去唾液酸糖蛋白受体
化学
内化
结合
紫杉醇
药品
内吞作用
组合化学
体外
生物活性
药理学
生物化学
受体
肝细胞
化疗
生物
数学分析
遗传学
数学
作者
Rostislav A. Petrov,S. Yu. Maklakova,Yan A. Ivanenkov,Stanislav A. Petrov,Olga V. Sergeeva,Emil Yu. Yamansarov,Irina V. Saltykova,Igor I. Kireev,Irina B. Alieva,Ekaterina V. Deyneka,Alina A. Sofronova,Anastasiia V. Aladinskaia,Alexandre V. Trofimenko,R. S. Yamidanov,С. В. Ковалев,Victor Kotelianski,Timofei S. Zatsepin,Е. К. Белоглазкина,Alexander G. Majouga
标识
DOI:10.1016/j.bmcl.2017.12.032
摘要
Asialoglycoprotein receptor (ASGP-R) is a promising biological target for drug delivery into hepatoma cells. Nevertheless, there are only few examples of small-molecule conjugates of ASGP-R selective ligand equipped by a therapeutic agent for the treatment of hepatocellular carcinoma (HCC). In the present work, we describe a convenient and versatile synthetic approach to novel mono- and multivalent drug-conjugates containing N-acetyl-2-deoxy-2-aminogalactopyranose and anticancer drug – paclitaxel (PTX). Several molecules have demonstrated high affinity towards ASGP-R and good stability under physiological conditions, significant in vitro anticancer activity comparable to PTX, as well as good internalization via ASGP-R-mediated endocytosis. Therefore, the conjugates with the highest potency can be regarded as a promising therapeutic option against HCC.
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