The SLC22 Drug Transporter Family

Pflugers Arch. 2004 Feb;447(5):666-76. doi: 10.1007/s00424-003-1089-9. Epub 2003 Jul 19.

Abstract

The SLC22 family comprises organic cation transporters (OCTs), zwitterion/cation transporters (OCTNs), and organic anion transporters (OATs). These transporters contain 12 predicted alpha-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, alpha-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.

Publication types

  • Review

MeSH terms

  • Animals
  • Biological Transport / physiology
  • Humans
  • Multigene Family / physiology
  • Organic Anion Transporters / chemistry
  • Organic Anion Transporters / genetics
  • Organic Anion Transporters / physiology*
  • Organic Cation Transport Proteins / chemistry
  • Organic Cation Transport Proteins / genetics
  • Organic Cation Transport Proteins / physiology*
  • Pharmacokinetics

Substances

  • Organic Anion Transporters
  • Organic Cation Transport Proteins