Asialoglycoprotein receptor and its application in liver-targeted drug delivery

Yuan Yu Huang; Zi Cai Liang

doi:10.16476/j.pibb.2015.0028

Asialoglycoprotein receptor and its application in liver-targeted drug delivery

Yuan Yu Huang^*, Zi Cai Liang

^*Corresponding author for this work

Peking University

Research output: Contribution to journal › Article › peer-review

11 Citations (Scopus)

Abstract

Asialoglycoprotein receptor (ASGPR) was specifically expressed by hepatocytes, which could recognize and bind asialoglycoprotein, galactose (Gal), galactosamine, N-acetylgalactosamine (GalNAc), etc. with high affinity. In a receptor-mediated-endocytosis (RME) manner, various molecules could be delivered into hepatocytes effectively. In this review, we firstly introduced the discovery, structure, function, expression pattern and endocytosis properties of ASGPR. Then the influence factors of ligand/receptor interaction and RME, including ligand species, valence, orientation and particle size, were analyzed. In addition, studies on ASGPR-mediated drug delivery in the past decades were reviewed. More importantly, progress in GalNAc-conjugation or -modification technologies employed in liver-targeted transportation of siRNA, antisense and antagomir were summarized.

Original language	English
Pages (from-to)	501-510
Number of pages	10
Journal	Progress in Biochemistry and Biophysics
Volume	42
Issue number	6
DOIs	https://doi.org/10.16476/j.pibb.2015.0028
Publication status	Published - 2015
Externally published	Yes

Keywords

ASGPR
Antisense oligonucleotides
Drug delivery
GalNAc
Liver-targeting
SiRNA

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10.16476/j.pibb.2015.0028

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abstract = "Asialoglycoprotein receptor (ASGPR) was specifically expressed by hepatocytes, which could recognize and bind asialoglycoprotein, galactose (Gal), galactosamine, N-acetylgalactosamine (GalNAc), etc. with high affinity. In a receptor-mediated-endocytosis (RME) manner, various molecules could be delivered into hepatocytes effectively. In this review, we firstly introduced the discovery, structure, function, expression pattern and endocytosis properties of ASGPR. Then the influence factors of ligand/receptor interaction and RME, including ligand species, valence, orientation and particle size, were analyzed. In addition, studies on ASGPR-mediated drug delivery in the past decades were reviewed. More importantly, progress in GalNAc-conjugation or -modification technologies employed in liver-targeted transportation of siRNA, antisense and antagomir were summarized.",

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AU - Huang, Yuan Yu

AU - Liang, Zi Cai

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AB - Asialoglycoprotein receptor (ASGPR) was specifically expressed by hepatocytes, which could recognize and bind asialoglycoprotein, galactose (Gal), galactosamine, N-acetylgalactosamine (GalNAc), etc. with high affinity. In a receptor-mediated-endocytosis (RME) manner, various molecules could be delivered into hepatocytes effectively. In this review, we firstly introduced the discovery, structure, function, expression pattern and endocytosis properties of ASGPR. Then the influence factors of ligand/receptor interaction and RME, including ligand species, valence, orientation and particle size, were analyzed. In addition, studies on ASGPR-mediated drug delivery in the past decades were reviewed. More importantly, progress in GalNAc-conjugation or -modification technologies employed in liver-targeted transportation of siRNA, antisense and antagomir were summarized.

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KW - Antisense oligonucleotides

KW - Drug delivery

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KW - Liver-targeting

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Asialoglycoprotein receptor and its application in liver-targeted drug delivery

Abstract

Keywords

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