Drug Transporters

Drug-drug interactions (DDI) are severe drug-induced side effects. The occurrence of drug–drug interactions is due to the effects of drugs on uptake and efflux transporters, which can be roughly divided into two categories: induction and inhibition. Drug transporters that distribute in small intestine, liver, and kidney are determinants of the pharmacokinetic profile of drugs. Transporter-mediated DDI in these three organs can considerably influence the pharmacokinetics and clinical effects of drugs.

Drug transporters mediate the uptake and efflux of a broad variety of drugs and drug metabolites. Most uptake transporters are members of the solute carrier (SLC) family, while most efflux transporters are members of the ATP-binding cassette (ABC) transporter family.

Drug Transporters

Uptake Transporters

Solute carriers (SLC) family are important membrane transporters involved in the ADME process of drugs. They facilitate the uptake of hydrophobic and amphiphilic organic compounds, such as conjugated steroids, thyroid hormones, eicosanoids, and bile acids. Creative Bioarray provides a wide range of uptake transporter inhibition and induction assays to assess the potential interactions between candidate compounds and these drug transporters.

ClassName (gene nomenclature)
Organic anion-transporting
polypeptide family
Organic anion transporter familyOAT1 / SLC22A6
OAT2 / SLC22A7
OAT3 / SLC22A8
Organic cation transporter familyOCT1 / SLC22A1
OCT2 / SLC22A2

Efflux Transporters

In contrast to the SLC family, ATP binding cassette (ABC) transporters inhibit intestinal absorption and blood-brain barrier penetration of most drugs, making them excrete from the body via bile and urine. Creative Bioarray can help clients analyze the potential roles of ABC superfamily members in the process of drug-drug interactions.

ClassName (gene nomenclature)
ABC transportersP-glycoprotein (P-gp), Multi-drug resistance 1 (MDR1/ABCB1)
Multi-drug resistance-associated protein 2 (MRP2/ABCC2)
Breast cancer-resistance protein (BCRP/ABCG2)

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