ABC Transporters

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Presentation Description

Creative Biogene offers a wide range of ABC transporters assays, including P-gp (MDR1/ABCB1), BCRP (ABCG2) and BSEP (sPgp/ABCB11), etc. P-gp, BCRP and BSEP are highly expressed in the luminal membrane of enterocytes, endothelial cells in the brain, the border membrane of renal proximal tubules and canalicular membrane of hepatocytes.

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Presentation Transcript

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ABC Transporters Members of ABC superfamily use ATP as energy source which allows them to pump substrates against a concentration gradient. Drugs can be simultaneously substrates or inhibitors of more than one efflux transporter suggesting that ABC transporters employ a combined role in detoxification at above organs. Furthermore the simultaneous down- regulation and induction of these transporters can occur following administration of a single compound. Down-regulation or inhibition of ABC efflux transporters can be used as a strategy to improve oral drug bioavailability of known substrates as these transporters prevent drugmolecules from being absorbed Margarida et al. 2012.

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MDR1 It is a vital factor in absorption and pharmacokinetics because drugs are excreted by MDR1 from cells to the lumen of the small intestine. Digoxin and paclitaxel are typical substrates. MDR1 is mainly expressed in tumor cells causing multidrug resistance of anticancer drugs. MDR1 is also expressed in the bile canaliculus of hepatocytes and in proximal tubules and excretes compounds into the bile and urine. In addition MDR1 is expressed in the blood brain barrier BBB and prevents many compounds from entering the brain.

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MRP2 MRP2 excreted drugs into bile from the liver and into the lumen of the small intestine or into urine from the kidney. MRP2 could cause multidrug resistance and drug-drug interactions along with MDR1 and BCRP . Cisplatin and indinavir are typical substrates.

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