Membrane transporters in drug development
- K. Giacomini, Shiew-Mei Huang, Lei Zhang
- Biology, MedicineNature reviews. Drug discovery
- 1 March 2010
Overall, it is advised that the timing of transporter investigations should be driven by efficacy, safety and clinical trial enrolment questions, as well as a need for further understanding of the absorption, distribution, metabolism and excretion properties of the drug molecule, and information required for drug labelling.
Conjugate export pumps of the multidrug resistance protein (MRP) family: localization, substrate specificity, and MRP2-mediated drug resistance.
- J. König, A. Nies, Y. Cui, I. Leier, D. Keppler
- BiologyBiochimica et Biophysica Acta
- 6 December 1999
Drug resistance and ATP-dependent conjugate transport mediated by the apical multidrug resistance protein, MRP2, permanently expressed in human and canine cells.
- Y. Cui, J. König, J. Buchholz, H. Spring, I. Leier, D. Keppler
- Biology, ChemistryMolecular Pharmacology
- 1 May 1999
The cloned MRP2 (symbol ABCC2), a MRP family member localized to the apical membrane of polarized cells, demonstrates that MRP 2 confers resistance to cytotoxic drugs.
Localization and Genomic Organization of a New Hepatocellular Organic Anion Transporting Polypeptide*
- J. König, Yunhai Cui, A. Nies, D. Keppler
- BiologyJournal of Biological Chemistry
- 28 July 2000
Human OATP8 is a new uptake transporter in the basolateral hepatocyte membrane with an overlapping but distinct substrate specificity as compared with OATp2, which is localized to the same membrane domain.
A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane.
- J. König, Y. Cui, A. Nies, D. Keppler
- Biology, ChemistryAmerican Journal of Physiology - Gastrointestinal…
- 2000
The results indicate that OATP2 is important for the uptake of organic anions, including bilirubin conjugates and sulfobromophthalein, in human liver.
Hepatic Uptake of Bilirubin and Its Conjugates by the Human Organic Anion Transporter SLC21A6*
- Yunhai Cui, J. König, I. Leier, U. Buchholz, D. Keppler
- Biology, MedicineJournal of Biological Chemistry
- 30 March 2001
Human OATP2 may play a key role in the prevention of hyperbilirubinemia by facilitating the selective entry of unconjugated bilirubin and its glucuronate conjugates into human hepatocytes.
The MRP gene encodes an ATP-dependent export pump for leukotriene C4 and structurally related conjugates.
- I. Leier, G. Jedlitschky, U. Buchholz, S. Cole, R. Deeley, D. Keppler
- Biology, ChemistryJournal of Biological Chemistry
- 11 November 1994
The Multidrug Resistance Protein 5 Functions as an ATP-dependent Export Pump for Cyclic Nucleotides*
- G. Jedlitschky, B. Burchell, D. Keppler
- BiologyJournal of Biological Chemistry
- 29 September 2000
Evidence is provided that cyclic nucleotides are physiological substrates for MRP5 and may represent a novel pharmacological target for the enhancement of tissue levels of cGMP.
cDNA Cloning of the Hepatocyte Canalicular Isoform of the Multidrug Resistance Protein, cMrp, Reveals a Novel Conjugate Export Pump Deficient in Hyperbilirubinemic Mutant Rats*
- M. Büchler, J. König, D. Keppler
- BiologyJournal of Biological Chemistry
- 21 June 1996
The results identify cMrp as a canalicular transport protein with a novel sequence and with a function similar to the one of the MRP.
Cotransport of reduced glutathione with bile salts by MRP4 (ABCC4) localized to the basolateral hepatocyte membrane
- M. Rius, A. Nies, J. Hummel‐Eisenbeiss, G. Jedlitschky, D. Keppler
- Biology, MedicineHepatology
- 1 August 2003
It is found that MRP4 can mediate the efflux of GSH from hepatocytes into blood by cotransport with monoanionic bile salts and may function as an overflow pathway during impaired bile salt secretion across the canalicular membrane into bile.
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