Target intelligence / Profile preview

Hepatocyte cell-surface receptors

Molecular classification
Receptor, Transporter, Glycoprotein, Ion channel, Other
01

Overview

Hepatocyte cell-surface receptors represent a broad category of proteins located on the plasma membrane of liver cells, serving as vital interfaces for metabolic, signaling, and transport processes (PMID: 8428960). This group includes several high-profile therapeutic targets, most notably the asialoglycoprotein receptor (ASGPR; UniProt P07306), which is utilized for the targeted delivery of N-acetylgalactosamine (GalNAc)-conjugated RNA interference (RNAi) and antisense oligonucleotide (ASO) drugs such as givosiran and inclisiran (PMID: 30305311). Another critical member is the sodium/taurocholate cotransporting polypeptide (NTCP; UniProt Q14973), which acts as the primary entry point for hepatitis B and D viruses and is targeted by the entry inhibitor bulevirtide (PMID: 32659211). Additionally, receptors like the low-density lipoprotein receptor (LDLR; UniProt P01130) and scavenger receptor class B member 1 (SR-BI; UniProt Q8WTV0) are essential for lipid homeostasis and are involved in the entry of the hepatitis C virus (PMID: 24436984). Because this term encompasses a wide array of proteins with distinct structures and functions, it is considered a functional category rather than a single molecular target. Consequently, drug development efforts are typically focused on specific individual receptors within this class to achieve precise therapeutic outcomes in liver-related diseases.

Other names
Liver cell surface receptorsHepatic cell surface receptorsHepatocyte receptorsHepatocyte-specific surface proteins
02

Mechanism of action

Receptor-mediated endocytosis for targeted drug delivery; inhibition of viral attachment and entry; modulation of lipoprotein clearance and bile acid transport.

03

Biological functions

EndocytosisMetabolismSignal transductionCell adhesionViral entryOther
04

Disease associations

InfectionCancerCardiovascular diseaseMetabolic diseaseInflammationOther
05

Safety considerations

HepatotoxicityInjection site reactionsOff-target effects in non-hepatic tissuesPotential for interference with endogenous ligand transportImmune-mediated liver injury
06

Interacting drugs

Givosiran

7 more in the full profile.

07

Biomarkers

Alanine aminotransferase (ALT)Aspartate aminotransferase (AST)Low-density lipoprotein cholesterol (LDL-C)Hepatitis B surface antigen (HBsAg)Viral loadBile acids

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