A high throughput flow cytometric assay platform targeting transporter inhibition

Drug Discovery Today: Technologies

Volumn 12, Issue , 2014, Pages

  Tegos, George P ^a,b,c,d   Evangelisti, Annette M ^a   Strouse, J Jacob ^a   Ursu, Oleg ^a,e   Bologa, Cristian ^a,e   Sklar, Larry A ^a,b  

^a UNIVERSITY OF NEW MEXICO   (United States)

^b UNIVERSITY OF NEW MEXICO SCHOOL OF MEDICINE   (United States)

^c MASSACHUSETTS GENERAL HOSPITAL   (United States)

^d HARVARD MEDICAL SCHOOL   (United States)

^e UNIVERSITY OF NEW MEXICO HEALTH SCIENCES CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ABC TRANSPORTER; MOLECULAR LIBRARY;

ARTICLE; ASSAY; CHEMISTRY; EFFUSION; FLOW CYTOMETRY; HIGH THROUGHPUT SCREENING; MAMMAL; MOLECULE; NONHUMAN; YEAST; ANIMAL; ANTAGONISTS AND INHIBITORS; DRUG DEVELOPMENT; ENZYME SPECIFICITY; HUMAN; MOLECULAR LIBRARY; PHARMACOLOGY; PROCEDURES; TRANSPORT AT THE CELLULAR LEVEL;

ANIMALS; ATP-BINDING CASSETTE TRANSPORTERS; BIOLOGICAL TRANSPORT; DRUG DISCOVERY; FLOW CYTOMETRY; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; SMALL MOLECULE LIBRARIES; SUBSTRATE SPECIFICITY;

EID: 84901196769     PISSN: None     EISSN: 17406749     Source Type: Journal    
DOI: 10.1016/j.ddtec.2014.03.010     Document Type: Review

References (48)

1. A. Palmeira, E. Sousa, M.H. Vasconcelos, and M.M. Pinto Three decades of P-gp inhibitors: skimming through several generations and scaffolds Curr Med Chem 19 2012 1946 2025
2. C. Kourtesi, A.R. Ball, Y.Y. Huang, S.M. Jachak, D.M. Vera, and P. Khondkar et al. Microbial efflux systems and inhibitors: approaches to drug discovery and the challenge of clinical implementation Open Microbiol J 7 2013 34 52
3. M. Dean, A. Rzhetsky, and R. Allikmets The human ATP-binding cassette (ABC) transporter superfamily Genome Res 11 2001 1156 1166
4. J.I. Fletcher, M. Haber, M.J. Henderson, and M.D. Norris ABC transporters in cancer: more than just drug efflux pumps Nat Rev Cancer 10 2010 147 156
5. D. Rees, E. Johnson, and O. Lewinson ABC transporters: the power to change Nat Rev Mol Cell Biol 10 2009 218 227
6. Q. Ren, and I.T. Paulsen Comparative analyses of fundamental differences in membrane transport capabilities in prokaryotes and eukaryotes PLoS Comput Biol 3 2005 e27
7. B. Goldman Multidrug resistance: can new drugs help chemotherapy score against cancer? J Natl Cancer Inst 95 2003 255 257
8. R. Krishna, and L.D. Mayer Multidrug resistance (MDR) in cancer. Mechanisms, reversal using modulators of MDR and the role of MDR modulators in influencing the pharmacokinetics of anticancer drugs Eur J Pharm Sci 11 2000 265 283
9. B. Sarkadi, L. Homolya, G. Szakacs, and A. Varadi Human multidrug resistance ABCB and ABCG transporters: participation in a chemoimmunity defense system Physiol Rev 86 2006 1179 1236
10. L. Su, D.D. Mruk, W.Y. Lui, W.M. Lee, and C.Y. Cheng P-glycoprotein regulates blood-testis barrier dynamics via its effects on the occludin/zonula occludens 1 (ZO-1) protein complex mediated by focal adhesion kinase (FAK) Proc Natl Acad Sci U S A 108 2011 19623 19628
11. International Transporter Consortium GK, S.M. Huang, D.J. Tweedie, L.Z. Benet, K.L. Brouwer, and X. Chu et al. Membrane transporters in drug development Nat Rev Drug Discov 9 2010 215 236
12. Y. Lai, and P. Hsiao Beyond the ITC White Paper: emerging sciences in drug transporters and opportunities for drug development Curr Pharm Des 2013 [Epub ahead of print]
13. A. Tamaki, C. Ierano, G. Szakacs, R.W. Robey, and S.E. Bates The controversial role of ABC transporters in clinical oncology Essays Biochem 50 2011 209 232
14. G. Tegos, M. Haynes, J.J. Strouse, M.M.T. Khan, C.G. Bologa, and T.I. Oprea et al. Microbial efflux inhibition: tactics & strategies Curr Pharm Des 17 2011 1291 1302
15. H. Nikaido, and J.M. Pagès Broad-specificity efflux pumps and their role in multidrug resistance of Gram-negative bacteria FEMS Microbiol Rev 36 2012 340 363
16. M. Falasca, and K.J. Linton Investigational ABC transporter inhibitors Expert Opin Investig Drugs 21 2012 657 666
17. G. Szakacs, A. Varadi, C. Ozvegy-Laczka, and B. Sarkadi The role of ABC transporters in drug absorption, distribution, metabolism, excretion and toxicity (ADME-Tox) Drug Discov Today 13 2008 379 393
18. P. Eckford, and F.J. Sharom ABC efflux pump-based resistance to chemotherapy drugs Chem Rev 109 2009 2989 3011
19. G. Szakacs, J.K. Paterson, J.A. Ludwig, C. Booth-Genthe, and M.M. Gottesman Targeting multidrug resistance in cancer Nat Rev Drug Discov 5 2006 219 234
20. R. Robey, S. Shukla, E.M. Finley, R.K. Oldham, D. Barnett, and S.V. Ambudkar et al. Inhibition of P-glycoprotein (ABCB1)- and multidrug resistance-associated protein 1 (ABCC1)-mediated transport by the orally administered inhibitor, CBT-1((R)) Biochem Pharmacol 75 2008 1302 1312
21. Y. Li, J.L. Revalde, G. Reid, and J.W. Paxton Modulatory effects of curcumin on multi-drug resistance-associated protein 5 in pancreatic cancer cells Cancer Chemother Pharmacol 68 2011 603 610
22. J. Campanale, and A. Hamdoun Programmed reduction of ABC transporter activity in sea urchin germline progenitors Development 139 2012 783 792
23. V. Mamidipudi, T. Shi, H. Brady, S. Surapaneni, R. Chopra, and S.L. Aukerman et al. Increased cellular accumulation and distribution of amrubicin contribute to its activity in anthracycline-resistant cancer cells Cancer Chemother Pharmacol 69 2012 965 976
24. I. Lebedeva, P. Pande, and W.F. Patton Sensitive and specific fluorescent probes for functional analysis of the three major types of mammalian ABC transporters PLoS ONE 6 2011 e22429
25. L. Di, C. Whitney-Pickett, J.P. Umland, H. Zhang, X. Zhang, and D.F. Gebhard et al. Development of a new permeability assay using low-efflux MDCKII cells J Pharm Sci 100 2011 4974 4985
26. A. Golebiewska, N.H. Brons, R. Bjerkvig, and S.P. Niclou Critical appraisal of the side population assay in stem cell and cancer stem cell research Cell Stem Cell 8 2011 136 147
27. X. Xia, J. Yang, F. Li, Y. Li, X. Zhou, and Y. Dai et al. Image-based chemical screening identifies drug efflux inhibitors in lung cancer cells Cancer Res 70 2010 7723 7733
28. S. Shukla, A.P. Skoumbourdis, M.J. Walsh, A.M. Hartz, K.L. Fung, and C.P. Wu et al. Synthesis and characterization of a BODIPY conjugate of the BCR-ABL kinase inhibitor Tasigna (nilotinib): evidence for transport of Tasigna and its fluorescent derivative by ABC drug transporters Mol Pharm 8 2011 1292 1302
29. J. Pedersen, P. Matsson, C.A. Bergström, U. Norinder, J. Hoogstraate, and P. Artursson Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2) J Med Chem 51 2008 3275 3287
30. Z. Bikadi, I. Hazai, D. Malik, K. Jemnitz, Z. Veres, and P. Hari et al. Predicting P-glycoprotein-mediated drug transport based on support vector machine and three-dimensional crystal structure of P-glycoprotein PLoS ONE 6 2011 e25815
31. G. Sager, E. Orvoll, R. Lysaa, I. Kufareva, R. Abagyan, and A.W. Ravna Novel cGMP efflux inhibitors - identified by virtual ligand screening (VLS) and confirmed by experimental studies J Med Chem 55 2012 3049 3057
32. E. Dolghih, C. Bryant, A.R. Renslo, and M.P. Jacobson Predicting binding to P-glycoprotein by flexible receptor docking PLoS Comput Biol 7 2011 e1002083
33. P. Crivori, B. Reinach, D. Pezzetta, and I. Poggesi Computational models for identifying potential P-glycoprotein substrates and inhibitors Mol Pharm 3 2006 33 44
34. P. Kannan, S. Telu, S. Shukla, S.V. Ambudkar, V.W. Pike, and C. Halldin et al. The specific P-glycoprotein inhibitor Tariquidar is also a substrate and an inhibitor for breast cancer resistance protein (BCRP/ABCG2) ACS Chem Neurosci 2 2011 82 89
35. V. Poongavanam, N. Haider, and G.F. Ecker Fingerprint-based in silico models for the prediction of P-glycoprotein substrates and inhibitors Bioorg Med Chem 20 2012 5388 5395
36. F. Broccatelli, G. Cruciani, L.Z. Benet, and T.I. Oprea BDDCS class prediction for new molecular entities Mol Pharm 9 2012 570 580
37. B. Edwards, F.W. Kuckuck, E.R. Prossnitz, J.T. Ransom, and L.A. Sklar HTPS flow cytometry: a novel platform for automated high throughput drug discovery and characterization J Biomol Screen 6 2001 83 90
38. S. Winter, D.M. Lovato, H.M. Khawaja, B.S. Edwards, I.D. Steele, and S.M. Young et al. High-throughput screening for daunorubicin-mediated drug resistance identifies mometasone furoate as a novel ABCB1-reversal agent J Biomol Screen 13 2008 185 193
39. I. Ivnitski-Steele, R.S. Larson, D.M. Lovato, H.M. Khawaja, S.S. Winter, and T.I. Oprea et al. High-throughput flow cytometry to detect selective inhibitors of ABCB1, ABCC1, and ABCG2 transporters Assay Drug Dev Technol 2 2008 263 276
40. I. Ivnitski-Steele, A.R. Holmes, E. Lamping, B.C. Monk, R.D. Cannon, and L.A. Sklar Identification of Nile red as a fluorescent substrate of the Candida albicans ATP-binding cassette transporters Cdr1p and Cdr2p and the major facilitator superfamily transporter Mdr1p Anal Biochem 394 2009 87 91
41. A. Holmes, M.V. Keniya, I. Ivnitski-Steele, B.C. Monk, E. Lamping, and L.A. Sklar et al. The monoamine oxidase A inhibitor clorgyline is a broad-spectrum inhibitor of fungal ABC and MFS transporter efflux pump activities which reverses the azole resistance of Candida albicans and Candida glabrata clinical isolates Antimicrob Agents Chemother 56 2012 1508 1515
42. NIH Molecular Libraries Selective Efflux Inhibition of ATP-binding Cassette Sub-family G Member 2. Chapter ML230 IN Probe Reports from the Molecular Libraries Program [Internet] NLo
43. J.J. Strouse, I. Ivnitski-Steele, H.M. Khawaja, D. Perez, J. Ricci, and T. Yao et al. A selective ATP-binding cassette subfamily G member 2 efflux inhibitor revealed via high-throughput flow cytometry J Biomol Screen 18 2013 26 38
44. C. Chan, C. Prudom, S.M. Raines, S. Charkhzarrin, S.D. Melman, and L.P. De Haro et al. Inhibitors of V-ATPase proton transport reveal uncoupling functions of tether linking cytosolic and membrane domains of V0 subunit a (Vph1p) J Biol Chem 287 2012 10236 10250
45. P. Nordmann, T. Naas, N. Fortineau, and L. Poirel Superbugs in the coming new decade; multidrug resistance and prospects for treatment of Staphylococcus aureus, Enterococcus spp. and Pseudomonas aeruginosa in 2010 Curr Opin Microbiol 10 2007 436 440
46. L. Dijkshoorn, A. Nemec, and H. Seifert An increasing threat in hospitals: multidrug-resistant Acinetobacter baumannii Nat Rev Microbiol 5 2007 939 951
47. P. Polireddy, MMd.T. Khan, H. Chavan, S. Young, X. Ma, and A. Waller et al. A novel HTS flow cytometric assay reveals functional modulators of the ATP binding cassette transporter ABCB6 PLoS ONE 7 2012 e40005
48. R. Johnson, C. Allen, S.D. Melman, A. Waller, S.M. Young, and L.A. Sklar et al. Identification of inhibitors of vacuolar proton-translocating ATPase pumps in yeast by high-throughput screening flow cytometry Anal Biochem 398 2010 203 211