof.2017.042.02.2564106
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发表时间：
2017-02
影响因子：
0.2
通讯作者：
Mixson AJ
中科院分区：
文献类型：
--
作者：
Leng Q;Woodle MC;Mixson AJ
由于高间质压力，肿瘤通常会抑制低分子量药物的摄取，而由于渗透性和滞留性（EPR）的增强，肿瘤对大分子的摄取会增加。小分子药物单独或合并在纳米颗粒（NP）很大程度上依赖于这种物理肿瘤摄取（被动）的治疗活性。虽然被动靶向NP如隐形脂质体多柔比星（Doxil®）有效且安全性提高，但药物向肿瘤的输送仍然受到明显限制。为了改善肿瘤传递和疗效，肿瘤穿透肽（TPP）含有靶向肿瘤并激活神经匹林-1受体（NRP1）的序列，已与小分子和大分子治疗分子共同给药或偶联。在这篇综述中，我们将讨论以NRP1转运系统为靶点的tpp介导的治疗方法。
Whereas uptake of low molecular weight agents is generally inhibited in tumors due to high interstitial pressure, tumor uptake of macromolecules is increased due to enhanced permeability and retention (EPR). Small molecule drugs alone or incorporated in nanoparticles (NP) have largely been dependent on such physical tumor uptake (passive) for therapeutic activity. Although passive targeted NP such as Stealth Liposomal Doxorubicin (Doxil ®) are effective with improved safety, drug delivery to tumors is still significantly limited. To improve tumor delivery and efficacy, tumor-penetrating peptides (TPP), which contain sequences that target the tumor and activate the neuropilin-1 receptor (NRP1), have either been co-administered with or conjugated to both small and large therapeutic molecules. In this review, we will discuss TPP-mediated therapeutics which target the NRP1 transport system of tumors.