Target intelligence / Profile preview

Solute carrier organic anion transporter family member 3A1 (Organic anion-transporting polypeptide 3A1) (SLCO3A1)

Target
SLCO3A1
Molecular classification
Transporter, Solute carrier family, Organic anion-transporting polypeptide family
01

Overview

Solute carrier organic anion transporter family member 3A1 (SLCO3A1), commonly known as OATP3A1, is a transmembrane protein that mediates the sodium-independent transport of various endogenous and exogenous organic anions. It is ubiquitously expressed in human tissues, with particularly high concentrations in the brain, heart, testis, and lactiferous ducts, where it transports critical substrates such as prostaglandins (PGE1, PGE2) and thyroid hormones (T4, T3). In the liver, OATP3A1 acts as an adaptive bile acid efflux transporter that is significantly upregulated during cholestasis to protect hepatocytes from bile acid-induced injury. Beyond its physiological roles, OATP3A1 is overexpressed in multiple malignancies, including breast and colorectal cancers, where it may contribute to tumor progression by facilitating the uptake of steroid hormones. The transporter is also linked to inflammatory conditions like Crohn's disease and neurological disorders, making it a potential target for therapeutic modulation. As a transporter of drugs like simvastatin and benzylpenicillin, OATP3A1 is a significant site for potential drug-drug interactions that can affect the pharmacokinetics and safety profiles of various therapeutic agents.

Other names
OATP3A1OATP-DOATPDSLC21A11SLC21A9PGE1 transporterOATP-RP3OATPRP3Solute carrier family 21 member 9Solute carrier family 21 member 11
02

Mechanism of action

OATP3A1 functions primarily as a sodium-independent uptake transporter for organic anions and hormones, facilitating their entry into cells; however, it can also act as an adaptive efflux transporter for bile acids under cholestatic conditions.

03

Biological functions

Organic anion transportProstaglandin transportThyroid hormone transportBile acid effluxNF-kappaB signaling regulationNeuropeptide transport
04

Disease associations

CancerCholestasisInflammatory bowel diseaseEpilepsyIntestinal perforationPrimary hypertrophic osteoarthropathyAttention deficit hyperactivity disorderNicotine dependence
05

Safety considerations

Drug-drug interactionsAltered clearance of endogenous prostaglandinsInterference with thyroid hormone homeostasis
06

Interacting drugs

Simvastatin

8 more in the full profile.

07

Biomarkers

OATP3A1 mRNA expression levelOATP3A1 protein expression level

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