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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:

  • mNtcp
  • mOct1


3rd German Pharm-Tox Summit
Göttingen, Germany
26 February - 1 March 2018

Saarbrücken, Germany
8 March 2018


AAPS Workshop
Virginia, USA
16 - 18 April 2018


20th Barrier- and

Bad Herrenalb, Germany
7 - 9 May 2018

Greifswalder Transporttage 2018
Greifswald, Germany
October 2018


Guidance for Industry (FDA and EMA)