Asialoglycoprotein receptor (ASGPR) (ASGPR)

The Asialoglycoprotein receptor (ASGPR), frequently referred to as the hepatic galactose receptor, is a transmembrane C-type lectin primarily expressed on the sinusoidal surface of hepatocytes [9, 10]. Its primary biological function is the recognition, binding, and clathrin-mediated endocytosis of desialylated (asialo) glycoproteins that display terminal galactose or N-acetylgalactosamine (GalNAc) residues, thereby clearing them from systemic circulation and maintaining plasma glycoprotein homeostasis [1, 15]. Beyond its physiological role, ASGPR is implicated in the entry mechanisms of hepatotropic viruses like Hepatitis B and is utilized as a biomarker in hepatocellular carcinoma [2, 3, 9]. In the biotechnology sector, ASGPR is a premier target for liver-specific drug delivery, particularly for RNA therapeutics [12, 13]. By conjugating small interfering RNAs (siRNAs) or antisense oligonucleotides to multivalent GalNAc clusters, pharmaceutical companies can achieve highly specific hepatocyte uptake and potent gene silencing with significantly reduced systemic toxicity [12, 15]. This receptor-mediated targeting strategy is the foundation for several FDA-approved treatments, including Givosiran and Inclisiran, used to treat various genetic, metabolic, and cardiovascular conditions [13, 15].

Other names

Galactose receptorHepatic lectinAshwell-Morell receptorHepatic galactose receptorAsialoglycoprotein receptor 1 (ASGR1)Asialoglycoprotein receptor 2 (ASGR2)

Facilitates hepatocyte-specific drug delivery via multivalent binding to terminal galactose or N-acetylgalactosamine (GalNAc) residues, followed by clathrin-mediated endocytosis and lysosomal escape [10, 12, 15].