Target intelligence / Profile preview

Hepatocyte Organic Anion Transporting Polypeptide 1B3 (OATP1B3)

Target
OATP1B3
Molecular classification
Membrane Transporter, Transporter, Organic Anion Transporter
01

Overview

Hepatocyte Organic Anion Transporting Polypeptide 1B3 (OATP1B3) is a key membrane transporter protein predominantly expressed in human liver cells (hepatocytes). It plays a crucial role in the hepatic uptake of a wide range of endogenous and exogenous organic anions, including drugs, hormones, and their metabolites. Polymorphisms or genetic variants affecting OATP1B3 can lead to reduced transporter activity, resulting in decreased drug clearance from plasma and increased susceptibility to adverse effects. Altered tissue distribution or aberrant expression patterns have been observed in some cancers. Transport by OATP1B3 does not require ATP hydrolysis but relies on electrochemical gradients across membranes.

Other names
SLCO1B3OATP-8LST-3
02

Mechanism of action

Facilitated diffusion of organic anions into hepatocytes

03

Biological functions

Hepatic Uptake of Organic AnionsDrug DispositionHormone TransportBile Acid Transport
04

Disease associations

Drug-Drug InteractionsPharmacogenomicsCancer
05

Safety considerations

Statin-induced rhabdomyolysis (due to decreased drug clearance)Drug-drug interactions (due to competition for transport)
06

Interacting drugs

Statins

2 more in the full profile.

07

Biomarkers

OATP1B3 polymorphisms

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