利用 pH 响应型细胞穿透多聚（二硫键）将抗体靶向递送至癌细胞内。

targeted delivery of antibodies into cancer cells with pH-responsive cell-penetrating poly(disulfide)s.

机构信息

Institute of Drug Metabolism and Pharmaceutical Analysis, Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Cancer Center, & Hangzhou Institute of Innovative Medicine, Zhejiang University, Hangzhou 310058, China.

Department of Chemistry, National University of Singapore, 3 Science Drive 3, 117543, Singapore.

出版信息

Chem Commun (Camb). 2022 Jan 27;58(9):1314-1317. doi: 10.1039/d1cc06840g.

DOI:10.1039/d1cc06840g

PMID:35005760

Abstract

Cell-penetrating poly(disulfide)s (CPDs) are promising vehicles for cytosolic delivery of proteins. However, currently available arginine-rich CPD has rarely been reported for systemic delivery due to its "always" positive charge. Herein, we developed pH-responsive CPD that executes tumor targeting delivery protonation of imidazole groups within the acidic tumor microenvironment.

摘要

细胞穿透多硫化物 (CPD) 是一种很有前途的胞质蛋白递呈载体。然而，由于其“始终”带正电荷，目前可用的富含精氨酸的 CPD 很少被报道用于全身递送。在此，我们开发了一种 pH 响应的 CPD，该 CPD 在酸性肿瘤微环境中通过质子化咪唑基团来执行肿瘤靶向递呈。