TY - JOUR
T1 - Asialoglycoprotein receptor and its application in liver-targeted drug delivery
AU - Huang, Yuan Yu
AU - Liang, Zi Cai
PY - 2015
Y1 - 2015
N2 - 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.
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.
KW - ASGPR
KW - Antisense oligonucleotides
KW - Drug delivery
KW - GalNAc
KW - Liver-targeting
KW - SiRNA
UR - http://www.scopus.com/inward/record.url?scp=84938056583&partnerID=8YFLogxK
U2 - 10.16476/j.pibb.2015.0028
DO - 10.16476/j.pibb.2015.0028
M3 - Article
AN - SCOPUS:84938056583
SN - 1000-3282
VL - 42
SP - 501
EP - 510
JO - Progress in Biochemistry and Biophysics
JF - Progress in Biochemistry and Biophysics
IS - 6
ER -