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用双特异性抗癌和抗血管生成聚合物-阿仑膦酸盐-紫杉烷共轭物靶向骨转移。

Targeting bone metastases with a bispecific anticancer and antiangiogenic polymer-alendronate-taxane conjugate.

作者信息

Miller Keren, Erez Rotem, Segal Ehud, Shabat Doron, Satchi-Fainaro Ronit

机构信息

Department of Physiology and Pharmacology, Sackler School of Medicine, Tel Aviv University, Tel Aviv 69978, Israel.

出版信息

Angew Chem Int Ed Engl. 2009;48(16):2949-54. doi: 10.1002/anie.200805133.

DOI:10.1002/anie.200805133
PMID:19294707
Abstract

A polymer therapeutic designed for combination anticancer and antiangiogenic therapy inhibited the proliferation of prostate carcinoma cells and the proliferation, migration, and tube-formation of endothelial cells. The nanoconjugate was formed from an N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer, the bisphosphonate alendronate (for bone targeting), and the chemotherapy agent paclitaxel (PTX), which is cleaved by cathepsin B (see scheme).

摘要

一种设计用于联合抗癌和抗血管生成治疗的聚合物疗法可抑制前列腺癌细胞的增殖以及内皮细胞的增殖、迁移和管形成。该纳米缀合物由N-(2-羟丙基)甲基丙烯酰胺(HPMA)共聚物、双膦酸盐阿仑膦酸钠(用于骨靶向)和化疗药物紫杉醇(PTX)形成,紫杉醇可被组织蛋白酶B裂解(见图)。

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