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1

Lemaire, Sandrine, Françoise Van Bambeke, Marie-Paule Mingeot-Leclercq, and Paul M. Tulkens. "Modulation of the Cellular Accumulation and Intracellular Activity of Daptomycin towards Phagocytized Staphylococcus aureus by the P-Glycoprotein (MDR1) Efflux Transporter in Human THP-1 Macrophages and Madin-Darby Canine Kidney Cells." Antimicrobial Agents and Chemotherapy 51, no. 8 (2007): 2748–57. http://dx.doi.org/10.1128/aac.00090-07.

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ABSTRACT P-glycoprotein (P-gp; MDR1), a major efflux transporter, recognizes various antibiotics and is present in macrophages. We have examined its effect on the modulation of the intracellular accumulation and activity of daptomycin towards phagocytized Staphylococcus aureus (ATCC 25923) in human THP-1 macrophages, in comparison with MDCK epithelial cells (wild type and MDCK-MDR1 overexpressing P-gp; the bulk of the protein was immunodetected at the surface of all three cell types). Daptomycin displayed concentration-dependent intracellular activity (Hill equation pattern) in THP-1 and MDCK
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Liu, Li-Li, Yong-Mei Guan, Xue-Ping Lu, Xin-Li Liang, and Li-Hua Chen. "Mechanisms of P-Glycoprotein Modulation by Semen Strychni Combined with Radix Paeoniae Alba." Evidence-Based Complementary and Alternative Medicine 2017 (2017): 1–8. http://dx.doi.org/10.1155/2017/1743870.

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Semen Strychni has been extensively used as a Chinese herb, but its therapeutic window is narrowed by the strong toxicity of the compound, which limits its effectiveness. Radix Paeoniae Alba has been reported to reduce the toxic effects and increase the therapeutic effects of Semen Strychni, but the underlying mechanism remains unknown. This research aimed to explore the mechanism through which P-glycoprotein (P-gp) is modulated by Semen Strychni combined with Radix Paeoniae Alba in vitro. An MTT assay was used to study cytotoxicity in an MDCK-MDR1 cell model. Rh123 efflux and accumulation wer
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Ceckova, Martina, Josef Reznicek, Zuzana Ptackova, et al. "Role of ABC and Solute Carrier Transporters in the Placental Transport of Lamivudine." Antimicrobial Agents and Chemotherapy 60, no. 9 (2016): 5563–72. http://dx.doi.org/10.1128/aac.00648-16.

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ABSTRACTLamivudine is one of the antiretroviral drugs of choice for the prevention of mother-to-child transmission (MTCT) in HIV-positive women. In this study, we investigated the relevance of drug efflux transporters P-glycoprotein (P-gp) (MDR1 [ABCB1]), BCRP (ABCG2), MRP2 (ABCC2), and MATE1 (SLC47A1) for the transmembrane transport and transplacental transfer of lamivudine. We employedin vitroaccumulation and transport experiments on MDCK cells overexpressing drug efflux transporters,in situ-perfused rat term placenta, and vesicular uptake in microvillous plasma membrane (MVM) vesicles isola
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Liu, Yun-Feng, Yong-Mei Guan, Shi-Yu Huang, Lu Wu, Wei-Feng Zhu, and Li-Hua Chen. "The Influence and Mechanism of Paeoniflorin and Albiflorin on Strychnine and Brucine Transport Through Madin-Darby Canine Kidney/Multidrug Resistance1 Cells In Vitro Model." Journal of Biobased Materials and Bioenergy 14, no. 5 (2020): 616–23. http://dx.doi.org/10.1166/jbmb.2020.1998.

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This research sought to study the influence and potentialmechanism of paeoniflorin and albiflorin on strychnine and brucine transport in MDCK-MDR1 cells regulated by P-gp. Cytotoxicity of drugs was tested by MTT assay, and the transport studies were performed in both directions in MDCK-MDR1 cells. The influence of drugs on P-gp ATPase, and the efflux function of P-gp, the expression levels of P-gp and MDR1 mRNA were also estimated. Strychnine and brucine showed well absorption, and the main transport mechanism might be passive diffusion. Verapamil could significantly decrease the efflux rate (
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Zhang, Miao, Lin Guo, Long-Fei Lin, et al. "Absorption Characteristics of Combination Medication of Realgar and Indigo Naturalis: In Vitro Transport across MDCK-MDR1 Cells and In Vivo Pharmacokinetics in Mice after Oral Administration." Evidence-Based Complementary and Alternative Medicine 2018 (September 6, 2018): 1–10. http://dx.doi.org/10.1155/2018/6493630.

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Realgar and indigo naturalis are clinically combined to treat varieties of leukemia. Exploring the drug-drug interactions might be beneficial to find active substances and develop new targeted drugs. This study aimed at exploring the change of arsenic concentration in mice and across MDCK-MDR1 cells and the cytotoxicity on K562 cells when realgar and indigo naturalis were combined. In the presence or absence of indigo naturalis, pharmacokinetics and cell-based permeability assays were used to evaluate the change of arsenic concentration, and K562 cell line was applied to evaluate the change of
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LIU, Qiang, XiaoLing GAO, YiFeng CHAI, GuoRong FAN, Jun CHEN, and ZhanYing HONG. "Transmembrane transport mechanism of tetrahydropalmatine in MDCK-MDR1 cell line." Pharmaceutical Care and Research 12, no. 1 (2012): 34–37. http://dx.doi.org/10.5428/pcar20120110.

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de Souza, Jacqueline, Leslie Z. Benet, Yong Huang, and Sílvia Storpirtis. "Comparison of bidirectional lamivudine and zidovudine transport using MDCK, MDCK–MDR1, and Caco-2 cell monolayers." Journal of Pharmaceutical Sciences 98, no. 11 (2009): 4413–19. http://dx.doi.org/10.1002/jps.21744.

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Liu, Yun-Feng, Yong-Mei Guan, Shi-Yu Huang, Lu Wu, Wei-Feng Zhu, and Li-Hua Chen. "Paeoniflorin and albiflorin regulate P-gp-mediated aconitine and hypaconitine transport through an Madin Darby canine kidney-multi drug resistance protein 1 cell model." Materials Express 11, no. 8 (2021): 1394–401. http://dx.doi.org/10.1166/mex.2021.2051.

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Aconitine and hypaconitine are the main active ingredients of Radix Aconiti, paeoniflorin and albiflorin are the primary components of Radix Paeoniae Alba. Both Radix Aconiti and Radix Paeoniae Alba are herbs that are commonly used in traditional Chinese medicine. This study sought to explore the mechanistic transport of aconitine and hypaconitine across MDCK-MDR1 cells and to assess the effect of paeoniflorin and albiflorin on aconitine and hypaconitine transmembrane transport as a potential attenuation mechanism. Drug cytotoxicity was tested via the MTT (3-(4,5-Dimethylthiazol-2-yl)-2,5-diph
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Dong, Wei, Zhen-Gen Liao, Guo-Wei Zhao, et al. "Reversal Effect of Oxypeucedanin on P-glycoprotein-mediated Drug Transport." Molecules 23, no. 8 (2018): 1841. http://dx.doi.org/10.3390/molecules23081841.

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P-glycoprotein affects the transport of numerous drugs including chemotherapeutic drugs vincristine sulfate (VCR) and docetaxel (DTX), and is one of the main causes for multidrug resistance. Our previous studies have shown that oxypeucedanin (OPD) can enhance the intestinal transit of puerarin and VCR. However, the underlying mechanism is unclear. This study investigated the potential mechanism by which OPD improves P-gp-mediated drug transport. Molecular docking was performed to predict the binding force between OPD and P-gp and the contribution of OPD on P-gp activity. We observed the effect
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Feng, Bo, Mark West, Nandini C. Patel, et al. "Validation of Human MDR1-MDCK and BCRP-MDCK Cell Lines to Improve the Prediction of Brain Penetration." Journal of Pharmaceutical Sciences 108, no. 7 (2019): 2476–83. http://dx.doi.org/10.1016/j.xphs.2019.02.005.

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Sawamoto, T., T. Van Gelder, U. Christians, N. Okamura, W. Jacobsen, and L. Benet. "Membrane transport of mycophenolate mofetil and its active metabolite, mycophenolic acid in MDCK and MDR1-MDCK cell monolayers." Journal of Heart and Lung Transplantation 20, no. 2 (2001): 234–35. http://dx.doi.org/10.1016/s1053-2498(00)00525-8.

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Simoff, Ivailo, Maria Karlgren, Maria Backlund, et al. "Complete Knockout of Endogenous Mdr1 (Abcb1) in MDCK Cells by CRISPR-Cas9." Journal of Pharmaceutical Sciences 105, no. 2 (2016): 1017–21. http://dx.doi.org/10.1016/s0022-3549(15)00171-9.

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Liang, Xin-li, Tao Tang, Guo-wei Zhao, et al. "Mechanism underlying bergapten-mediated regulation of vincristine transport in MDCK-MDR1 cells." Chinese Herbal Medicines 10, no. 3 (2018): 255–62. http://dx.doi.org/10.1016/j.chmed.2018.06.003.

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Zhang, Lin, Shouying Du, Yang Lu, et al. "Influence of puerarin, paeoniflorin, and menthol on structure and barrier function of tight junctions in MDCK and MDCK-MDR1 Cells." Journal of Traditional Chinese Medical Sciences 2, no. 2 (2015): 111–19. http://dx.doi.org/10.1016/j.jtcms.2016.01.008.

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Karyekar, Chetan S., Natalie D. Eddington, Tushar S. Garimella, Paul O. Gubbins, and Thomas C. Dowling. "Evaluation of P-glycoprotein–Mediated Renal Drug Interactions in an MDR1-MDCK Model." Pharmacotherapy 23, no. 4 (2003): 436–42. http://dx.doi.org/10.1592/phco.23.4.436.32125.

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Sánchez-Dengra, Bárbara, Isabel Gonzalez-Alvarez, Marival Bermejo, and Marta Gonzalez-Alvarez. "Physiologically Based Pharmacokinetic (PBPK) Modeling for Predicting Brain Levels of Drug in Rat." Pharmaceutics 13, no. 9 (2021): 1402. http://dx.doi.org/10.3390/pharmaceutics13091402.

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One of the main obstacles in neurological disease treatment is the presence of the blood–brain barrier. New predictive high-throughput screening tools are essential to avoid costly failures in the advanced phases of development and to contribute to the 3 Rs policy. The objective of this work was to jointly develop a new in vitro system coupled with a physiological-based pharmacokinetic (PBPK) model able to predict brain concentration levels of different drugs in rats. Data from in vitro tests with three different cells lines (MDCK, MDCK-MDR1 and hCMEC/D3) were used together with PK parameters
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Yang, Sihyung, Tanja Wenzler, Patrik N. Miller, et al. "Pharmacokinetic Comparison To Determine the Mechanisms Underlying the Differential Efficacies of Cationic Diamidines against First- and Second-Stage Human African Trypanosomiasis." Antimicrobial Agents and Chemotherapy 58, no. 7 (2014): 4064–74. http://dx.doi.org/10.1128/aac.02605-14.

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ABSTRACTHuman African trypanosomiasis (HAT), a neglected tropical disease, is fatal without treatment. Pentamidine, a cationic diamidine, has been used to treat first-stage (hemolymphatic) HAT since the 1940s, but it is ineffective against second-stage (meningoencephalitic, or central nervous system [CNS]) infection. Novel diamidines (DB75, DB820, and DB829) have shown promising efficacy in both mouse and monkey models of first-stage HAT. However, only DB829 cured animals with second-stage infection. In this study, we aimed to determine the mechanisms underlying the differential efficacies of
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Yang, Bing, Shouying Du, Yang Lu, et al. "Influence of paeoniflorin and menthol on puerarin transport across MDCK and MDCK-MDR1 cells as blood-brain barrier in vitro model." Journal of Pharmacy and Pharmacology 70, no. 3 (2017): 349–60. http://dx.doi.org/10.1111/jphp.12853.

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Chen, Zhen-Zhen, Yang Lu, Shou-Ying Du, Ke-Xin Shang, and Cheng-Bo Cai. "Influence of borneol and muscone on geniposide transport through MDCK and MDCK-MDR1 cells as blood–brain barrier in vitro model." International Journal of Pharmaceutics 456, no. 1 (2013): 73–79. http://dx.doi.org/10.1016/j.ijpharm.2013.08.017.

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Navarro, C., I. González-Álvarez, M. González-Álvarez, et al. "Influence of polyunsaturated fatty acids on Cortisol transport through MDCK and MDCK-MDR1 cells as blood–brain barrier in vitro model." European Journal of Pharmaceutical Sciences 42, no. 3 (2011): 290–99. http://dx.doi.org/10.1016/j.ejps.2010.12.005.

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Thomas, Julia, Lihui Wang, Richard E. Clark, and Munir Pirmohamed. "Active transport of imatinib into and out of cells: implications for drug resistance." Blood 104, no. 12 (2004): 3739–45. http://dx.doi.org/10.1182/blood-2003-12-4276.

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Imatinib is a tyrosine kinase inhibitor that is effective in the treatment of chronic myeloid leukemia (CML). Not all patients achieve cytogenetic response. Some patients even lose the initial cytogenetic response. In this study, we investigated the active cellular transport of imatinib to gain a better understanding of the possible mechanisms of imatinib resistance. We used the leukemic cell line CCRFCEM and its drug-resistant subline VBL100 to measure the uptake of carbon 14 (14C)-labeled imatinib. Imatinib uptake was temperature dependent, indicative of an active uptake process. Additionall
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Karlgren, Maria, Ivailo Simoff, Maria Backlund, et al. "A CRISPR-Cas9 Generated MDCK Cell Line Expressing Human MDR1 Without Endogenous Canine MDR1 ( cABCB1 ): An Improved Tool for Drug Efflux Studies." Journal of Pharmaceutical Sciences 106, no. 9 (2017): 2909–13. http://dx.doi.org/10.1016/j.xphs.2017.04.018.

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Crowe, Andrew. "P-Glycoprotein-Mediated Efflux Using a Rapidly Maturing Caco2 Clone (CLEFF4) in Only 5 Days without Requiring Modified Growth Medium." SLAS DISCOVERY: Advancing the Science of Drug Discovery 26, no. 1 (2020): 151–60. http://dx.doi.org/10.1177/2472555220942758.

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In drug discovery it is essential that one of the parameters tested for any new chemical entity is its affinity for human efflux systems, most notably P-glycoprotein (P-gp). These efflux systems affect not only rates of oral absorption but also rates of excretion through the liver, blood–brain barrier, and accumulation in potential target cells that upregulate efflux systems. Current methods to determine drugs’ P-gp transport potential include in vitro bidirectional transport studies, and the two most common cell lines used are Caco2 and MDR1-transfected MDCK models. Caco2 cells are human but
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Barthomeuf, Chantal, Michel Demeule, Jérôme Grassi, Ashraf Saidkhodjaev, and Richard Beliveau. "Conferone from Ferula schtschurowskiana Enhances Vinblastine Cytotoxicity in MDCK-MDR1 Cells by Competitively Inhibiting P-Glycoprotein Transport." Planta Medica 72, no. 7 (2006): 634–39. http://dx.doi.org/10.1055/s-2006-931574.

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Pastan, I., M. M. Gottesman, K. Ueda, E. Lovelace, A. V. Rutherford, and M. C. Willingham. "A retrovirus carrying an MDR1 cDNA confers multidrug resistance and polarized expression of P-glycoprotein in MDCK cells." Proceedings of the National Academy of Sciences 85, no. 12 (1988): 4486–90. http://dx.doi.org/10.1073/pnas.85.12.4486.

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Luo, Shuanghui, Zhiying Wang, Viral Kansara, Dhananjay Pal, and Ashim K. Mitra. "Activity of a sodium-dependent vitamin C transporter (SVCT) in MDCK-MDR1 cells and mechanism of ascorbate uptake." International Journal of Pharmaceutics 358, no. 1-2 (2008): 168–76. http://dx.doi.org/10.1016/j.ijpharm.2008.03.002.

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Jin, Xiannu, Thu-Lan Luong, Necole Reese, et al. "Comparison of MDCK-MDR1 and Caco-2 cell based permeability assays for anti-malarial drug screening and drug investigations." Journal of Pharmacological and Toxicological Methods 70, no. 2 (2014): 188–94. http://dx.doi.org/10.1016/j.vascn.2014.08.002.

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ZAHNER, D., J. ALBER, and E. PETZINGER. "Cloning and heterologous expression of the ovine (Ovis aries) P-glycoprotein (Mdr1) in Madin-Darby canine kidney (MDCK) cells." Journal of Veterinary Pharmacology and Therapeutics 33, no. 3 (2010): 304–11. http://dx.doi.org/10.1111/j.1365-2885.2009.01141.x.

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Raggers, René J., Ilse Vogels, and Gerrit van Meer. "Upregulation of the expression of endogenous Mdr1 P-glycoprotein enhances lipid translocation in MDCK cells transfected with human MRP2." Histochemistry and Cell Biology 117, no. 2 (2001): 181–85. http://dx.doi.org/10.1007/s00418-001-0352-4.

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Yang, Xi, Zhiyuan Ma, Sisi Zhou, et al. "Multiple Drug Transporters Are Involved in Renal Secretion of Entecavir." Antimicrobial Agents and Chemotherapy 60, no. 10 (2016): 6260–70. http://dx.doi.org/10.1128/aac.00986-16.

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ABSTRACTEntecavir (ETV) is a first-line antiviral agent for the treatment of chronic hepatitis B virus infection. Renal excretion is the major elimination path of ETV, in which tubular secretion plays the key role. However, the secretion mechanism has not been clarified. We speculated that renal transporters mediated the secretion of ETV. Therefore, the aim of our study was to elucidate which transporters contribute to the renal disposition of ETV. Our results revealed that ETV (50 μM) remarkably reduced the accumulation of probe substrates in MDCK cells stably expressing human multidrug and t
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Ho, Norman F. H., James Nielsen, Michelle Peterson, and Philip S. Burton. "Quantitative and Mechanistic Assessment of Model Lipophilic Drugs in Micellar Solutions in the Transport Kinetics Across MDR1-MDCK Cell Monolayers." Journal of Pharmaceutical Sciences 105, no. 2 (2016): 904–14. http://dx.doi.org/10.1016/j.xphs.2015.11.028.

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Luo, Shuanghui, Viral S. Kansara, Xiaodong Zhu, Nanda K. Mandava, Dhananjay Pal, and Ashim K. Mitra. "Functional Characterization of Sodium-Dependent Multivitamin Transporter in MDCK-MDR1 Cells and Its Utilization as a Target for Drug Delivery." Molecular Pharmaceutics 3, no. 3 (2006): 329–39. http://dx.doi.org/10.1021/mp0500768.

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KAMAU, SARAH W., STEFANIE D. KRÄMER, MAJA GÜNTHERT, and HEIDI WUNDERLI-ALLENSPACH. "EFFECT OF THE MODULATION OF THE MEMBRANE LIPID COMPOSITION ON THE LOCALIZATION AND FUNCTION OF P-GLYCOPROTEIN IN MDR1-MDCK CELLS." In Vitro Cellular & Developmental Biology - Animal 41, no. 7 (2005): 207. http://dx.doi.org/10.1290/0502016.1.

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Wegler, Christine, Meryem Gazit, Karolina Issa, Sujay Subramaniam, Per Artursson, and Maria Karlgren. "Expanding the Efflux In Vitro Assay Toolbox: A CRISPR-Cas9 Edited MDCK Cell Line with Human BCRP and Completely Lacking Canine MDR1." Journal of Pharmaceutical Sciences 110, no. 1 (2021): 388–96. http://dx.doi.org/10.1016/j.xphs.2020.09.039.

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Soldner, Andrea, Leslie Z. Benet, Ernst Mutschler, and Uwe Christians. "Active transport of the angiotensin-II antagonist losartan and its main metabolite EXP 3174 across MDCK-MDR1 and Caco-2 cell monolayers." British Journal of Pharmacology 129, no. 6 (2000): 1235–43. http://dx.doi.org/10.1038/sj.bjp.0703150.

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Tang, Fuxing, Hui Ouyang, Jerry Z. Yang, and Ronald T. Borchardt. "Bidirectional transport of rhodamine 123 and Hoechst 33342, fluorescence probes of the binding sites on P-glycoprotein, across MDCK–MDR1 cell monolayers." Journal of Pharmaceutical Sciences 93, no. 5 (2004): 1185–94. http://dx.doi.org/10.1002/jps.20046.

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Li, Jibin, Ying Wang, and Ismael J. Hidalgo. "Kinetic Analysis of Human and Canine P-Glycoprotein-Mediated Drug Transport in MDR1-MDCK Cell Model: Approaches to Reduce False-Negative Substrate Classification." Journal of Pharmaceutical Sciences 102, no. 9 (2013): 3436–46. http://dx.doi.org/10.1002/jps.23523.

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Zheng, Qin, Yu Tang, Peng-Yi Hu, et al. "The influence and mechanism of ligustilide, senkyunolide I, and senkyunolide A on echinacoside transport through MDCK-MDR1 cells as blood-brain barrier in vitro model." Phytotherapy Research 32, no. 3 (2017): 426–35. http://dx.doi.org/10.1002/ptr.5985.

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Hellinger, Éva, Szilvia Veszelka, Andrea E. Tóth, et al. "Comparison of brain capillary endothelial cell-based and epithelial (MDCK-MDR1, Caco-2, and VB-Caco-2) cell-based surrogate blood–brain barrier penetration models." European Journal of Pharmaceutics and Biopharmaceutics 82, no. 2 (2012): 340–51. http://dx.doi.org/10.1016/j.ejpb.2012.07.020.

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Lagas, Jurjen S., Rolf W. Sparidans, Robert A. B. van Waterschoot, Els Wagenaar, Jos H. Beijnen, and Alfred H. Schinkel. "P-Glycoprotein Limits Oral Availability, Brain Penetration, and Toxicity of an Anionic Drug, the Antibiotic Salinomycin." Antimicrobial Agents and Chemotherapy 52, no. 3 (2007): 1034–39. http://dx.doi.org/10.1128/aac.01041-07.

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ABSTRACT Salinomycin is a polyether organic anion that is extensively used as a coccidiostatic antibiotic in poultry and commonly fed to ruminant animals to improve feed efficiency. However, salinomycin also causes severe toxicity when accidentally fed to animals in high doses. In addition, humans are highly sensitive to salinomycin and severe toxicity has been reported. Multidrug efflux transporters like P-glycoprotein (P-gp), BCRP, and MRP2 are highly expressed in the intestine and can restrict the oral uptake and tissue penetration of xenobiotics. The purpose of this study was to investigat
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Hu, Peng-Yi, Dan Liu, Qin Zheng, Qing Wu, Yu Tang, and Ming Yang. "Elucidation of Transport Mechanism of Paeoniflorin and the Influence of Ligustilide, Senkyunolide I and Senkyunolide A on Paeoniflorin Transport through Mdck-Mdr1 Cells as Blood–Brain Barrier in Vitro Model." Molecules 21, no. 3 (2016): 300. http://dx.doi.org/10.3390/molecules21030300.

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Mease, Kirsten, Rucha Sane, Lalitha Podila, and Mitchell E. Taub. "Differential Selectivity of Efflux Transporter Inhibitors in Caco-2 and MDCK–MDR1 Monolayers: A Strategy to Assess the Interaction of a New Chemical Entity with P-gp, BCRP, and MRP2." Journal of Pharmaceutical Sciences 101, no. 5 (2012): 1888–97. http://dx.doi.org/10.1002/jps.23069.

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Saaby, Lasse, Peer Tfelt-Hansen, and Birger Brodin. "The putative P-gp inhibitor telmisartan does not affect the transcellular permeability and cellular uptake of the calcium channel antagonist verapamil in the P-glycoprotein expressing cell line MDCK II MDR1." Pharmacology Research & Perspectives 3, no. 4 (2015): e00151. http://dx.doi.org/10.1002/prp2.151.

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Rowbottom, Christopher, Alicia Pietrasiewicz, Elvana Viezaj, et al. "P131 - Optimization and validation of rodent chemical knock out model for P-glycoprotein using the selective inhibitor, valspodar, and application to internal cut-off values and calibration of MDCK-MDR1 Cell line." Drug Metabolism and Pharmacokinetics 35, no. 1 (2020): S62. http://dx.doi.org/10.1016/j.dmpk.2020.04.132.

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Annabi, Borhane, Michel Demeule, Jean-Christophe Currie, Alain Larocque, Cyndia Charfi, and Richard Béliveau. "Increasing potency and safety of anticancer drugs through sortilin receptor-mediated cancer therapy: A new targeted approach for the treatment of ovarian cancer." Journal of Clinical Oncology 37, no. 15_suppl (2019): e17068-e17068. http://dx.doi.org/10.1200/jco.2019.37.15_suppl.e17068.

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e17068 Background: The development of personalized therapies against ovarian cancer remains highly challenging in current modern oncology. One strategy to achieve greater selectivity and better anticancer drug delivery into cancer cells is to conjugate cytotoxic agents to specific peptide ligands that selectively target receptors abundantly and/or exclusively expressed on these cells. Increased expression of Sortilin, a scavenging receptor, has been clinically observed in invasive ovarian cancer biopsies, and correlated with tumor grades. In light of this, we developed a peptide conjugation pl
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Reznicek, Josef, Martina Ceckova, Zuzana Ptackova, et al. "MDR1 and BCRP Transporter-Mediated Drug-Drug Interaction between Rilpivirine and Abacavir and Effect on Intestinal Absorption." Antimicrobial Agents and Chemotherapy 61, no. 9 (2017). http://dx.doi.org/10.1128/aac.00837-17.

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ABSTRACT Rilpivirine (TMC278) is a highly potent nonnucleoside reverse transcriptase inhibitor (NNRTI) representing an effective component of combination antiretroviral therapy (cART) in the treatment of HIV-positive patients. Many antiretroviral drugs commonly used in cART are substrates of ATP-binding cassette (ABC) and/or solute carrier (SLC) drug transporters and, therefore, are prone to pharmacokinetic drug-drug interactions (DDIs). The aim of our study was to evaluate rilpivirine interactions with abacavir and lamivudine on selected ABC and SLC transporters in vitro and assess its import
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Zhang, Cheng-Yue, and Xiao-Da yang. "Effects of herbal aromatics on the permeability of MDCK-MDR1 monolayers." Journal of Chinese Pharmaceutical Sciences 20, no. 6 (2011). http://dx.doi.org/10.5246/jcps.2011.06.075.

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C. L. Lam, Kevin, and Ganesh Rajaraman. "Assessment of P‐Glycoprotein Substrate and Inhibition Potential of Test Compounds in MDR1‐Transfected MDCK Cells." Current Protocols in Pharmacology 58, no. 1 (2012). http://dx.doi.org/10.1002/0471141755.ph0713s58.

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Zhao, Jing, Ting Zhou, Jing-Ze Lu, et al. "Intra-Herb Interactions: Primary Metabolites in Coptidis Rhizoma Extract Improved the Pharmacokinetics of Oral Berberine Hydrochloride in Mice." Frontiers in Pharmacology 12 (June 7, 2021). http://dx.doi.org/10.3389/fphar.2021.675368.

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Primary plant metabolites can be used for artificial preparation of natural deep eutectic solvents (NADESs), which have strong dissolving capacity, good biocompatibility, and biodegradability. In this study, for the first time, we verified that NADESs were present in Coptidis Rhizoma extract and systematically investigated its effects and mechanisms on the pharmacokinetics of oral berberine hydrochloride (BBR), a co-existing bioactive constituent. First, three LC-MS/MS based methods were established and fully validated to determine the levels of 11 primary metabolites in Coptidis Rhizoma extra
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Kamau, Sarah, Stefanie KrÃ?mer, Maja GÃ?nthert, and Heidi Wunderli-Allenspach. "Effect of the modulation of the membrane lipid composition on the localization and function of P-glycoprotein in mdr1-MDCK cells." In Vitro Cellular and Developmental Biology--Animal, 2005. http://dx.doi.org/10.1290/0502016.

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