Drug Transporters
From PubPK
Transporters are membrane proteins whose primary function is to facilitate the flux of molecules into and out of cells. According to their transport mechanisms, transporters can be divided into passive and active transporters. Passive transporters, also called facilitated transporters, allow molecules to move across cell membrane down their electrochemical gradients. Such a spontaneous process decreases free energy and increases entropy in a system and therefore does not consume any chemical energy. In contrast to passive transporters, active transporters typically move molecules against their electrochemical gradients; such a process is entropically unfavorable and therefore needs coupling of the hydrolysis of adenosine triphosphate (ATP) as an energy source (You and Morris, 2007).
Transporters play an important role in the processes of drug absorption, distribution, metabolism and excretion (ADME). Transporters that are important in pharmacokinetics are generally expressed in tissues with barrier functions such as the liver, kidney, intestine, placenta, and brain (Giacomini and Sugiyama, 2005). Most drug transporters can be classified into two gene superfamilies: the ATP-binding cassette (ABC) superfamily and the solute carrier (SLC) superfamily.
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Human Drug Transporters
ATP-binding cassette (ABC) transporters
- ABCB1 (MDR1)
- ABCB4 (MDR3)
- ABCB11 (BSEP)
- ABCC1 (MRP1)
- ABCC2 (MRP2)
- ABCC3 (MRP3)
- ABCC4 (MRP4)
- ABCC5 (MRP5)
- ABCC6 (MRP6)
- ABCC10 (MRP7)
- ABCC11 (MRP8)
- ABCG2 (BCRP)
Solute carrier (SLC) transporters
- SLC10A1 (NTCP)
- SLC10A2 (NTCP2)
- SLC15A1 (PEPT1)
- SLC15A2 (PEPT2)
- SLC16A1 (MCT1)
- SLC16A4 (MCT5)
- SLC22A1 (OCT1)
- SLC22A2 (OCT2)
- SLC22A3 (OCT3)
- SLC22A4 (OCTN1)
- SLC22A5 (OCTN2)
- SLC22A6 (OAT1)
- SLC22A7 (OAT2)
- SLC22A8 (OAT3)
- SLC22A11 (OAT4)
- SLCO1A2 (OATP-A)
- SLCO1B1 (OATP-C)
- SLCO1B3 (OATP8)
- SLCO1C1 (OATP-F)
- SLCO2B1 (OATP-B)
- SLCO3A1 (OATP-D)
- SLCO4A1 (OATP-E)
See Also
- Drug Transport in the Liver
- Drug Transport in the Kidney
- Drug Transport in the Intestine
- Drug Transport in the Brain
External links
- Human ATP-Binding Cassette Transporters
- Human Transport Classification Database (TCDB)
- TP-search Transport Database
References
- Giacomini KM and Sugiyama Y (2005) Membrane transporters and drug response, in: Goodman & Gilman's The Pharmacological Basis of Therapeutics (Brunton LL, Lazo JS, and Parker KL eds), pp 41-70, 11th edition, McGraw-Hill, New York.
- You G and Morris ME (2007) Overview of Drug Transporter Families, in: Drug Transporters: Molecular Characterization and Role in Drug Disposition (You G and Morris ME eds), pp 1-10, Wiley, New York.
