Development of novel, 384-well high-throughput assay panels for human drug transporters: Drug interaction and safety assessment in support of discovery research

Journal of Biomolecular Screening

Volumn 18, Issue 9, 2013, Pages 1072-1083

  Tang, Huaping ^a   Shen, Ding Ren ^a   Han, Yong Hae ^a   Kong, Yan ^a   Balimane, Praveen ^a   Marino, Anthony ^a   Gao, Mian ^a   Wu, Sophie ^a   Xie, Dianlin ^a   Soars, Matthew G ^a   O'Connell, Jonathan C ^a   Rodrigues, A David ^a   Zhang, Litao ^a   Cvijic, Mary Ellen ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

high throughput human drug transporter assays

Indexed keywords

BILE ACID; BILIRUBIN;

ARTICLE; AUTOMATION; BIOASSAY; CONTROLLED STUDY; DRUG INTERACTION; DRUG RESEARCH; DRUG SAFETY; FLUORESCENCE; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; PRIORITY JOURNAL; RISK ASSESSMENT; STRUCTURE ACTIVITY RELATION;

HIGH-THROUGHPUT HUMAN DRUG TRANSPORTER ASSAYS;

BIOLOGICAL TRANSPORT; CELL SURVIVAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG APPROVAL; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; DRUG INTERACTIONS; DRUGS, INVESTIGATIONAL; FLUORESCENT DYES; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; KIDNEY; LIVER; MEMBRANE TRANSPORT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84884642266     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057113494807     Document Type: Article

References (30)

1. Bahadduri P. M., Polli J. E., Swaan P. W., Ekins S.. Targeting Drug Transporters: Combining In Silico and In Vitro Approaches to Predict In Vivo. Methods Mol. Biol. 2010 ; 637: 65-103
2. Mizuno N., Niwa T., Yotsumoto Y., Sugiyama Y.. Impact of Drug Transporter Studies on Drug Discovery and Development. Pharmacol. Rev. 2003 ; 55: 425-461 (Pubitemid 37013212)
3. Maeda K., Sugiyama Y.. Impact of Genetic Polymorphisms of Transporters on the Pharmacokinetic, Pharmacodynamic and Toxicological Properties of Anionic Drugs. Drug Metab. Pharmacokinet. 2008 ; 23: 223-235
4. Giacomini K. M., Huang S. M., Tweedie D. J., et al. Membrane Transporters in Drug Development. Nat. Rev. Drug Discov. 2010 ; 9: 215-236
5. Guideline on the Investigation of Drug Interactions. London: European Medicines Agency ; 2010 :
6. Guidance for Industry Drug Interaction Studies - Study Design, Data Analysis, Implications for Dosing, and Labeling Recommendations. Rockville, MD: Food and Drug Administration ; 2012 :
7. Hagenbuch B.. Drug Uptake Systems in Liver and Kidney: A Historic Perspective. Clin. Pharmacol. Ther. 2010 ; 87: 39-47
8. Juliano R. L., Ling V.. A Surface Glycoprotein Modulating Drug Permeability in Chinese Hamster Ovary Cell Mutants. Biochim. Biophys. Acta. 1976 ; 455: 152-162
9. Hediger M. A., Coady M. J., Ikeda T. S., Wright E. M.. Expression Cloning and cDNA Sequencing of the Na+/Glucose Co-transporter. Nature. 1987 ; 330: 379-381 (Pubitemid 18045465)
10. Aller S. G., Yu J., Ward A., et al. Structure of P-glycoprotein Reveals a Molecular Basis for Poly-Specific Drug Binding. Science. 2009 ; 323: 1718-1722
11. Giacomini K. M., Sugiyama Y. Goodman & Gilman's The Pharmacological Basis of Therapeutics. 11 th ed., McGraw-Hill: New York, 2005; pp 41-70. New York: McGraw-Hill ; 2005: 41-70.
12. Sahi J.. Use of In Vitro Transporter Assays to Understand Hepatic and Renal Disposition of New Drug Candidates. Expert Opin. Drug Metab. Toxicol. 2005 ; 1: 409-427
13. Weinglass A. B., Garcia M. L., Kaczorowski G. L.. Technologies for Transporter Drug Discovery. Channels. 2008 ; 2: 312-321
14. Duan Z., Choy E., Hornicek F. J.. NSC23925, Identified in a High-Throughput Cell-Based Screen, Reverses Multidrug Resistance. PLoS One. 2009 ; 4: e7415
15. Gui C., Obaidat A., Chaguturu R., Hagenbuch B.. Development of a Cell-Based High-Throughput Assay to Screen for Inhibitors of Organic Anion Transporting Polypeptides 1B1 and 1B3. Curr. Chem. Genomics. 2010 ; 4: 1-8
16. Heredi-Szabo K., Kis E., Molnar E., Gyorfi A., Krajcsi P.. Characterization of 5(6)-carboxy-2′,7′-dichlorofluorescein Transport by MRP2 and Utilization of This Substrate as a Fluorescent Surrogate for LTC4. J. Biomol. Screen. 2008 ; 13: 295-301 (Pubitemid 351442761)
17. Karlsson J. E., Heddle C., Rozkov A., et al. High-Activity P-glycoprotein, Multidrug Resistance Protein 2, and Breast Cancer Resistance Protein Membrane Vesicles Prepared from Transiently Transfected Human Embryonic Kidney 293-Epstein-Barr Virus Nuclear Antigen Cells. Drug Metab. Dispos. 2010 ; 38: 705-714
18. Wu J., Wheeldon I., Guo Y., et al. A Sandwiched Microarray Platform for Benchtop Cell-Based High Throughput Screening. Biomaterials. 2011 ; 32: 841-848
19. Mita S., Suzuki H., Akita H., et al. Inhibition of Bile Acid Transport across Na+/Taurocholate Cotransporting Polypeptide (SLC10A1) and Bile Salt Export Pump (ABCB 11)-Coexpressing LLC-PK1 Cells by Cholestasis-Inducing Drugs. Drug Metab. Dispos. 2006 ; 34: 1575-1581 (Pubitemid 44285400)
20. Elsby R., Smith V., Fox L., et al. Validation of Membrane Vesicle-Based Breast Cancer Resistance Protein and Multidrug Resistance Protein 2 Assays to Assess Drug Transport and the Potential for Drug-Drug Interaction to Support Regulatory Submissions. Xenobiotica. 2011 ; 41: 764-783
21. Han Y. H., Busler D., Hong Y., et al. Transporter Studies with the 3-O-Sulfate Conjugate of 17alpha-Ethinylestradiol: Assessment of Human Liver Drug Transporters. Drug Metab. Dispos. 2010 ; 38: 1072-1082
22. Zhang J. H., Chung T. D., Oldenburg K. R.. A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays. J. Biomol. Screen. 1999 ; 4: 67-73 (Pubitemid 29278954)
23. Ahlin G., Hilgendorf C., Karlsson J., Szigyarto C. A., Uhlen M., Artursson P.. Endogenous Gene and Protein Expression of Drug-Transporting Proteins in Cell Lines Routinely Used in Drug Discovery Programs. Drug Metab. Dispos. 2009 ; 37: 2275-2283
24. Soars M. G., Barton P., Ismair M., et al. The Development, Characterization, and Application of an OATP1B1 Inhibition Assay in Drug Discovery. Drug Metab. Dispos. 2012 ; 40: 1641-168
25. Pepperkok R., Ellenberg J.. High-Throughput Fluorescence Microscopy for Systems Biology. Nat. Rev. Mol. Cell Biol. 2006 ; 7: 690-696 (Pubitemid 44268214)
26. Sarkadi B., Homolya L., Szakacs G., et al. Human Multidrug Resistance ABCB and ABCG Transporters: Participation in a Chemoimmunity Defense System. Physiol. Rev. 2006 ; 86: 1179-1236 (Pubitemid 44521651)
27. Tiberghien F., Wenandy T., Loor F.. The Potent Immunosuppressive Cyclosporin FR901459 Inhibits the Human P-glycoprotein and Formyl Peptide Receptor Functions. J. Antibiot. 2000 ; 53: 509-515 (Pubitemid 30345269)
28. Cvijic M. E., Chen J., Kubala S., et al. GPCR Assay Automation for Leveraging Lead Optimization. J. Lab. Autom. 2012 ; 17: 266-274
29. Zhang L., Cvijic M. E., Lippy J., et al. Case Study: Technology Initiative Led to Advanced Lead Optimization Screening Processes at Bristol-Myers Squibb, 2004-2009. Drug Discov. Today. 2012 ; 17: 733-740
30. Kim R. B.. Transporters and Drug Discovery: Why, When, and How. Mol. Pharm. 2006 ; 3: 26-32 (Pubitemid 43331748)