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Inhibition of poly(ADP-ribose) polymerase in tumors from BRCA mutation carriers.
TLDR
Olaparib has few of the adverse effects of conventional chemotherapy, inhibits PARP, and has antitumor activity in cancer associated with the BRCA1 or BRCa2 mutation. Expand
Potent and specific inhibition of the breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C.
TLDR
A new tetracyclic analogue of FTC, Ko143, is evaluated as a practical inhibitor of BCRP, proving highly active for increasing the intracellular drug accumulation and reversing Bcrp1/BCRP-mediated multidrug resistance. Expand
Subcellular localization and distribution of the breast cancer resistance protein transporter in normal human tissues.
TLDR
The apical localization in the epithelium of the small intestine and colon indicates a possible role of BCRP in the regulation of the uptake of p.o. delivered B CRP substrates by back-transport of substrate drugs entering from the gut lumen and is consistent with the hypothesis of a protective role ofBCRP for the fetus. Expand
An update on in vitro test methods in human hepatic drug biotransformation research: pros and cons.
TLDR
The practical aspects of selected in vitro human liver models are described and several more or less serious specific drawbacks for each model are described which prevents their widespread use and acceptance by the regulatory authorities as an alternative for in vivo screening. Expand
Photodynamic therapy in oncology.
TLDR
The data show that, when properly used, PDT is an effective alternative treatment option in oncology and is slowly gaining acceptance as an alternative to conventional cancer therapies. Expand
Evidence for Two Interacting Ligand Binding Sites in Human Multidrug Resistance Protein 2 (ATP Binding Cassette C2)*
TLDR
It is proposed that MRP2 contains two similar but nonidentical ligand binding sites: one site from which substrate is transported and a second site that regulates the affinity of the transport site for the substrate. Expand
Clinical Pharmacokinetics of Therapeutic Monoclonal Antibodies
TLDR
The parenteral administration, slow tissue distribution and long elimination half-life are the most pronounced clinical pharmacokinetic characteristics of mAbs. Expand
Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918.
TLDR
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. Expand
Piraña and PCluster: A modeling environment and cluster infrastructure for NONMEM
TLDR
A graphical user interface, Piraña, was developed that offers a complete modeling environment for NONMEM, enabling both novice and advanced users to increase efficiency of their workflow. Expand
Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918.
TLDR
Coadministration of the BCRP and P-gp inhibitor GF120918 resulted in a significant increase of the systemic exposure of oral topotecan. Expand
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