, Volume 447, Issue 5, pp 666-676
Date: 19 Jul 2003

The SLC22 drug transporter family

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Abstract

The SLC22 family comprises organic cation transporters (OCTs), zwitterion/cation transporters (OCTNs), and organic anion transporters (OATs). These transporters contain 12 predicted α-helical transmembrane domains (TMDs) and one large extracellular loop between TMDs 1 and 2. Transporters of the SLC22 family function in different ways: (1) as uniporters that mediate facilitated diffusion in either direction (OCTs), (2) as anion exchangers (OAT1, OAT3 and URAT1), and (3) as Na+/l-carnitine cotransporter (OCTN2). They participate in the absorption and/or excretion of drugs, xenobiotics, and endogenous compounds in intestine, liver and/or kidney, and perform homeostatic functions in brain and heart. The endogenous substrates include monoamine neurotransmitters, choline, l-carnitine, α-ketoglutarate, cAMP, cGMP, prostaglandins, and urate. Defect mutations of transporters of the SLC22 family may cause specific diseases such as "primary systemic carnitine deficiency" or "idiopathic renal hypouricemia" or change drug absorption or excretion.