Target intelligence / Profile preview

Human organic anion transporter 1 (OAT1)

Target
OAT1
Molecular classification
Transporter, Major facilitator superfamily (MFS), Solute carrier family (SLC)
01

Overview

Human organic anion transporter 1 (OAT1), encoded by the SLC22A6 gene, is a transmembrane protein primarily expressed on the basolateral membrane of proximal tubular cells in the kidneys. It mediates the uptake and exchange of a wide range of small, hydrophilic organic anions from plasma into renal tubular cells for subsequent excretion into urine. This process is essential for clearing endogenous metabolites as well as various drugs from circulation. OAT1 functions as part of a coordinated system with other transporters such as NaDC3, which replenishes intracellular dicarboxylates required for its activity. The protein belongs to both the solute carrier family and major facilitator superfamily. Its function is critical in pharmacokinetics—alterations can lead to significant changes in drug disposition, efficacy, toxicity risk, and susceptibility to nephrotoxic injury.

Other names
Solute carrier family 22 member 6SLC22A6hOAT1Organic anion transporter 1
02

Mechanism of action

Inhibition of OAT1-mediated transport to alter renal clearance or tissue distribution of drugs/metabolites

03

Biological functions

Renal excretion of organic anionsCellular uptake and exchange of small hydrophilic organic anionsRegulation of endogenous and exogenous compound levels in plasma and tissues
04

Disease associations

Drug-induced nephrotoxicity (due to altered drug transport)Other (potential involvement in kidney diseases, pharmacokinetics, and drug-drug interactions)
05

Safety considerations

Risk of drug-drug interactions due to inhibition or competition at the transporter site, potentially leading to increased toxicity or reduced efficacy for co-administered medications cleared via OAT1
06

Interacting drugs

Dabrafenib

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