Target intelligence / Profile preview

Organic anion transporter 1 (OAT1), Organic anion transporter 3 (OAT3) (OAT1 (SLC22A6), OAT3 (SLC22A8))

Target
OAT1 (SLC22A6), OAT3 (SLC22A8)
Molecular classification
Transporter (solute carrier family 22, SLC22), Integral membrane protein, Major Facilitator Superfamily (MFS) member
01

Overview

Organic anion transporter 1 and Organic anion transporter 3 are high-capacity, multispecific transport proteins of the SLC22 family, mainly expressed in the basolateral membrane of renal proximal tubule cells. They mediate the secondary active uptake of a wide range of endogenous metabolites, environmental toxins, and therapeutic drugs from the blood into kidney cells. Inside the cell, these compounds are subsequently extruded into the urine via other transporters and excreted from the body. Their function is essential for drug clearance, renal homeostasis, and systemic detoxification. Dysfunction or pharmacological inhibition of these transporters can have profound effects on drug efficacy, toxicity, and the progression of renal diseases.

Other names
Solute carrier family 22 member 6SLC22A6New Kidney Transporter (NKT)Solute carrier family 22 member 8SLC22A8
02

Mechanism of action

Antiport mechanism: organic anion uptake exchanged for intracellular dicarboxylates (e.g., α-ketoglutarate). Substrate translocation from blood to intracellular compartment, facilitating excretion.

03

Biological functions

Renal secretion of organic anionsDetoxification and excretion of waste (uremic toxins)Pharmacokinetics and drug clearanceInter-organ metabolite communication
04

Disease associations

Chronic kidney disease (impaired OAT1/OAT3 function disrupts toxin elimination)Drug-induced kidney injury (toxicity from drug accumulation)Hereditary metabolic disorders (mutations affecting transporter function)
05

Safety considerations

Drug-drug interactions: competition or inhibition at OAT1/OAT3 affects drug elimination, leading to increased toxicityGenetic polymorphisms or mutations can alter drug response or predispose to adverse effectsNephrotoxicity (impaired clearance can exacerbate kidney damage, especially with nephrotoxic drugs)
06

Interacting drugs

Antiviral nucleoside phosphonates (tenofovir, adefovir)

5 more in the full profile.

07

Biomarkers

Decreased transporter function or expression can serve as biomarker for renal clearance capacityElevated serum levels of organic anion toxins (e.g., indoxyl sulfate) can indicate OAT1/OAT3 dysfunction

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