Creative Biogene is the leading company offering the ABC (ATP binding cassette) transporters assays. With our abundant experience and expertise in transporters-based drug discovery, talented scientists in Creative Biogene are dedicating to providing the unmatched services to accelerate your research program and significantly increase your chance to success.
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. In these positions, the intestinal absorption, blood-brain barrier penetration and facilitate excretion into the bile and urine were limited.
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).
Fig.1 The model of ABC transporters alternate between the inward- and the outward-facing conformation
MDR1 (Multidrug Resistance protein, P-gp, ABCB1) is participated in the transport and excretion of mainly hydrophobic drugs out of cells. 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.
MRP2 (cMOAT/ABCC2) is expressed in a lot of tissues and transports relatively hydrophilic drugs. 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.
BCRP (MXR, ABCG2) is expressed in a series tumor cells and like MDR1 and MRP2, it may cause multidrug resistance against anticancer drugs too. In addition, BCRP is also expressed in the small intestine, liver and brain, and is involved in the excretion of drugs. Mitoxantrone and statins are typical substrates. In addition, some substrates are also known to overlap with MDR1 or MRP1.
With years of experience in ABC transporters assays, Creative Biogene offers the best services in this filed with the highest efficiency and quality and the most competitive price. Our first-class staffs with abundant know-how in different types of ABC transporters will work closely with your team and find the best inhibitors of your target transporters. Creative Biogene is a reliable partner who can help you significantly accelerate the speed to achieve your research goals.
If you have any special requirements in ABC transporters assay services, please feel free to contact us at email@example.com or 1-631-626-9181. We are looking forward to working together with your attractive projects.
- Margarida, E., José, G. M., Gra?a, S., Leslie, Z. B. (2012) ‘Intestinal drug transporters: An overview’, Adv Drug Deliv Rev, 65(10), 1340-56