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Drug efflux transporter

Gene Protein Expression/
Substrates Inhibitors Short description
ABCB1 MDR1 liver, BBB, kidney, intestine, placenta
(apical membranes)
rhodamine123 verapamil,
MDR1 (also called P-glycoprotein) is an ATP-dependent drug efflux pump for xenobiotic compounds with broad substrate specificity. It is responsible for decreased drug accumulation in multidrug-resistant cells and often mediates the development of resistance to anticancer drugs.
ABCG2 BCRP placenta, breast, liver,
intestine (apical membranes)
estrone-3-sulfate Ko143 BCRP functions as a xenobiotic transporter which may play a major role in multi-drug resistance. It likely serves as a cellular defense mechanism in response to mitoxantrone and anthracycline exposure. Recently it has been shown to transport organic anions but also steroids like cholesterol, estradiol, progesterone, testosterone.
ABCB11 BSEP liver (apical membranes) taurocholate cyclosporineA, glibenclamide, rifampicin BSEP is the major canalicular bile salt export pump in man responsible for active transport of bile salts across the hepatocyte canalicular membrane into bile.
ABCC2 MRP2 liver, kidney (apical membranes) 5(6)-carboxy-2,'7'-dichlorofluorescein (CDCF) MK-571
The multi-drug resistance protein 2 (MRP2) is located in the canalicular membrane of hepatocytes and in the apical membrane of kidney proximale tubules. MRP2 is an ATP-dependent export pump for xenobiotic compounds and therefore decrease the efficiency of many drugs.



New validated products:

  • MRP2
  • roct1


2nd German Pharm-Tox Summit
Heidelberg, Germany
March 06-09, 2017

19th Barrier- and

Bad Herrenalb, Germany
May 15-17, 2017

14th European ISSX Meeting
Köln, Germany

June 26- 29, 2017

2nd Symposium on Transporters in Drug Discovery
London, UK
May 15-16, 2017

Münster Transporttage 2017
Münster, Germany
October 21 – 22, 2017


Guidance for Industry (FDA and EMA)