Target intelligence / Profile preview

Solute carrier organic anion transporter family member 1A2 (OATP1A2)

Target
OATP1A2
Molecular classification
Transporter, Membrane protein
01

Overview

Solute carrier organic anion transporter family member 1A2 is a sodium-independent membrane transporter encoded by the SLCO1A2 gene in humans. It mediates cellular uptake of a variety of endogenous and exogenous organic ions—including bile acids, steroid conjugates such as dehydroepiandrosterone sulfate (DHEAS), bromosulphophthalein, and certain drugs—in tissues such as liver, brain, lung, and intestine. The protein belongs to the SLC21 family (now often referred to as SLCO) and plays a key role in xenobiotic metabolism and pharmacokinetics. Genetic variation in SLCO1A2 has been associated with differences in drug response; it has also been identified as a susceptibility locus for some neurodegenerative diseases.

Other names
SLCO1A2OATPOATP-AOATP1SLC21A3Organic anion-transporting polypeptide 1Sodium-independent organic anion transporterSolute carrier family 21 member 3
02

Mechanism of action

Drugs targeting or utilizing this transporter typically act by modulating or relying on its function for cellular uptake and distribution—especially hepatic and intestinal transport—of their active forms or metabolites.

03

Biological functions

Cellular uptake of organic ions (including bile acids, steroidal compounds, bromosulphophthalein)Intestinal absorption of bile acidsXenobiotic metabolic process
04

Disease associations

Cancer (implicated in drug disposition and resistance)Neurodegenerative disease (identified as a susceptibility locus for parkinsonian tauopathy)
05

Safety considerations

Altered drug pharmacokinetics leading to toxicity or therapeutic failure due to genetic variation or inhibition/induction of this transporterDrug-drug interactions when multiple substrates compete for transport
06

Interacting drugs

Statins

2 more in the full profile.

07

Biomarkers

Expression levels of SLCO1A2Genetic variants of SLCO1A2

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