SPA: a peptide antagonist that acts as a cell-penetrating peptide for drug delivery
SPA: a peptide antagonist that acts as a cell-penetrating peptide for drug delivery
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SPA：一种肽拮抗剂，可作为药物输送的细胞穿透肽
DOI：
10.1080/10717544.2019.1706669
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发表时间：
2019-12
期刊：
影响因子：
6
通讯作者：
Wei Zhang
中科院分区：
文献类型：
--
作者：
Jingjing Song;Sujie Huang;Zhengzheng Zhang;Bo Jia;Huan Xie;Ming Kai;Wei Zhang
摘要尽管细胞穿透肽（CPPs）已被证明是高效的药物转运蛋白，但理想的肿瘤治疗肽载体仍在迫切寻找。肽拮抗剂作为靶向分子由于其与激动剂相比具有高的肿瘤蓄积和抗肿瘤活性而引起了广泛的关注。SPA是P物质的衍生物，是一种具有抗肿瘤活性的强效拮抗剂。基于SPA的氨基酸组成，我们推测它可以像CPP一样跨细胞膜转运。在这项研究中，我们的结果表明，SPA可以进入细胞类似于CPP。SPA作为载体能有效地将喜树碱和质粒导入细胞。此外，我们的研究结果表明，SPA具有低毒性正常细胞和高酶的稳定性。综上所述，我们的结果验证了SPA有效药物递送的能力。更重要的是，我们的研究开辟了一个新的途径，设计理想的CPP肽拮抗剂的基础上。
Abstract Although cell-penetrating peptides (CPPs) has been proven to be efficient transporter for drug delivery, ideal peptide vectors for tumor therapy are still being urgently sought. Peptide antagonists have attracted substantial attention as targeting molecules because of their high tumor accumulation and antitumor activity compared with agonists. SPA, a derivative of substance P, is a potent antagonist that exhibits antitumor activity. Based on the amino acid composition of SPA, we speculate that it can translocate across cell membranes as CPPs do. In this study, our results demonstrated that SPA could enter cells similarly to a CPP. As a vector, SPA could efficiently deliver camptothecin and plasmids into cells. In addition, our results showed that SPA exhibited low toxicity to normal cells and high enzymatic stability. Taken together, our results validated the ability of SPA for efficient drug delivery. More importantly, our study opens a new avenue for designing ideal CPPs based on peptide antagonists.
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DOI：
10.1002/anie.201801361
发表时间：
2018-09-10
期刊：
Angewandte Chemie (International ed. in English)
影响因子：
--
作者：
Peraro L;Kritzer JA
通讯作者：
Kritzer JA
影响因子：
2.7
作者：
Henne, Walter A.;Doorneweerd, Derek D.;Low, Philip S.
通讯作者：
Low, Philip S.
DOI：
10.1016/j.jconrel.2012.05.017
发表时间：
2012-08
期刊：
Journal of controlled release : official journal of the Controlled Release Society
影响因子：
--
作者：
Jan Hoyer;I. Neundorf
通讯作者：
Jan Hoyer;I. Neundorf
影响因子：
11.2
作者：
Papo, N;Braunstein, A;Shai, Y
通讯作者：
Shai, Y
影响因子：
4.8
作者：
Najjar, Kristina;Erazo-Oliveras, Alfredo;Pellois, Jean-Philippe
通讯作者：
Pellois, Jean-Philippe