Target intelligence / Profile preview

Hepatocyte Uptake Transporters (None)

Target
None
Molecular classification
Transporter, Membrane Protein, OATP/SLCO family, OCT/SLC22A family, NTCP/SLC10A family
01

Overview

Hepatocyte uptake transporters are membrane proteins located on the basolateral surface of hepatocytes that mediate the uptake of various compounds from the blood into the liver. They are essential for hepatic drug clearance, metabolism, and biliary excretion. Key families include OATPs, OCT1, and NTCP. Alterations in transporter function can significantly impact drug disposition and lead to drug-drug interactions or altered drug efficacy.

Other names
Hepatic Uptake TransportersLiver Uptake TransportersSinusoidal Uptake Transporters
02

Mechanism of action

Facilitate the transport of substrates across the hepatocyte membrane, influencing drug concentrations within the liver and subsequent metabolism or excretion.

03

Biological functions

Hepatic drug clearanceHepatic metabolismBiliary excretionHepatic uptake of endogenous compoundsHomeostasis of bile acidsHomeostasis of bilirubin conjugates
04

Disease associations

Drug-induced liver injuryHyperbilirubinemiaCholestasisHepatitisDrug resistance
05

Safety considerations

Drug-drug interactions via transporter competitionGenetic polymorphisms affecting transporter functionVariability in transporter expression levelsPotential for altered drug disposition and toxicity
06

Interacting drugs

Rosuvastatin

3 more in the full profile.

07

Biomarkers

Plasma levels of probe substrates (e.g., rosuvastatin, pravastatin)Activity assays in human hepatocytes

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