Target intelligence / Profile preview

Solute carrier family 22 member 6 and 8 (OAT1 and OAT3) (SLC22A6/SLC22A8)

Target
SLC22A6/SLC22A8
Molecular classification
Transporter, Solute carrier family, Organic anion transporter
01

Overview

Solute carrier family 22 member 6 (OAT1) and member 8 (OAT3) are essential multispecific transporters primarily expressed on the basolateral membrane of renal proximal tubule cells [5, 10, 14]. They facilitate the uptake of a diverse range of organic anions from the systemic circulation into the kidney for subsequent excretion into the urine [5, 15]. These transporters handle critical endogenous substrates, including uric acid, prostaglandins, and uremic toxins, as well as numerous pharmaceutical agents such as beta-lactam antibiotics, antivirals, and diuretics [5, 10, 11]. Due to their broad substrate specificity, OAT1 and OAT3 are major sites for clinically significant drug-drug interactions, where competitive inhibition can prolong the half-life of co-administered drugs or protect against nephrotoxicity [10, 15, 16]. They are recognized as therapeutic targets in the management of hyperuricemia and gout, and their dysfunction is linked to the progression of chronic kidney disease and acute kidney injury [1, 3, 17]. Understanding their activity is vital for predicting drug pharmacokinetics and ensuring therapeutic safety [9, 12].

Other names
Organic anion transporter 1Organic anion transporter 3OAT1OAT3NKTNovel kidney transporterROAT1HOAT1HOAT3
02

Mechanism of action

Inhibition of basolateral uptake to modulate drug clearance or reduce intracellular toxicity

03

Biological functions

Renal excretionOrganic anion transportXenobiotic clearanceHomeostasisUrate transport
04

Disease associations

Chronic kidney diseaseHyperuricemiaGoutDrug-induced nephrotoxicityAcute kidney injury
05

Safety considerations

Drug-drug interactionsNephrotoxicityAltered systemic exposure of co-administered drugs
06

Interacting drugs

Probenecid

9 more in the full profile.

07

Biomarkers

CreatinineUric acidIndoxyl sulfatep-Cresol sulfate

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