叶酸靶向 pH 敏感硼替佐米缀合物用于癌症治疗。
Folate-targeted pH-sensitive bortezomib conjugates for cancer treatment.
机构信息
Department of Pharmaceutical Sciences, Irma Lerma Rangel College of Pharmacy, Texas A&M University, College Station, Texas 77843, USA.
出版信息
Chem Commun (Camb). 2019 Apr 4;55(29):4254-4257. doi: 10.1039/c9cc01344j.
Abstract
In this study, a folate-targeted pH-sensitive bortezomib conjugate was developed for cancer-specific drug delivery and therapy. The conjugate showed improved cellular uptake, penetration, and anticancer activity compared to free bortezomib, a bortezomib-mannitol derivative, and a PEGylated bortezomib conjugate in folate receptor overexpressing cancer cells and their 3D spheroids.
摘要
在这项研究中，开发了一种叶酸靶向 pH 敏感硼替佐米缀合物，用于癌症特异性药物递送和治疗。与游离硼替佐米、硼替佐米甘露醇衍生物以及叶酸受体过表达癌细胞及其 3D 球体中的聚乙二醇化硼替佐米缀合物相比，该缀合物显示出改善的细胞摄取、穿透和抗癌活性。
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