The research of liver-targeted drugs based on asialoglycoprotein receptor
10.16438/j.0513-4870.2022-0755
- VernacularTitle:基于去唾液酸糖蛋白受体的肝靶向药物的研究
- Author:
Guo-zhang LONG
;
Zhuo ZHANG
;
Wu-hong CHEN
;
You-hong HU
- Publication Type:Research Article
- Keywords:
asialoglycoprotein receptor;
liver-targeted;
ligand;
release strategy;
rug development
- From:
Acta Pharmaceutica Sinica
2023;58(2):235-245
- CountryChina
- Language:Chinese
-
Abstract:
Asialoglycoprotein receptor (ASGPR) is highly expressed on the surface of parenchymal liver cells. It can specifically recognize and bind to desialylated glycoproteins which contain terminal galactose or N-acetylgalactosamine residues, and endocytosed by clathrin-mediated endocytosis, transported and then degraded in lysosome. Based on this character, ASGPR mediated liver-targeted drug delivery is likely to increase drug distribution, reduce potential side effects and lower dose. This article reviewed the expression, structure, ligand binding and endocytosis of ASGPR, and summarized the design and optimization of ASGPR ligands and the release strategies. Finally, we put forward some expects about the clinical drug development for ASGPR.
