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Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs
The breast cancer resistance protein protects against a major chlorophyll-derived dietary phototoxin and protoporphyria
- J. Jonker, M. Buitelaar, A. Schinkel
- BiologyProceedings of the National Academy of Sciences…
- 12 November 2002
The results indicate that humans or animals with low or absent BCRP activity may be at increased risk for developing protoporphyria and diet-dependent phototoxicity and provide a striking illustration of the importance of drug transporters in protection from toxicity of normal food constituents.
Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan.
- J. Jonker, J. Smit, A. Schinkel
- Biology, MedicineJournal of the National Cancer Institute
- 18 October 2000
Bcrp1 mediates apically directed drug transport, appears to reduce drug bioavailability, and protects fetuses against drugs, and it is proposed that strategic application of BCRP inhibitors may lead to more effective oral chemotherapy with topotecan or other B CRP substrate drugs.
An update on in vitro test methods in human hepatic drug biotransformation research: pros and cons.
Multidrug-resistance protein 5 is a multispecific organic anion transporter able to transport nucleotide analogs.
- J. Wijnholds, C. Mol, P. Borst
- Biology, ChemistryProceedings of the National Academy of Sciences…
- 20 June 2000
It is speculated that MRP5 might play a role in some cases of unexplained resistance to thiopurines in acute lymphoblastic leukemia and/or to antiretroviral nucleoside analogs in HIV-infected patients.
Clinical Pharmacokinetics of Therapeutic Monoclonal Antibodies
The parenteral administration, slow tissue distribution and long elimination half-life are the most pronounced clinical pharmacokinetic characteristics of mAbs.
Increased sensitivity to anticancer drugs and decreased inflammatory response in mice lacking the multidrug resistance-associated protein
The results suggest that this ubiquitous GS-X pump, which mediates the cellular excretion of many drugs, glutathione S-conjugates of lipophilic xenobiotics and endogenous cysteinyl leukotrienes, is dispensable in mice, making treatment of MDR with MRP-specific reversal agents potentially feasible.
Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918.
It is concluded that the affinities of topoisomerase I drugs for BCRP are, in decreasing order: SN-38 > topotecan > 9-aminocamptothecin > CPT-11 > NX211 > DX8951f > BNP1350 • GF120918.
Characterization of the MRP4- and MRP5-mediated Transport of Cyclic Nucleotides from Intact Cells*
- P. Wielinga, I. van der Heijden, G. Reid, J. Beijnen, J. Wijnholds, P. Borst
- BiologyJournal of Biological Chemistry
- 16 May 2003
The data indicate that MRP4 and MRP5 are low affinity cyclic nucleotide transporters that may at best function as overflow pumps, decreasing steep increases in cGMP levels under conditions where cG MP synthesis is strongly induced and phosphodiesterase activity is limiting.