Solute carrier organic anion transporter family member 4C1 (OATP4C1) (OATP4C1)

Human organic anion transporting polypeptide 4C1 (OATP4C1), encoded by the SLCO4C1 gene, is a sodium-independent transporter primarily expressed on the basolateral membrane of renal proximal tubule cells [1, 6]. It plays a critical role in the renal handling of both endogenous compounds and exogenous drugs by facilitating their uptake from the blood into the kidney for urinary excretion [2, 16]. Key endogenous substrates include thyroid hormones (T3 and T4), cAMP, and uremic toxins such as asymmetric dimethylarginine (ADMA) and guanidinosuccinate [1, 5, 18]. OATP4C1 is also responsible for the transport of clinically important drugs like digoxin, methotrexate, and sitagliptin [3, 16]. In the context of chronic kidney disease (CKD), the accumulation of uremic toxins due to impaired OATP4C1 function is associated with hypertension, cardiac hypertrophy, and further renal inflammation [8, 9]. Consequently, OATP4C1 is considered a potential therapeutic target; for instance, statins have been shown to upregulate its expression via the aryl hydrocarbon receptor, enhancing toxin clearance [8, 9]. Additionally, OATP4C1 is a significant site for drug-drug interactions, as its activity can be inhibited by various medications, including ritonavir and verapamil, potentially leading to altered pharmacokinetics of co-administered substrates [2, 14].

Other names

SLCO4C1OATP-HOATP-M1OATPXSLC21A20PRO2176

Substrate for renal uptake and excretion, Inhibition of transporter activity, Transcriptional induction of expression