![[Feedback]](/icons/banner/feedbackACT.gif){kind=icon}
![[For Subscribers]](/icons/banner/subscriberACT.gif){kind=icon}
![[Archive]](/icons/banner/archiveACT.gif){kind=icon}
![[Search]](/icons/banner/searchACT.gif){kind=icon}
![[Contents]](/icons/banner/tocACT.gif){kind=icon}
|
|
|
|
|
||
JS Lee, K Paull, M Alvarez, C Hose, A Monks, M Grever, AT Fojo and SE Bates
Medicine Branch, National Cancer Institute, National Institutes of Health, Bethesda, Maryland 20892.
Fifty-eight cell lines in the National Cancer Institute drug screen were analyzed for their ability to efflux the fluorescent dye rhodamine 123 as a functional assay for P-glycoprotein (Pgp). Using flow cytometry, the rhodamine fluorescence was measured for each cell line under four incubation conditions, i.e., after accumulation in the presence or absence of the Pgp antagonist cyclosporin A and after efflux in rhodamine-free medium in the presence or absence of cyclosporin A. The results in some cell lines were compatible with Pgp- mediated efflux. There was a significant correlation between mdr-1 expression and rhodamine efflux in the 58 cell lines (r = 0.788, p = 0.0001). Using the rhodamine efflux data as a seed for COMPARE analysis with the cytotoxicity data on > 30,000 compounds in the National Cancer Institute drug screen database, hundreds of compounds with high correlation coefficients were identified. Selected compounds were tested for reversal of cross-resistance in a multidrug-resistant cell line. A high degree of reversibility, up to 10,000-fold, for some of the compounds was noted in the presence of the Pgp antagonist PSC 833. This finding suggested that compounds with predominately Pgp-mediated resistance were being identified. Using these compounds as seeds for COMPARE analysis against a more restricted database of 187 standard agents, a series of standard compounds were repeatedly identified as having high correlation coefficients with the newly identified Pgp substrates. These standard agents, including phyllanthoside, bisantrene, and homoharringtonine, constitute an mdr-1 profile. New agents identified as being highly correlated with these compounds may benefit from clinical trials with Pgp antagonists.
This article has been cited by other articles:
|
|
 |
|
  H. Liu, Y. Liu, and J.-T. Zhang A new mechanism of drug resistance in breast cancer cells: fatty acid synthase overexpression-mediated palmitate overproduction Mol. Cancer Ther., February 1, 2008; 7(2): 263 - 270. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 J. Xu, H. Peng, Q. Chen, Y. Liu, Z. Dong, and J.-T. Zhang Oligomerization Domain of the Multidrug Resistance-Associated Transporter ABCG2 and Its Dominant Inhibitory Activity Cancer Res., May 1, 2007; 67(9): 4373 - 4381. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 J. F. Deeken and W. Loscher The Blood-Brain Barrier and Cancer: Transporters, Treatment, and Trojan Horses Clin. Cancer Res., March 15, 2007; 13(6): 1663 - 1674. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. N. Weinstein Spotlight on molecular profiling: "Integromic" analysis of the NCI-60 cancer cell lines Mol. Cancer Ther., November 1, 2006; 5(11): 2601 - 2605. [Full Text] [PDF]
|
|
|
|
|
|
R. W. Robey, Z. Zhan, R. L. Piekarz, G. L. Kayastha, T. Fojo, and S. E. Bates Increased MDR1 Expression in Normal and Malignant Peripheral Blood Mononuclear Cells Obtained from Patients Receiving Depsipeptide (FR901228, FK228, NSC630176) Clin. Cancer Res., March 1, 2006; 12(5): 1547 - 1555. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 U. Henriksen, J. U. Fog, T. Litman, and U. Gether Identification of Intra- and Intermolecular Disulfide Bridges in the Multidrug Resistance Transporter ABCG2 J. Biol. Chem., November 4, 2005; 280(44): 36926 - 36934. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 E. S. Perloff, S. X. Duan, P. R. Skolnik, D. J. Greenblatt, and L. L. von Moltke ATAZANAVIR: EFFECTS ON P-GLYCOPROTEIN TRANSPORT AND CYP3A METABOLISM IN VITRO Drug Metab. Dispos., June 1, 2005; 33(6): 764 - 770. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 U. Henriksen, U. Gether, and T. Litman Effect of Walker A mutation (K86M) on oligomerization and surface targeting of the multidrug resistance transporter ABCG2 J. Cell Sci., April 1, 2005; 118(7): 1417 - 1426. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
J. P. Alao, E. W-F. Lam, S. Ali, L. Buluwela, W. Bordogna, P. Lockey, R. Varshochi, A. V. Stavropoulou, R. C. Coombes, and D. M. Vigushin Histone Deacetylase Inhibitor Trichostatin A Represses Estrogen Receptor {alpha}-Dependent Transcription and Promotes Proteasomal Degradation of Cyclin D1 in Human Breast Carcinoma Cell Lines Clin. Cancer Res., December 1, 2004; 10(23): 8094 - 8104. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
Y. Huang, P. Anderle, K. J. Bussey, C. Barbacioru, U. Shankavaram, Z. Dai, W. C. Reinhold, A. Papp, J. N. Weinstein, and W. Sadee Membrane Transporters and Channels: Role of the Transportome in Cancer Chemosensitivity and Chemoresistance Cancer Res., June 15, 2004; 64(12): 4294 - 4301. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 R. L. Piekarz, R. W. Robey, Z. Zhan, G. Kayastha, A. Sayah, A. H. Abdeldaim, S. Torrico, and S. E. Bates T-cell lymphoma as a model for the use of histone deacetylase inhibitors in cancer therapy: impact of depsipeptide on molecular markers, therapeutic targets, and mechanisms of resistance Blood, June 15, 2004; 103(12): 4636 - 4643. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. P. Jansen, C. E. Camalier, C. Stark, and N. H. Colburn Characterization of programmed cell death 4 in multiple human cancers reveals a novel enhancer of drug sensitivity Mol. Cancer Ther., February 1, 2004; 3(2): 103 - 110. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 T. Litman, T. Skovsgaard, and W. D. Stein Pumping of Drugs by P-Glycoprotein: A Two-Step Process? J. Pharmacol. Exp. Ther., December 1, 2003; 307(3): 846 - 853. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
S. Raje, J. Cao, A. H. Newman, H. Gao, and N. D. Eddington Evaluation of the Blood-Brain Barrier Transport, Population Pharmacokinetics, and Brain Distribution of Benztropine Analogs and Cocaine Using in Vitro and in Vivo Techniques J. Pharmacol. Exp. Ther., November 1, 2003; 307(2): 801 - 808. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. E. Goldsmith, M. Kitazono, P. Fok, T. Aikou, S. Bates, and T. Fojo The Histone Deacetylase Inhibitor FK228 Preferentially Enhances Adenovirus Transgene Expression in Malignant Cells Clin. Cancer Res., November 1, 2003; 9(14): 5394 - 5401. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
M. J. Peart, K. M. Tainton, A. A. Ruefli, A. E. Dear, K. A. Sedelies, L. A. O'Reilly, N. J. Waterhouse, J. A. Trapani, and R. W. Johnstone Novel Mechanisms of Apoptosis Induced by Histone Deacetylase Inhibitors Cancer Res., August 1, 2003; 63(15): 4460 - 4471. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
E. V. Batrakova, S. Li, V. Y. Alakhov, D. W. Miller, and A. V. Kabanov Optimal Structure Requirements for Pluronic Block Copolymers in Modifying P-glycoprotein Drug Efflux Transporter Activity in Bovine Brain Microvessel Endothelial Cells J. Pharmacol. Exp. Ther., February 1, 2003; 304(2): 845 - 854. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
L. Campbell, A.-N. G. Abulrob, L. E. Kandalaft, S. Plummer, A. J. Hollins, A. Gibbs, and M. Gumbleton Constitutive Expression of P-Glycoprotein in Normal Lung Alveolar Epithelium and Functionality in Primary Alveolar Epithelial Cultures J. Pharmacol. Exp. Ther., January 1, 2003; 304(1): 441 - 452. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
V. Sandor, S. Bakke, R. W. Robey, M. H. Kang, M. V. Blagosklonny, J. Bender, R. Brooks, R. L. Piekarz, E. Tucker, W. D. Figg, et al. Phase I Trial of the Histone Deacetylase Inhibitor, Depsipeptide (FR901228, NSC 630176), in Patients with Refractory Neoplasms Clin. Cancer Res., March 1, 2002; 8(3): 718 - 728. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 H. Ando, Y. Nishio, K. Ito, A. Nakao, L. Wang, Y. L. Zhao, K. Kitaichi, K. Takagi, and T. Hasegawa Effect of Endotoxin on P-Glycoprotein-Mediated Biliary and Renal Excretion of Rhodamine-123 in Rats Antimicrob. Agents Chemother., December 1, 2001; 45(12): 3462 - 3467. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
E. V. Batrakova, S. Li, S. V. Vinogradov, V. Y. Alakhov, D. W. Miller, and A. V. Kabanov Mechanism of Pluronic Effect on P-Glycoprotein Efflux System in Blood-Brain Barrier: Contributions of Energy Depletion and Membrane Fluidization J. Pharmacol. Exp. Ther., November 1, 2001; 299(2): 483 - 493. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
R. L. Piekarz, R. Robey, V. Sandor, S. Bakke, W. H. Wilson, L. Dahmoush, D. M. Kingma, M. L. Turner, R. Altemus, and S. E. Bates Inhibitor of histone deacetylation, depsipeptide (FR901228), in the treatment of peripheral and cutaneous T-cell lymphoma: a case report Blood, November 1, 2001; 98(9): 2865 - 2868. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
E. Stormer, M. D. Perloff, L. L. von Moltke, and D. J. Greenblatt Methadone Inhibits Rhodamine123 Transport in Caco-2 Cells Drug Metab. Dispos., July 1, 2001; 29(7): 954 - 956. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 D. E. Lorke, M. Krüger, R. Buchert, K. H. Bohuslavizki, M. Clausen, and U. Schumacher In Vitro and In Vivo Tracer Characteristics of an Established Multidrug-Resistant Human Colon Cancer Cell Line J. Nucl. Med., April 1, 2001; 42(4): 646 - 654. [Abstract] [Full Text]
|
|
|
|
|
|
L. J. Yu, J. Matias, D. A. Scudiero, K. M. Hite, A. Monks, E. A. Sausville, and D. J. Waxman P450 Enzyme Expression Patterns in the NCI Human Tumor Cell Line Panel Drug Metab. Dispos., March 1, 2001; 29(3): 304 - 312. [Abstract] [Full Text]
|
|
|
|
|
|
S. D. Mertins, T. G. Myers, M. Hollingshead, D. Dykes, E. Bodde, P. Tsai, C. A. Jefferis, R. Gupta, W. M. Linehan, M. Alley, et al. Screening for and Identification of Novel Agents Directed at Renal Cell Carcinoma Clin. Cancer Res., March 1, 2001; 7(3): 620 - 633. [Abstract] [Full Text]
|
|
|
|
|
|
R. Yumoto, T. Murakami, M. Sanemasa, R. Nasu, J. Nagai, and M. Takano Pharmacokinetic Interaction of Cytochrome P450 3A-Related Compounds with Rhodamine 123, a P-Glycoprotein Substrate, in Rats Pretreated with Dexamethasone Drug Metab. Dispos., February 1, 2001; 29(2): 145 - 151. [Abstract] [Full Text]
|
|
|
|
|
|
R. W. Robey, W. Y. Medina-Pérez, K. Nishiyama, T. Lahusen, K. Miyake, T. Litman, A. M. Senderowicz, D. D. Ross, and S. E. Bates Overexpression of the ATP-binding Cassette Half-Transporter, ABCG2 (MXR/BCRP/ABCP1), in Flavopiridol-resistant Human Breast Cancer Cells Clin. Cancer Res., January 1, 2001; 7(1): 145 - 152. [Abstract] [Full Text]
|
|
|
|
 |
|
 E. Bello-Reuss, S. Ernest, O. B. Holland, and M. R. Hellmich Role of multidrug resistance P-glycoprotein in the secretion of aldosterone by human adrenal NCI-H295 cells Am J Physiol Cell Physiol, June 1, 2000; 278(6): C1256 - C1265. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 S. Maesaki, P. Marichal, H. V. Bossche, D. Sanglard, and S. Kohno Rhodamine 6G efflux for the detection of CDR1-overexpressing azole-resistant Candida albicans strains J. Antimicrob. Chemother., July 1, 1999; 44(1): 27 - 31. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
R. Yumoto, T. Murakami, Y. Nakamoto, R. Hasegawa, J. Nagai, and M. Takano Transport of Rhodamine 123, a P-Glycoprotein Substrate, across Rat Intestine and Caco-2 Cell Monolayers in the Presence of Cytochrome P-450 3A-Related Compounds J. Pharmacol. Exp. Ther., April 1, 1999; 289(1): 149 - 155. [Abstract] [Full Text]
|
|
|
|
 |
|
 H.-M. Koo, M. Gray-Goodrich, G. Kohlhagen, M. J. McWilliams, M. Jeffers, A. Vaigro-Wolff, W. G. Alvord, A. Monks, K. D. Paull, Y. Pommier, et al. The ras Oncogene-Mediated Sensitization of Human Cells to Topoisomerase II Inhibitor-Induced Apoptosis J Natl Cancer Inst, February 3, 1999; 91(3): 236 - 244. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
R. Robey, S. Bakke, W. Stein, B. Meadows, T. Litman, S. Patil, T. Smith, T. Fojo, and S. Bates Efflux of Rhodamine From CD56+ Cells as a Surrogate Marker for Reversal of P-Glycoprotein-Mediated Drug Efflux by PSC 833 Blood, January 1, 1999; 93(1): 306 - 314. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 M. Alvarez, R. Robey, V. Sandor, K. Nishiyama, Y. Matsumoto, K. Paull, S. Bates, and T. Fojo Using the National Cancer Institute Anticancer Drug Screen to Assess the Effect of MRP Expression on Drug Sensitivity Profiles Mol. Pharmacol., November 1, 1998; 54(5): 802 - 814. [Abstract] [Full Text]
|
|
|
|
|
|
G. Kohlhagen, K. D. Paull, M. Cushman, P. Nagafuji, and Y. Pommier Protein-Linked DNA Strand Breaks Induced by NSC 314622, a Novel Noncamptothecin Topoisomerase I Poison Mol. Pharmacol., July 1, 1998; 54(1): 50 - 58. [Abstract] [Full Text]
|
|
|
|
|
|
G. Klopman, L. M. Shi, and A. Ramu Quantitative Structure-Activity Relationship of Multidrug Resistance Reversal Agents Mol. Pharmacol., August 1, 1997; 52(2): 323 - 334. [Abstract] [Full Text]
|
|
|
|
|
|
S. Scala, N. Akhmed, U. S. Rao, K. Paull, L.-B. Lan, B. Dickstein, J.-S. Lee, G. H. Elgemeie, W. D. Stein, and S. E. Bates P-Glycoprotein Substrates and Antagonists Cluster into Two Distinct Groups Mol. Pharmacol., June 1, 1997; 51(6): 1024 - 1033. [Abstract] [Full Text]
|
|
|
|
|
|
M. Kolaczkowski, M. van der Rest, A. Cybularz-Kolaczkowska, J.-P. Soumillion, W. N. Konings, and A. Goffeau Anticancer Drugs, Ionophoric Peptides, and Steroids as Substrates of the Yeast Multidrug Transporter Pdr5p J. Biol. Chem., December 6, 1996; 271(49): 31543 - 31548. [Abstract] [Full Text] [PDF]
|
|
 |
 |
 |
|
 |
 |
 |
