Abcb1a

Summary

Gene Symbol: Abcb1a
Description: ATP-binding cassette, sub-family B (MDR/TAP), member 1A
Alias: Abcb4, Evi32, Mdr1a, Mdr3, P-gp, Pgp, Pgy-3, Pgy3, mdr-3, multidrug resistance protein 1A, ATP-binding cassette sub-family B member 1A, ATP-binding cassette, sub-family B (MDR/TAP), member 4, ATP-binding cassette, subfamily B, member 1A, P-glycoprotein 3, ecotropic viral integration site 32, multi-drug resistance 3, multidrug resistance protein 3, multiple drug resistant 1a
Species: mouse

Top Publications

  1. ncbi P-glycoprotein deficiency in a subpopulation of CF-1 mice enhances avermectin-induced neurotoxicity
    G R Lankas
    Department of Safety Assessment, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    Toxicol Appl Pharmacol 143:357-65. 1997
  2. ncbi Identification of a P-glycoprotein-deficient subpopulation in the CF-1 mouse strain using a restriction fragment length polymorphism
    D R Umbenhauer
    Department of Safety Assessment, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    Toxicol Appl Pharmacol 146:88-94. 1997
  3. ncbi Structural and functional analyses of the promoter of the murine multidrug resistance gene mdr3/mdr1a reveal a negative element containing the AP-1 binding site
    M Ikeguchi
    Department of Molecular Pathology, University of Texas, M D Anderson Cancer Center, Houston 77030
    DNA Cell Biol 10:639-49. 1991
  4. doi Preservation of transendothelial glucose transporter 1 and P-glycoprotein transporters in a cortical slice culture model of the blood-brain barrier
    R S Camenzind
    Section of Functional Neuroanatomy, Institute of Anatomy, Department of Biomedicine, University of Basel, Pestalozzistrasse 20, CH 4056 Basel, Switzerland
    Neuroscience 170:361-71. 2010
  5. pmc Two members of the mouse mdr gene family confer multidrug resistance with overlapping but distinct drug specificities
    A Devault
    Department of Biochemistry, McGill University, Montreal, Quebec, Canada
    Mol Cell Biol 10:1652-63. 1990
  6. pmc The three mouse multidrug resistance (mdr) genes are expressed in a tissue-specific manner in normal mouse tissues
    J M Croop
    Department of Pediatric Hematology and Oncology, Childrens Hospital, Boston, Massachusetts
    Mol Cell Biol 9:1346-50. 1989
  7. pmc Absence of the mdr1a P-Glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A
    A H Schinkel
    The Netherlands Cancer Institute, Division of Molecular Biology, Amsterdam, The Netherlands
    J Clin Invest 96:1698-705. 1995
  8. ncbi Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs
    A H Schinkel
    Division of Molecular Biology, The Netherlands Cancer Institute, Amsterdam
    Cell 77:491-502. 1994
  9. pmc P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs
    A H Schinkel
    The Netherlands Cancer Institute, Division of Molecular Biology, 1066 CX Amsterdam, The Netherlands
    J Clin Invest 97:2517-24. 1996
  10. ncbi What have we learnt thus far from mice with disrupted P-glycoprotein genes?
    P Borst
    Division of Molecular Biology, Netherlands Cancer Institute
    Eur J Cancer 32:985-90. 1996

Scientific Experts

Detail Information

Publications118 found, 100 shown here

  1. ncbi P-glycoprotein deficiency in a subpopulation of CF-1 mice enhances avermectin-induced neurotoxicity
    G R Lankas
    Department of Safety Assessment, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    Toxicol Appl Pharmacol 143:357-65. 1997
    ....
  2. ncbi Identification of a P-glycoprotein-deficient subpopulation in the CF-1 mouse strain using a restriction fragment length polymorphism
    D R Umbenhauer
    Department of Safety Assessment, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
    Toxicol Appl Pharmacol 146:88-94. 1997
    ..Sensitive "-/-" animals are deficient in P-glycoprotein in those tissues known to express primarily mdr1a, but have normal P-glycoprotein levels in tissues known to express primarily mdr1b or mdr2, suggesting that the ..
  3. ncbi Structural and functional analyses of the promoter of the murine multidrug resistance gene mdr3/mdr1a reveal a negative element containing the AP-1 binding site
    M Ikeguchi
    Department of Molecular Pathology, University of Texas, M D Anderson Cancer Center, Houston 77030
    DNA Cell Biol 10:639-49. 1991
    We have previously shown that the multidrug-resistance/P-glycoprotein gene, mdr3/mdr1a, is activated in mouse hepatocellular carcinomas (HCC)...
  4. doi Preservation of transendothelial glucose transporter 1 and P-glycoprotein transporters in a cortical slice culture model of the blood-brain barrier
    R S Camenzind
    Section of Functional Neuroanatomy, Institute of Anatomy, Department of Biomedicine, University of Basel, Pestalozzistrasse 20, CH 4056 Basel, Switzerland
    Neuroscience 170:361-71. 2010
    ..Our results provide evidence that endothelial transporters and their functional properties can be maintained in organotypic cortical slices cultures, thus making it an attractive model system for the study of the blood-brain barrier...
  5. pmc Two members of the mouse mdr gene family confer multidrug resistance with overlapping but distinct drug specificities
    A Devault
    Department of Biochemistry, McGill University, Montreal, Quebec, Canada
    Mol Cell Biol 10:1652-63. 1990
    We report the cloning and functional analysis of a complete clone for the third member of the mouse mdr gene family, mdr3. Nucleotide and predicted amino acid sequence analyses showed that the three mouse mdr genes encode highly ..
  6. pmc The three mouse multidrug resistance (mdr) genes are expressed in a tissue-specific manner in normal mouse tissues
    J M Croop
    Department of Pediatric Hematology and Oncology, Childrens Hospital, Boston, Massachusetts
    Mol Cell Biol 9:1346-50. 1989
    ..5, 5, and 6 kilobases have been detected. Each of the mdr genes has a specific RNA transcript pattern. These results should be considered in relation to understanding the normal physiological function of the mdr multigene family...
  7. pmc Absence of the mdr1a P-Glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A
    A H Schinkel
    The Netherlands Cancer Institute, Division of Molecular Biology, Amsterdam, The Netherlands
    J Clin Invest 96:1698-705. 1995
    We have previously shown that absence of the mouse mdr1a (also called mdr3) P-glycoprotein in mdr1a (-/-) "knockout" mice has a profound effect on the tissue distribution and elimination of vinblastine and ivermectin, and hence on the ..
  8. ncbi Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs
    A H Schinkel
    Division of Molecular Biology, The Netherlands Cancer Institute, Amsterdam
    Cell 77:491-502. 1994
    We have generated mice homozygous for a disruption of the mdr1a (also called mdr3) gene, encoding a drug-transporting P-glycoprotein...
  9. pmc P-glycoprotein in the blood-brain barrier of mice influences the brain penetration and pharmacological activity of many drugs
    A H Schinkel
    The Netherlands Cancer Institute, Division of Molecular Biology, 1066 CX Amsterdam, The Netherlands
    J Clin Invest 97:2517-24. 1996
    The mouse mdr1a (also called mdr3) P-GP is abundant in the blood-brain barrier, and its absence in mdr1a (-/-) mice leads to highly increased levels of the drugs ivermectin, vinblastine, digoxin, and cyclosporin A in the brain...
  10. ncbi What have we learnt thus far from mice with disrupted P-glycoprotein genes?
    P Borst
    Division of Molecular Biology, Netherlands Cancer Institute
    Eur J Cancer 32:985-90. 1996
  11. ncbi MDR1 P-glycoprotein is a lipid translocase of broad specificity, while MDR3 P-glycoprotein specifically translocates phosphatidylcholine
    A van Helvoort
    Department of Cell Biology, Faculty of Medicine and Institute of Biomembranes, Universiteit Utrecht, The Netherlands
    Cell 87:507-17. 1996
    The human MDR1 P-glycoprotein (Pgp) extrudes a variety of drugs across the plasma membrane. The homologous MDR3 Pgp is required for phosphatidylcholine secretion into bile...
  12. pmc Normal viability and altered pharmacokinetics in mice lacking mdr1-type (drug-transporting) P-glycoproteins
    A H Schinkel
    Division of Molecular Biology, The Netherlands Cancer Institute, Amsterdam
    Proc Natl Acad Sci U S A 94:4028-33. 1997
    ..roles, we have generated mice genetically deficient in the mdr1b gene [mdr1b (-/-) mice] and in both the mdr1a and mdr1b genes [mdr1a/1b (-/-) mice]...
  13. ncbi A novel model of inflammatory bowel disease: mice deficient for the multiple drug resistance gene, mdr1a, spontaneously develop colitis
    C M Panwala
    Department of Molecular Immunology, Immunex Corporation, Seattle, WA 98101, USA
    J Immunol 161:5733-44. 1998
    The murine multiple drug resistance (mdr) gene, mdr1a, encodes a 170-kDa transmembrane protein that is expressed in many tissues including intestinal epithelial cells, a subset of lymphoid cells and hematopoietic cells...
  14. ncbi mdr1a-encoded P-glycoprotein is not required for peripheral T cell proliferation, cytokine release, or cytotoxic effector function in mice
    M D Eisenbraun
    Cellular and Molecular Biology Graduate Program, Department of Pathology, University of Michigan School of Medicine, Ann Arbor 48109, USA
    J Immunol 163:2621-7. 1999
    ..Protein expression and rhodamine-123 efflux studies revealed that peripheral T cells exclusively utilize the mdr1a-encoded isoform rather than the homologous mdr1b or mdr2 isoforms...
  15. ncbi Altered expression of hepatic cytochromes P-450 in mice deficient in one or more mdr1 genes
    E G Schuetz
    Department of Pharmaceutical Sciences, St Jude Children s Research Hospital, Memphis, Tennessee, USA
    Mol Pharmacol 57:188-97. 2000
    ..We began with variants of a CF-1 mouse strain containing a defective mdr1a gene that is inherited in a Mendelian fashion...
  16. pmc Multidrug resistance protein 1 protects the choroid plexus epithelium and contributes to the blood-cerebrospinal fluid barrier
    J Wijnholds
    Division of Molecular Biology and Center for Biomedical Genetics, The Netherlands Cancer Institute, 1066 CX Amsterdam, The Netherlands
    J Clin Invest 105:279-85. 2000
    ..Here, we generated Mrp1/Mdr1a/Mdr1b triple-knockout (TKO) mice, and used them together with Mdr1a/Mdr1b double-knockout (DKO) mice to study the ..
  17. ncbi P-Glycoprotein, a gatekeeper in the blood-brain barrier
    - Schinkel
    Division of Experimental Therapy, The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands
    Adv Drug Deliv Rev 36:179-194. 1999
    ..The clinical application of P-glycoprotein blockers should also be considered in order to improve the blood-brain barrier permeability of certain drugs that currently display insufficient brain penetration for effective therapy...
  18. ncbi The pharmacological phenotype of combined multidrug-resistance mdr1a/1b- and mrp1-deficient mice
    D R Johnson
    Department of Pharmacology and Developmental Therapeutics Program, Cancer Center and Section of Comparative Medicine, Yale University School of Medicine, New Haven, Connecticut 06520, USA
    Cancer Res 61:1469-76. 2001
    ..transporters to the toxicity of cancer chemotherapy agents, we have used mice genetically deficient in both the mdr1a and mdr1b genes [mdr1a/1b(-/-) mice], the mrp1 gene [mrp1(-/-) mice], and the combined genes mdr1a/1b and mrp1 [..
  19. ncbi P-glycoprotein expression in mouse brain increases with maturation
    Catherine E Tsai
    Department of Pediatrics, Magee Womens Hospital Research Institute, University of Pittsburgh School of Medicine, 300 Halket Street, Pittsburgh, PA 15213, USA
    Biol Neonate 81:58-64. 2002
    The mdr1a isoform of P-glycoprotein (Pgp) is an integral plasma membrane efflux pump expressed in adult brain capillary endothelial cells and astrocytes of the blood-brain barrier...
  20. ncbi Penetration of endogenous steroid hormones corticosterone, cortisol, aldosterone and progesterone into the brain is enhanced in mice deficient for both mdr1a and mdr1b P-glycoproteins
    M Uhr
    Max Planck Institute of Psychiatry, Munich, Germany
    J Neuroendocrinol 14:753-9. 2002
    ..We used mice deficient for both murine mdr1a and mdr1b P-gps [mdr1a/1b(-/-)] to determine the uptake of [3H]-cortisol, [3H]-corticosterone, [3H]-aldosterone ..
  21. ncbi ABCB1 (MDR1)-type P-glycoproteins at the blood-brain barrier modulate the activity of the hypothalamic-pituitary-adrenocortical system: implications for affective disorder
    Marianne B Muller
    Max Planck Institute of Psychiatry, Kraepelinstrasse 2 10, 80804 Munich, Germany
    Neuropsychopharmacology 28:1991-9. 2003
    ....
  22. ncbi Contribution of the ABC transporters Bcrp1 and Mdr1a/1b to the side population phenotype in mammary gland and bone marrow of mice
    Johan W Jonker
    Division of Experimental Therapy, The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands
    Stem Cells 23:1059-65. 2005
    ..The ATP-binding cassette transporters Bcrp1 (Abcg2) and Mdr1a/1b (Abcb1a/1b) have been implicated as being responsible for this phenotype...
  23. ncbi Differential, strain-specific cellular and subcellular distribution of multidrug transporters in murine choroid plexus and blood-brain barrier
    A Soontornmalai
    University of Zurich, Institute of Pharmacology and Toxicology, Winterthurerstrasse 190, CH 8057 Zurich, Switzerland
    Neuroscience 138:159-69. 2006
    ..Analysis of Mdr1a(0/0) and Mrp1(0/0) mice, generated in the FVB strain, revealed no major alteration in expression of the remaining ..
  24. pmc A revised role for P-glycoprotein in the brain distribution of dexamethasone, cortisol, and corticosterone in wild-type and ABCB1A/B-deficient mice
    Brittany L Mason
    Pharmaceutical Science Research Division, King s College London, London, UK
    Endocrinology 149:5244-53. 2008
    ..Therefore, our current understanding of the role of P-gp in hypothalamic-pituitary-adrenal regulation in mice requires revision...
  25. pmc Structure of P-glycoprotein reveals a molecular basis for poly-specific drug binding
    Stephen G Aller
    Department of Molecular Biology, Scripps Research Institute, 10550 North Torrey Pines Road, CB105, La Jolla, CA 92037, USA
    Science 323:1718-22. 2009
    ..The inward-facing conformation represents an initial stage of the transport cycle that is competent for drug binding...
  26. ncbi P-glycoprotein and breast cancer resistance protein affect disposition of tandutinib, a tyrosine kinase inhibitor
    Johnny J Yang
    Drug Metabolism and Pharmacokinetics, Millennium Pharmaceuticals Inc, Takeda Oncology Company, 40 Landsdowne Street, Cambridge, MA 02139, USA
    Drug Metab Lett 4:201-12. 2010
    ..In mice, after intravenous administration of tandutinib, the mean plasma AUC values in the Bcrp1(-/-) mice and Mdr1a/b(-/-) mice was 1.53- and 1.20-fold greater than that of the wild type (WT) mice, respectively...
  27. pmc Cerebral amyloid-β proteostasis is regulated by the membrane transport protein ABCC1 in mice
    Markus Krohn
    Department of Neurology, Neurodegeneration Research Laboratory, University of Rostock, Rostock, Germany
    J Clin Invest 121:3924-31. 2011
    ..Thus, by altering the temporal aggregation profile of Aβ, pharmacological activation of ABC transporters could impede the neurodegenerative cascade that culminates in the dementia of AD...
  28. ncbi Transbilayer movement of NBD-labeled phospholipids in red blood cell membranes: outward-directed transport by the multidrug resistance protein 1 (MRP1)
    D W Dekkers
    Department of Biochemistry, Cardiovascular Research Institute Maastricht, Maastricht University, The Netherlands
    Biochemistry 37:14833-7. 1998
    ..Experiments with RBC from knock-out mice for multidrug resistance P-glycoproteins (Mdr1a/1b-/- and Mdr2-/-) and multidrug resistance protein 1 (Mrp1-/-) revealed that Mrp1 is responsible for the observed ..
  29. ncbi Properties of P-glycoprotein with mutations in the "catalytic carboxylate" glutamate residues
    Gregory Tombline
    Department of Biochemistry and Biophysics, University of Rochester Medical Center, Rochester, New York 14642, USA
    J Biol Chem 279:46518-26. 2004
    ..Here the role of these residues (Glu-552 and Glu-1197 in mouse MDR3 Pgp) was studied further. Mutation E552Q or E1197Q reduced Pgp-ATPase to low but still measurable rates...
  30. ncbi The multidrug resistance gene mdr1a influences resistance to ectromelia virus infection by mechanisms other than conventional immunity
    Dongmei Xu
    Division of Immunology and Genetics, John Curtin School of Medical Research, Australian National University, Canberra, ACT 2601
    Immunol Cell Biol 82:462-70. 2004
    ..We employed mdr1a gene knock out (mdr1a-/-) mice and ectromelia virus (EV) to elucidate the role of P-gp in resistance to EV...
  31. ncbi Mammalian multidrug resistance gene: complete cDNA sequence indicates strong homology to bacterial transport proteins
    P Gros
    Cell 47:371-80. 1986
    ..We propose that an energy-dependent transport mechanism is responsible for the multidrug-resistant phenotype...
  32. ncbi Multidrug resistance and the role of P-glycoprotein knockout mice
    A H Schinkel
    The Netherlands Cancer Institute, Division of Molecular Biology, Amsterdam, The Netherlands
    Eur J Cancer 31:1295-8. 1995
    ..effects of the blocking of this protein, we have generated mice with a genetic disruption of the drug-transporting mdr1a P-glycoprotein...
  33. ncbi Genetic dissection of the function of mammalian P-glycoproteins
    P Borst
    The Netherlands Cancer Institute, Department of Molecular Biology, Amsterdam, The Netherlands
    Trends Genet 13:217-22. 1997
    ..Recent experiments with polarized cells support the idea that drug-transporting P-glycoproteins act by flipping drugs from the inner to the outer leaflet of the plasma membrane...
  34. ncbi Development of an in situ mouse brain perfusion model and its application to mdr1a P-glycoprotein-deficient mice
    C Dagenais
    Division of Drug Delivery and Disposition, School of Pharmacy, University of North Carolina at Chapel Hill, USA
    J Cereb Blood Flow Metab 20:381-6. 2000
    ..of passive and carrier-mediated transport across the blood-brain barrier (BBB) was developed and applied to mdr1a P-glycoprotein (Pgp)-deficient mice [mdr1a(-/-)]. Cerebral flow was estimated from diazepam uptake...
  35. ncbi Neither lipophilicity nor membrane-perturbing potency of phenothiazine maleates correlate with the ability to inhibit P-glycoprotein transport activity
    Andrzej B Hendrich
    Department of Biophysics Wrocław Medical University ul Chalubinskiego 10 50 368 Wrocław, Poland
    Mol Membr Biol 20:53-60. 2003
    ..No clear relation was found between effects exerted by phenothiazine maleates on model membranes and their ability to modulate P-glycoprotein transport activity...
  36. ncbi P-glycoprotein-mediated multidrug resistance phenotype of L1210/VCR cells is associated with decreases of oligo- and/or polysaccharide contents
    R Fiala
    Institute of Molecular Physiology and Genetics, Slovak Academy of Sciences, Vlarska 5, 83334 Bratislava, Slovak Republic
    Biochim Biophys Acta 1639:213-24. 2003
    ..drug-sensitive L1210 cells to vincristine) is associated with overexpression of mdr1 gene product P-glycoprotein (Pgp)-the ATP-dependent drug efflux pump...
  37. ncbi Synergy between conserved ABC signature Ser residues in P-glycoprotein catalysis
    Gregory Tombline
    Department of Biochemistry and Biophysics, University of Rochester Medical Center, Rochester, New York 14642, USA
    J Biol Chem 279:5363-73. 2004
    ..Because the transition state complex is currently believed to form in the dimerized state of the nucleotide binding domains, one may also conclude that both Ser-OH are necessary for correct formation of the dimer state...
  38. ncbi The ABC transporter structure and mechanism: perspectives on recent research
    P M Jones
    Department of Cell and Molecular Biology, University of Technology Sydney, Broadway, NSW, Australia
    Cell Mol Life Sci 61:682-99. 2004
    ....
  39. ncbi The important role of Bcrp (Abcg2) in the biliary excretion of sulfate and glucuronide metabolites of acetaminophen, 4-methylumbelliferone, and harmol in mice
    Maciej J Zamek-Gliszczynski
    University of North Carolina School of Pharmacy, Chapel Hill, NC 27599 7360, USA
    Mol Pharmacol 70:2127-33. 2006
    ..and glucuronide (4MUG), and harmol sulfate (HS) and glucuronide (HG) was studied in Abcc2(-/-), Abcg2(-/-), and Abcb1a(-/-)/Abcb1b(-/-) mouse livers perfused with the respective parent compounds using a cassette dosing approach...
  40. ncbi Disposition of the cholesterol absorption inhibitor ezetimibe in mdr1a/b (-/-) mice
    Stefan Oswald
    Department of Clinical Pharmacology, University of Greifswald, Friedrich Loeffler Strasse 23d, Greifswald, Germany
    J Pharm Sci 96:3478-84. 2007
    ..In brief, serum concentrations, organ distribution and elimination of EZ were determined in 10 male wild-type and mdr1a/b (-/-) mice after oral treatment with EZ (10 mg/kg, 10 days)...
  41. ncbi P-glycoprotein has negligible effects on estradiol and testosterone in mice
    Martin Ebinger
    Max Planck Institute of Psychiatry, 80804 Munich, Germany
    Neurosci Lett 427:6-9. 2007
    ..The organ/plasma quotients showed no significant group effects. We concluded that P-gp does not influence the penetration of testosterone and estradiol to a biologically significant extent...
  42. doi MDR1A (ABCB1)-deficient CF-1 mutant mice are susceptible to cerebral malaria induced by Plasmodium berghei ANKA
    Sylvie Barraud de Lagerie
    Clinical Pharmacy Unit EA 2706, University of Paris Sud 11, 5 rue JB Clement, Chatenay Malabry, 92296, France
    J Parasitol 94:1139-42. 2008
    ..study was to investigate the susceptibility of the CF1 mouse strain, carrying a spontaneous mutation of the mdr1a gene, to infection with Plasmodium berghei ANKA (PbA)...
  43. doi Moderate increase in Mdr1a/1b expression causes in vivo resistance to doxorubicin in a mouse model for hereditary breast cancer
    Marina Pajic
    Division of Molecular Biology and Centre for Biomedical Genetics, The Netherlands Cancer Institute, Amsterdam, The Netherlands
    Cancer Res 69:6396-404. 2009
    ..The presence of MDR1A in drug-resistant tumors with a moderate increase in Mdr1a transcripts could be shown with a newly generated ..
  44. pmc P-glycoprotein, but not multidrug resistance protein 4, plays a role in the systemic clearance of irinotecan and SN-38 in mice
    Michael Tagen
    Department of Pharmaceutical Sciences, St Jude Children s Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105, USA
    Drug Metab Lett 4:195-201. 2010
    ..b>Mdr1a/b(-/-), Mrp4(-/-), and wild-type mice were administered 20 or 40 mg/kg irinotecan, and plasma samples were ..
  45. pmc Desipramine treatment has minimal effects on the brain accumulation of glucocorticoids in P-gp-deficient and wild-type mice
    Brittany L Mason
    Institute of Pharmaceutical Science, King s College London, London, UK
    Psychoneuroendocrinology 36:1351-60. 2011
    ..Overall, under the conditions tested, these results do not support the hypothesis that treatment with desipramine can inhibit P-gp at the BBB and subsequently increase the accumulation of glucocorticoids in the brain...
  46. pmc Drug transporters on arachnoid barrier cells contribute to the blood-cerebrospinal fluid barrier
    Kazuto Yasuda
    Department of Pharmaceutical Sciences, St Jude Children s Research Hospital, Memphis, Tennessee 38105, USA
    Drug Metab Dispos 41:923-31. 2013
    ..Thus, like blood-brain barrier cells and choroid plexus cells, AB cells highly express drug transport proteins and likely contribute to the blood-CSF drug permeation barrier...
  47. doi Impact of P-glycoprotein and breast cancer resistance protein on the brain distribution of antiepileptic drugs in knockout mouse models
    Haruka Nakanishi
    Department of Clinical Pharmacy and Education, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto 606 8501, Japan
    Eur J Pharmacol 710:20-8. 2013
    ..study, we examined the contribution of Pgp and Bcrp to the brain distribution of 12 antiepileptic drugs (AEDs) in Mdr1a/1b(-/-) and Mdr1a/1b(-/-)/Bcrp(-/-) mice within a therapeutic concentration range...
  48. doi P-glycoprotein (MDR1/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) restrict brain accumulation of the JAK1/2 inhibitor, CYT387
    S Durmus
    The Netherlands Cancer Institute, Division of Molecular Oncology, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands
    Pharmacol Res 76:9-16. 2013
    ..CYT387 (10 mg/kg) was orally administered to wild-type (WT), Bcrp1(-/-), Mdr1a/1b(-/-) and Bcrp1;Mdr1a/1b(-/-) mice and plasma and brain concentrations were analyzed...
  49. doi Irinotecan and temozolomide brain distribution: a focus on ABCB1
    Lauriane Goldwirt
    Clinical Pharmacy Department EA 4123, College of Pharmacy, Paris Sud University, 5 Rue Jean Baptiste Clement, 92296, Chatenay Malabry, France
    Cancer Chemother Pharmacol 74:185-93. 2014
    ..on the role of ABCB1, the main efflux transporter at the BBB level, through pharmacokinetics studies in CF1 mdr1a(+/+) and mdr1a(-/-) mice...
  50. pmc Selective resistance to the PARP inhibitor olaparib in a mouse model for BRCA1-deficient metaplastic breast cancer
    Linda Henneman
    Division of Molecular Pathology and Cancer Genomics Centre, The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands
    Proc Natl Acad Sci U S A 112:8409-14. 2015
    ..mouse carcinosarcomas resembling MBC show intrinsic resistance to olaparib caused by increased P-glycoprotein (Pgp) drug efflux transporter expression...
  51. pmc Human-Mouse Chimeras with Normal Expression and Function Reveal That Major Domain Swapping Is Tolerated by P-Glycoprotein (ABCB1)
    Kristen M Pluchino
    Laboratory of Cell Biology, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, Maryland 20892, United States
    Biochemistry 55:1010-23. 2016
    ..Overall, chimeras with one or two mouse P-gp domains were deemed functionally equivalent to human wild-type P-gp, demonstrating the ability of human P-gp to tolerate major structural changes. ..
  52. pmc Brain penetration of the OAB drug trospium chloride is not increased in aged mice
    Jasmin Kranz
    Institute of Pharmacology and Toxicology, Justus Liebig University of Giessen, Frankfurter Str 107, 35392, Giessen, Germany
    World J Urol 31:219-24. 2013
    ....
  53. ncbi Thioridazine induces apoptosis of multidrug-resistant mouse lymphoma cells transfected with the human ABCB1 and inhibits the expression of P-glycoprotein
    Gabriella Spengler
    Institute of Medical Microbiology and Immunobiology, Faculty of Medicine, University of Szeged, Szeged, Hungary
    Anticancer Res 31:4201-5. 2011
    ....
  54. doi Death receptors DR6 and TROY regulate brain vascular development
    Stephen J Tam
    Neurodegeneration Labs, Department of Neuroscience, Genentech, 1 DNA Way, South San Francisco, CA 94080, USA
    Dev Cell 22:403-17. 2012
    ..These findings define a role for death receptors DR6 and TROY in CNS-specific vascular development...
  55. pmc The antiepileptic drug mephobarbital is not transported by P-glycoprotein or multidrug resistance protein 1 at the blood-brain barrier: a positron emission tomography study
    Severin Mairinger
    Health and Environment Department, Molecular Medicine, AIT Austrian Institute of Technology GmbH, Seibersdorf, Austria
    Epilepsy Res 100:93-103. 2012
    ..We performed paired PET scans in rats, wild-type (FVB) and Mdr1a/b((-/-)) mice, before and after intravenous administration of the Pgp inhibitor tariquidar (15mg/kg)...
  56. pmc Changes in the brain accumulation of glucocorticoids in abcb1a-deficient CF-1 mice
    B L Mason
    Institute of Pharmaceutical Science, King s College London, London, UK
    J Neuroendocrinol 24:1440-6. 2012
    ..P-gp is coded by a single human gene, ABCB1, and shares 80% homology with the murine drug-transporting isoforms, abcb1a and abcb1b, which share 92% homology with each other...
  57. pmc P-glycoprotein (Mdr1a/1b) and breast cancer resistance protein (Bcrp) decrease the uptake of hydrophobic alkyl triphenylphosphonium cations by the brain
    Carolyn M Porteous
    Department of Chemistry, University of Otago, Dunedin, New Zealand
    Biochim Biophys Acta 1830:3458-65. 2013
    ..While this approach has delivered TPP-conjugated compounds to the brain, the amounts taken up are lower than by other organs...
  58. pmc Structural analysis of the mouse mdr1a (P-glycoprotein) promoter reveals the basis for differential transcript heterogeneity in multidrug-resistant J774.2 cells
    S I Hsu
    Department of Molecular Pharmacology, Albert Einstein College of Medicine, Bronx, New York 10461 1602
    Mol Cell Biol 10:3596-606. 1990
    ..isoforms reflects the amplification or transcriptional activation or both of two mdr gene family members, mdr1a and mdr1b...
  59. ncbi Isolation and expression of a complementary DNA that confers multidrug resistance
    P Gros
    Nature 323:728-31. 1986
    ..Furthermore, because the cDNA was isolated from a drug-sensitive cell, mutations in the primary sequence of mdr are not required to produce a multidrug-resistance phenotype...
  60. ncbi Functional dissection of P-glycoprotein nucleotide-binding domains in chimeric and mutant proteins. Modulation of drug resistance profiles
    L Beaudet
    Department of Biochemistry, McGill University, Montreal, Quebec, Canada
    J Biol Chem 270:17159-70. 1995
    ..For this, we constructed and tested the biological activity in yeast and mammalian cells of a series of chimeric mdr3 cDNAs in which discrete domains of the N-terminal NBD (NBD1) were replaced by the homologous segments of the C-..
  61. ncbi Mouse multidrug resistance 1a/3 gene is the earliest known endothelial cell differentiation marker during blood-brain barrier development
    Y Qin
    Roche Institute of Molecular Biology, Roche Research Center, Nutley, New Jersey 07110, USA
    Dev Dyn 202:172-80. 1995
    ..Here we describe that expression of the mouse multidrug resistance 1a/3 (mdr1a/3) gene can be detected specifically in subsets of vascular endothelial cells associated with neural tissues at as ..
  62. pmc Functional expression of P-glycoprotein encoded by the mouse mdr3 gene in yeast cells
    S Ruetz
    Department of Biochemistry, McGill University, Montreal, PQ, Canada
    Proc Natl Acad Sci U S A 90:11588-92. 1993
    We have expressed P-glycoprotein (P-gp) encoded by the mouse mdr3 gene in the yeast Saccharomyces cerevisiae and have developed an experimental protocol to isolate and purify inside-out plasma membrane vesicles (IOVs) from these cells...
  63. ncbi Identification of two nuclear protein binding sites and their role in the regulation of the murine multidrug resistance mdr1a promoter
    D Cohen
    Department of Molecular Pharmacology, Albert Einstein College of Medicine, Bronx, NY 10461
    DNA Cell Biol 13:641-9. 1994
    ..In murine MDR cells, mdr1a and/or mdr1b genes are overexpressed and P-gp isoforms are overproduced...
  64. ncbi Transcriptional activation of the mouse mdr3 gene coincides with the appearance of novel transcription initiation sites in multidrug-resistant P388 tumor cells
    P Lepage
    Department of Biochemistry, McGill University, Montreal, Qu57ebec, Canada
    Cancer Res 53:1657-64. 1993
    ..of the mouse lymphoid tumor P388, multidrug resistance is associated with the exclusive overexpression of the mdr3 gene...
  65. ncbi Differences between nuclear run-off and mRNA levels for multidrug resistance gene expression in the cephalocaudal axis of the mouse intestine
    J Chianale
    Department of Gastroenterology, School of Medicine, Catholic University of Chile, Santiago, Chile
    Biochim Biophys Acta 1264:369-76. 1995
    P-glycoprotein is a multidrug transporter encoded by the mdr3 gene in the mouse intestinal epithelium...
  66. ncbi Expression of c-fos precedes MDR3 in vincristine and adriamycin selected multidrug resistant murine erythroleukemia cells
    A Bhushan
    Vermont Cancer Center, University of Vermont College of Medicine, Burlington 05405, USA
    Biochem Biophys Res Commun 226:819-21. 1996
    ..murine erythroleukemia sublines selected for resistance to vincristine or adriamycin which eventually overexpress mdr3. We speculate that early expression of c-fos prepares cells for overexpression of other genes, such as mdr3, that ..
  67. pmc Hepatobiliary and intestinal clearance of amphiphilic cationic drugs in mice in which both mdr1a and mdr1b genes have been disrupted
    J W Smit
    Department of Pharmacokinetics and Drug Delivery, University Center for Pharmacy, Groningen Institute for Drug Studies, The Netherlands
    Br J Pharmacol 124:416-24. 1998
    1. We have used mice with homozygously disrupted mdr1a and mdr1b genes (mdr1a/1b (-/-) mice) to study the role of the mdr1-type P-glycoprotein (P-gp) in the elimination of cationic amphiphilic compounds from the body...
  68. ncbi Unchanged cytochrome P450 3A (CYP3A) expression and metabolism of midazolam, triazolam, and dexamethasone in mdr(-/-) mouse liver microsomes
    M D Perloff
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, New England Medical Center Hospital, Boston, MA 02111, USA
    Biochem Pharmacol 57:1227-32. 1999
    ..68+/-0.09 pmol/microg protein. Although CYP3A and P-gp share aspects of activity and expression, disruption of the mdrl genes does not affect CYP3A-mediated metabolism or protein expression in the mouse...
  69. ncbi Use of a peptide mimotope to guide the humanization of MRK-16, an anti-P-glycoprotein monoclonal antibody
    Y Tang
    Ixsys, Inc, San Diego, California 92121, USA
    J Biol Chem 274:27371-8. 1999
    ..Thus, peptide mimotopes which can be identified for virtually any antibody including those that recognize conformational or carbohydrate epitopes, can serve as antigen templates for antibody engineering...
  70. ncbi Physiologically based pharmacokinetics of digoxin in mdr1a knockout mice
    M Kawahara
    Faculty of Pharmaceutical Sciences, Kanazawa University, 13 1 Takara machi, Kanazawa 920 0934, Japan
    J Pharm Sci 88:1281-7. 1999
    To determine the contribution of the mdr1a gene product to digoxin pharmacokinetics, we constructed a physiologically based pharmacokinetic model for digoxin in mdr1a (-/-) and mdr1a (+/+) mice...
  71. ncbi Elevated expression of hepatic proliferative markers during early hepatocarcinogenesis in hepatitis-B virus transgenic mice lacking mdr1a-encoded P-glycoprotein
    J J Bao
    Division of Pathology and Laboratory Medicine, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Mol Carcinog 29:103-11. 2000
    ..To address this issue further, we investigated the expression of mdr1a, a human MDR1 homolog, on the development of hepatocellular carcinoma in a transgenic mouse model carrying the ..
  72. ncbi P-glycoprotein (encoded by multidrug resistance genes) is not required for interleukin-2 secretion in mice and humans
    S Gollapudi
    Molecular Biology and Cellular Immunology Laboratories, Division of Basic and Clinical Immunology, University of California, Irvine, CA 92697 4069, USA
    Genes Immun 1:371-9. 2000
    ..In this study, we show that anti-CD3-stimulated lymphocytes from wild-type, mdr1a knock out and mdr1ab double knock out mice produce similar amounts of IL-2, IFN-gamma, IL-4, and IL-10...
  73. ncbi Cholesterol signaling at the endoplasmic reticulum occurs in npc1(-/-) but not in npc1(-/-), LDLR(-/-) mice
    R P Erickson
    Angel Charity for Children Wings for Genetic Research, University of Arizona College of Medicine, Tucson, Arizona 85724, USA
    Biochem Biophys Res Commun 284:326-30. 2001
    ..A large decrease in processed SREBP-1 was evident in fasted npc1(-/-) mice and npc1(-/-), mdr1a(-/-) mice, with no decrease evident in npc1(-/-), LDLR(-/-) mice...
  74. pmc Helicobacter bilis infection accelerates and H. hepaticus infection delays the development of colitis in multiple drug resistance-deficient (mdr1a-/-) mice
    Lillian Maggio-Price
    Department of Comparative Medicine, School of Medicine, University of Washington, Box 357190, Seattle, WA 981295, USA
    Am J Pathol 160:739-51. 2002
    b>mdr1a-deficient mice lack P-glycoprotein and spontaneously develop colitis with age. Helicobacter spp. are gram-negative organisms that have been associated with colitis in certain mouse strains, but Helicobacter spp...
  75. ncbi mdr1a deficiency corrects sterility in Niemann-Pick C1 protein deficient female mice
    Robert P Erickson
    Department of Pediatrics, Section of Medical and Molecular Genetics, Angel Charity for Children Wings for Genetic Research, Steele Memorial Children s Research Center, Arizona, USA
    Mol Reprod Dev 62:167-73. 2002
    ..We have introduced the mdr1a knockout into the npc1 mutant line...
  76. ncbi Radixin deficiency causes conjugated hyperbilirubinemia with loss of Mrp2 from bile canalicular membranes
    Shojiro Kikuchi
    Department of Cell Biology, Faculty of Medicine, Kyoto University, Sakyo ku, Kyoto 606 8501, Japan
    Nat Genet 31:320-5. 2002
    ..These findings indicate that radixin is required for secretion of conjugated bilirubin through its support of Mrp2 localization at BCMs...
  77. ncbi P-glycoprotein catalytic mechanism: studies of the ADP-vanadate inhibited state
    Ina L Urbatsch
    Department of Biochemistry and Biophysics, University of Rochester Medical Center, Rochester, New York 14642, USA
    J Biol Chem 278:23171-9. 2003
    Kinetics of inhibition of ATPase activity of pure mouse Mdr3 P-glycoprotein upon incubation with MgADP and vanadate were studied along with the trapping of [14C]ADP in presence of vanadate...
  78. pmc Macroscopic, microscopic and biochemical characterisation of spontaneous colitis in a transgenic mouse, deficient in the multiple drug resistance 1a gene
    Katharine H Banner
    Pfizer Global Research and Development, Discovery Biology, Sandwich, Kent, UK
    Br J Pharmacol 143:590-8. 2004
    ..that have been implicated in inflammatory bowel disease (IBD) (IL-8 and IFN-gamma) in the colon/rectum of mdr1a(-/-) mice, and by determining the sensitivity of these, together with the macroscopic, microscopic and disease ..
  79. pmc Dual infection with Helicobacter bilis and Helicobacter hepaticus in p-glycoprotein-deficient mdr1a-/- mice results in colitis that progresses to dysplasia
    Lillian Maggio-Price
    Department of Comparative Medicine, School of Medicine, University of Washington, Seattle, WA 98195, USA
    Am J Pathol 166:1793-806. 2005
    ..b>Mdr1a-/- mice lack the membrane efflux pump p-glycoprotein and spontaneously develop IBD that can be modulated by ..
  80. ncbi An in silico approach for screening flavonoids as P-glycoprotein inhibitors based on a Bayesian-regularized neural network
    Yong Hua Wang
    Laboratory of Pharmaceutical Resource Discovery Dalian Institute of Chemical Physics, Graduate School of the Chinese Academy of Sciences, No 457 Zhongshan Road, 116023, Dalian, China
    J Comput Aided Mol Des 19:137-47. 2005
    ..Our study indicates that the BRNN-based in silico model has good potential in facilitating the prediction of P-gp flavonoid inhibitors and might be applied in further drug design...
  81. ncbi Temporal/spatial expression and efflux activity of ABC transporter, P-glycoprotein/Abcb1 isoforms and Bcrp/Abcg2 during early murine development
    Wojciech T Sawicki
    Department of Histology and Embryology, Medical University of Warsaw, Poland
    Gene Expr Patterns 6:738-46. 2006
    ..We found in 2-cell embryos abcb1a, abcb1b and abcg2 mRNAs which were believed to be maternally inherited...
  82. ncbi Prolongation of pentoxifylline aliphatic side chain positively affects the reversal of P-glycoprotein-mediated multidrug resistance in L1210/VCR line cells
    P Docolomansky
    Institute of Molecular Physiology and Genetics, Slovak Academy of Sciences, Vlarska 5, 833 34 Bratislava 37, Slovakia
    Gen Physiol Biophys 24:461-6. 2005
    ..We found that both PTX-UHM and PTX were able to reverse vincristine resistance of L1210/VCR cells, yet PTX-UHM was significantly more efficient in the reversal than PTX...
  83. ncbi Gefitinib modulates the function of multiple ATP-binding cassette transporters in vivo
    Markos Leggas
    Departments of Pharmaceutical Sciences, Hematology Oncology, and Molecular Pharmacology, St Jude Children s Research Hospital, Memphis, Tennessee 38105, USA
    Cancer Res 66:4802-7. 2006
    ..4-AQ molecules may offer a means to increase the low and variable oral drug absorption of transporter substrates while decreasing interpatient variability and reversing tumor drug resistance...
  84. ncbi Evaluation of the role of multidrug resistance-associated protein (Mrp) 3 and Mrp4 in hepatic basolateral excretion of sulfate and glucuronide metabolites of acetaminophen, 4-methylumbelliferone, and harmol in Abcc3-/- and Abcc4-/- mice
    Maciej J Zamek-Gliszczynski
    University of North Carolina, School of Pharmacy, Kerr Hall, CB 7360, Chapel Hill, NC 27599 7360, USA
    J Pharmacol Exp Ther 319:1485-91. 2006
    ..In addition, they reveal that Mrp3 mediates the hepatic basolateral excretion of diverse glucuronide conjugates...
  85. ncbi Mutational analysis of conserved aromatic residues in the A-loop of the ABC transporter ABCB1A (mouse Mdr3)
    Isabelle Carrier
    Department of Biochemistry and McGill Cancer Centre, McGill University, McIntyre Medical Sciences Building, Room 907, 3655 Sir William Osler Drive, Montreal, Que, Canada H3G 1Y6
    FEBS Lett 581:301-8. 2007
    ..Biochemistry 45, 7605-7616]. In mouse P-glycoprotein (Abcb1a), the aromatic residue of the A-loop in both NBDs is a tyrosine: Y397 in NBD1 and Y1040 in NBD2...
  86. ncbi P-glycoprotein-mediated active efflux of the anti-HIV1 nucleoside abacavir limits cellular accumulation and brain distribution
    Naveed Shaik
    Department of Pharmaceutics, University of Minnesota, 308 Harvard St SE, Room 9 125, Weaver Densford Hall, Minneapolis, MN 55455, USA
    Drug Metab Dispos 35:2076-85. 2007
    ..In vivo brain distribution studies showed that the AUC(plasma) in mdr1a(-/-) CF-1 mutant mice was approximately 2-fold greater than the AUC(plasma) in the wild type, whereas the AUC(..
  87. ncbi P-glycoprotein-deficient mice have proximal tubule dysfunction but are protected against ischemic renal injury
    M Huls
    Department of Pharmacology and Toxicology, Nijmegen Centre for Molecular Life Sciences, Radboud University Nijmegen Medical Centre, Nijmegen, The Netherlands
    Kidney Int 72:1233-41. 2007
    ..In contrast, knockout mice had no signs of tubular damage. Our data indicate that P-gp knockout mice have impaired renal function but are protected against ischemic renal injury...
  88. ncbi Seizure-induced up-regulation of P-glycoprotein at the blood-brain barrier through glutamate and cyclooxygenase-2 signaling
    Bjorn Bauer
    Institute of Pharmacology, Toxicology, and Pharmacy, Ludwig Maximilians University Munich, Koeniginstr 16, 80539 Munich, Germany
    Mol Pharmacol 73:1444-53. 2008
    ..Moreover, they provide insight into one mechanism that underlies drug resistance in epilepsy and possibly other central nervous system disorders...
  89. doi Polymorphisms in the drug transporter gene ABCB1 predict antidepressant treatment response in depression
    Manfred Uhr
    Max Planck Institute of Psychiatry, Kraepelinstr 10, 80804 Munich, Germany
    Neuron 57:203-9. 2008
    ..This finding can be viewed as a further step into personalized antidepressant treatment...
  90. doi Investigating the role of the invariant carboxylate residues E552 and E1197 in the catalytic activity of Abcb1a (mouse Mdr3)
    Isabelle Carrier
    Department of Biochemistry and McGill Cancer Centre, McGill University, Montreal, Canada
    FEBS J 275:3312-24. 2008
    ..In Abcb1a, this invariant carboxylate residue corresponds to E552 in NBD1 and E1197 in NBD2...
  91. ncbi Senescence-Accelerated Mouse (SAM) strains have a spontaneous mutation in the Abcb1a gene
    Guohong Zhang
    Department of Aging Biology, Institute on Aging and Adaptation, Shinshu University Graduate School of Medicine, Matsumoto, Japan
    Exp Anim 57:413-7. 2008
    ..has a spontaneous retroviral insertional mutation in the ATP-binding cassette, sub-family B (MDR/TAP), member 1A (Abcb1a) gene...
  92. doi Circadian clock-controlled intestinal expression of the multidrug-resistance gene mdr1a in mice
    Yuichi Murakami
    Pharmaceutics, Division of Clinical Pharmacy, Department of Medico Pharmaceutical Sciences, Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan
    Gastroenterology 135:1636-1644.e3. 2008
    ..Although intestinal expression of the mdr1a gene and its efflux pump function has been shown to exhibit 24-hour variation, the mechanism of the variations ..
  93. doi Reduction of brain infarction induced by a transient brain ischemia in mdr1a knockout mice
    Michihiro Murozono
    Department of Anesthesiology, Tokyo Medical University, Tokyo, Japan
    Neurochem Res 34:1555-61. 2009
    ..Neurosci Lett 24: 6-11, 2008)...
  94. pmc Compartment-specific roles of ATP-binding cassette transporters define differential topotecan distribution in brain parenchyma and cerebrospinal fluid
    Jun Shen
    Department of Pharmaceutical Sciences, St Jude Children s Research Hospital, Memphis, Tennessee 38105 2794, USA
    Cancer Res 69:5885-92. 2009
    ..The mean +/- SD ratios for wild-type, Mdr1a/b(-/-), Bcrp1(-/-), and Mdr1a/b(-/-)Bcrp1(-/-) mice were 3.07 +/- 0.09, 2.57 +/- 0.17, 1.63 +/- 0.12, and 0...
  95. pmc Characterization of an asymmetric occluded state of P-glycoprotein with two bound nucleotides: implications for catalysis
    Alena Siarheyeva
    Department of Molecular and Cellular Biology, University of Guelph, Guelph, Ontario N1G 2W1, Canada
    J Biol Chem 285:7575-86. 2010
    ....
  96. pmc Targeted genome modification in mice using zinc-finger nucleases
    Iara D Carbery
    Sigma Advanced Genetic Engineering Labs, Sigma Aldrich Biotechnology, St Louis, MO 63146, USA
    Genetics 186:451-9. 2010
    ..Three individual genes, multidrug resistant 1a (Mdr1a), jagged 1 (Jag1), and notch homolog 3 (Notch3), were targeted in FVB/N and C57BL/6 mice...
  97. doi Developmental expression of multidrug resistance phosphoglycoprotein (P-gp) in the mouse fetal brain and glucocorticoid regulation
    Sophie Petropoulos
    Department of Physiology, University of Toronto, Medical Sciences Building, 1 King s College Circle, Toronto, Ontario, Canada
    Brain Res 1357:9-18. 2010
    ..5-E15.5 (mid-gestation) or E12.5-E18.5 (late-gestation) and analyzed on E15.5 or E18.5. Abcb1a mRNA (P<0...
  98. doi Endoxifen, the active metabolite of tamoxifen, is a substrate of the efflux transporter P-glycoprotein (multidrug resistance 1)
    Wendy A Teft
    Department of Medicine, University of Western Ontario, London, ON, Canada
    Drug Metab Dispos 39:558-62. 2011
    ..relevance of P-glycoprotein to endoxifen disposition, plasma and tissue concentrations were also determined in Mdr1a-deficient mice after oral administration of endoxifen...
  99. doi Effects on enantiomeric drug disposition and open-field behavior after chronic treatment with venlafaxine in the P-glycoprotein knockout mice model
    Louise Karlsson
    Division of Drug Research, Clinical Pharmacology, Department of Medical and Health Sciences, Linkoping University, Linkoping, Sweden
    Psychopharmacology (Berl) 215:367-77. 2011
    ..To our knowledge, no studies have reported pharmacodynamic effects of any antidepressant drug in the P-gp knockout mice model...
  100. pmc Lysosomal trapping of a radiolabeled substrate of P-glycoprotein as a mechanism for signal amplification in PET
    Pavitra Kannan
    Molecular Imaging Branch, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892, USA
    Proc Natl Acad Sci U S A 108:2593-8. 2011
    ..In summary, tariquidar and [(11)C]dLop can be used in combination to selectively measure the function of P-gp at the blood-brain barrier...
  101. pmc P-glycoprotein induction by breast milk attenuates intestinal inflammation in experimental necrotizing enterocolitis
    Yigit S Guner
    Division of Pediatric Surgery, Saban Research Institute, Childrens Hospital Los Angeles, Los Angeles, CA 90027, USA
    Lab Invest 91:1668-79. 2011
    P-glycoprotein (Pgp), a product of the multi-drug resistance gene MDR1a, is a broad specificity efflux ATP cassette transmembrane transporter that is predominantly expressed in epithelial tissues...

Research Grants6

  1. BALANCED BIOACTIVITY OF ALZHEIMER BETA AMYLOID PRECURSOR
    STEVEN BARGER; Fiscal Year: 2004
    ..Specifically, elucidation of the cellular mechanisms through which sAPP activates microglia may provide targets for therapeutic intervention in Alzheimer's disease. ..
  2. Sp1, kappa-B enhancers and transcriptions in neurons
    STEVEN BARGER; Fiscal Year: 2009
    ..abstract_text> ..
  3. INTERACTIONS OF P GLYCOPROTEIN WITH CYTOCHROME P4503A
    Erin Schuetz; Fiscal Year: 2001
    ..an in vitro system (LS180 cells) in which human MDR1 Pgp is overexpressed and an in vivo system that lacks mdr1a/1b/Pgp (mdrla/lb (-/-) mice)...
  4. Pregnane X Receptor: Regulation and Pharmacogenomics
    Erin Schuetz; Fiscal Year: 2007
    ..In total this proposal describes a comprehensive set of experiments to determine how PXR is regulated. ..
  5. Phase I and Biological Studies of DB67 - A Blood Stable Camptothecin
    Markos Leggas; Fiscal Year: 2008
    ..Ultimately, the objective is to use DB-67 as a single agent or in combination with other molecular-targeted therapies or cytotoxics in frontline therapy with the goal to improve overall patient outcome. ..
  6. Commensals and Probiotics: Role in Intestinal Physiology
    Silvia Resta Lenert; Fiscal Year: 2008
    ....