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Organic anion transporter protein (OAT (for "organic anion transporter") and OATP (for "organic-anion-transporting polypeptide"), used according to family/subtype)

Target
OAT (for "organic anion transporter") and OATP (for "organic-anion-transporting polypeptide"), used according to family/subtype
Molecular classification
Transporter, Solute carrier family (includes SLC22A, SLCO), Major facilitator superfamily (MFS), ATP-binding cassette (ABC; for MRPs)
01

Overview

Organic anion transporter proteins are transmembrane proteins encompassing several families (notably the SLC22A family for OAT, SLCO family for OATP, and the ABCC family for MRP) mediating the transport of a diverse range of endogenous metabolites and xenobiotic compounds. These proteins play a pivotal physiological role in the renal secretion of organic anions, hepatic clearance of bile acids, steroid conjugates, and hormones, and serve as a major pathway for drug and toxin elimination. Their biological importance is underscored by their involvement in human disease (renal, hepatic, metabolic) and their critical role in determining drug pharmacokinetics, efficacy, and safety. Multiple drugs (statins, chemotherapeutic agents, antibiotics, etc.) are known substrates or inhibitors of organic anion transporters, and gene variants in these families can serve as biomarkers for treatment selection and safety monitoring.

Other names
Organic-anion-transporting polypeptideOAT (organic anion transporter)OATP (organic-anion-transporting polypeptide)SLC22 transporters (for OATs)SLCO transporters (for OATPs)Multidrug resistance-associated protein (MRP; related family)
02

Mechanism of action

Facilitate or inhibit transporter-mediated uptake/bioavailability of drugs Block transporter to modulate toxin/drug clearance Change drug plasma/bile/urine concentrations via competitive inhibition

03

Biological functions

Elimination of xenobiotics and drugsRenal secretion of organic anionsHepatic excretion of bile acids, bilirubin, and hormonesBlood-brain barrier substrate transportDrug absorption, distribution, and excretion
04

Disease associations

Cancer (tumor resistance, chemotherapy pharmacokinetics)Metabolic disease (e.g., hyperuricemia, Dubin-Johnson syndrome)Drug-induced toxicityRenal diseaseHepatic disease
05

Safety considerations

Drug-drug interactions due to overlapping substrate specificityGenetic polymorphisms affecting drug pharmacokineticsUnexpected toxicity from impaired transporter function (e.g., statin myopathy with SLCO1B1 variant)
06

Interacting drugs

Statins

6 more in the full profile.

07

Biomarkers

Polymorphisms in OAT/OATP genes (predict drug response, drug-drug interactions; e.g., SLCO1B1 variants for statin toxicity)Urinary or plasma substrate levels (e.g., para-aminohippuric acid for renal OAT function)

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