SPA: a peptide antagonist that acts as a cell-penetrating peptide for drug delivery

Drug Delivery

Ming Kai¹  Sujie Huang¹  Jingjing Song²  Huan Xie²  Zhengzheng Zhang³  Bo Jia³  Wei Zhang³ 

[1] Institute of Biochemistry and Molecular Biology, School of Life Sciences, Lanzhou University, Lanzhou, China;Institute of Pharmacology, Key Laboratory of Preclinical Study for New Drugs of Gansu Province, School of Basic Medical Sciences, Lanzhou University, Lanzhou, China;Institute of Physiology, Key Laboratory of Preclinical Study for New Drugs of Gansu Province, School of Basic Medical Sciences, Lanzhou University, Lanzhou, Chin;

关键词: Peptide antagonist;    cell penetrating peptide;    camptothecin delivery;    gene delivery;   

DOI  :  10.1080/10717544.2019.1706669

来源: publisher

【 摘 要 】

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.

【 授权许可】

CC BY