ABCG2: A perspective

Multidrug resistance in cancer: role of ATP–dependent transporters

2002 • 5,195 citations

ABC Transporters: From Microorganisms to Man

1992 • 3,956 citations

A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants

1976 • 3,228 citations

Overexpression of a Transporter Gene in a Multidrug-Resistant Human Lung Cancer Cell Line

1992 • 3,039 citations

Isolation and functional properties of murine hematopoietic stem cells that are replicating in vivo.

1996 • 2,901 citations

The ABC transporter Bcrp1/ABCG2 is expressed in a wide variety of stem cells and is a molecular determinant of the side-population phenotype

2001 • 2,274 citations

Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs

1994 • 2,255 citations

The Human ATP-Binding Cassette (ABC) Transporter Superfamily

2001 • 1,705 citations

Multidrug resistance proteins: role of P-glycoprotein, MRP1, MRP2, and BCRP (ABCG2) in tissue defense

2004 • 1,329 citations

Subcellular localization and distribution of the breast cancer resistance protein transporter in normal human tissues.

2001 • 1,116 citations

The Human ATP-Binding Cassette (ABC) Transporter Superfamily

2001 • 1,110 citations

Cell Surface P-Glycoprotein Associated with Multidrug Resistance in Mammalian Cell Lines

1983 • 1,001 citations

The GxxxG motif: A framework for transmembrane helix-helix association

2000 • 905 citations

Molecular cloning of cDNAs which are highly overexpressed in mitoxantrone-resistant cells: demonstration of homology to ABC transport genes.

1999 • 810 citations

The breast cancer resistance protein protects against a major chlorophyll-derived dietary phototoxin and protoporphyria

2002 • 807 citations

A human placenta-specific ATP-binding cassette gene (ABCP) on chromosome 4q22 that is involved in multidrug resistance.

1998 • 798 citations

The ABCG2 transporter is an efficient Hoechst 33342 efflux pump and is preferentially expressed by immature human hematopoietic progenitors

2002 • 754 citations

Cellular resistance to actinomycin D in Chinese hamster cells in vitro: cross-resistance, radioautographic, and cytogenetic studies.

1970 • 752 citations

Isolation of human mdr DNA sequences amplified in multidrug-resistant KB carcinoma cells.

1986 • 688 citations

Potent and specific inhibition of the breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C.

2002 • 682 citations

The Blood-Brain Barrier and Cancer: Transporters, Treatment, and Trojan Horses

2007 • 675 citations

The Stem Cell Marker Bcrp/ABCG2 Enhances Hypoxic Cell Survival through Interactions with Heme

2004 • 648 citations

Role of Breast Cancer Resistance Protein in the Bioavailability and Fetal Penetration of Topotecan

2000 • 640 citations

ATP-Binding Cassette Transporters in Bacteria

2004 • 635 citations

EVOLUTION OF THE ATP-BINDING CASSETTE (ABC) TRANSPORTER SUPERFAMILY IN VERTEBRATES

2005 • 614 citations

Trough imatinib plasma levels are associated with both cytogenetic and molecular responses to standard-dose imatinib in chronic myeloid leukemia

2006 • 592 citations

MDR1 gene overexpression confers resistance to imatinib mesylate in leukemia cell line models

2003 • 554 citations

The Gut as a Barrier to Drug Absorption

2001 • 518 citations

Isolation and genetic characterization of human KB cell lines resistant to multiple drugs

1985 • 517 citations

Bcrp1gene expression is required for normal numbers of side population stem cells in mice, and confers relative protection to mitoxantrone in hematopoietic cellsin vivo

2002 • 506 citations

Fumitremorgin C reverses multidrug resistance in cells transfected with the breast cancer resistance protein.

2000 • 494 citations

C421A polymorphism in the human breast cancer resistance protein gene is associated with low expression of Q141K protein and low-level drug resistance.

2002 • 432 citations

Acquired mutations in the MXR/BCRP/ABCP gene alter substrate specificity in MXR/BCRP/ABCP-overexpressing cells.

2001 • 427 citations

The breast cancer resistance protein BCRP (ABCG2) concentrates drugs and carcinogenic xenotoxins into milk

2005 • 412 citations

Localisation of breast cancer resistance protein in microvessel endothelium of human brain

2002 • 405 citations

Toxicological relevance of the multidrug resistance protein 1, MRP1 (ABCC1) and related transporters

2001 • 374 citations

ABCG2: determining its relevance in clinical drug resistance

2007 • 373 citations

Dasatinib or high-dose imatinib for chronic-phase chronic myeloid leukemia after failure of first-line imatinib: a randomized phase 2 trial

2007 • 372 citations

The Effect of Bcrp1 (Abcg2) on the In vivo Pharmacokinetics and Brain Penetration of Imatinib Mesylate (Gleevec): Implications for the Use of Breast Cancer Resistance Protein and P-Glycoprotein Inhibitors to Enable the Brain Penetration of Imatinib in Patients

2005 • 348 citations

Mutations at amino-acid 482 in the ABCG2 gene affect substrate and antagonist specificity

2003 • 347 citations

High-Affinity Interaction of Tyrosine Kinase Inhibitors with the ABCG2 Multidrug Transporter

2004 • 338 citations

Pheophorbide a Is a Specific Probe for ABCG2 Function and Inhibition

2004 • 332 citations

Imatinib Mesylate Is a Potent Inhibitor of the ABCG2 (BCRP) Transporter and Reverses Resistance to Topotecan and SN-38 in Vitro

2004 • 324 citations

Expression, Up-Regulation, and Transport Activity of the Multidrug-Resistance Protein Abcg2 at the Mouse Blood-Brain Barrier

2004 • 315 citations

Functional Characterization of the Human Multidrug Transporter, ABCG2, Expressed in Insect Cells

2001 • 310 citations

Single nucleotide polymorphisms result in impaired membrane localization and reduced atpase activity in multidrug transporter ABCG2

2003 • 309 citations

Coexpression of ATP-binding cassette proteins ABCG5 and ABCG8 permits their transport to the apical surface

2002 • 308 citations

Reversal of a novel multidrug resistance mechanism in human colon carcinoma cells by fumitremorgin C.

1998 • 301 citations

Dominant‐negative inhibition of breast cancer resistance protein as drug efflux pump through the inhibition of S‐S dependent homodimerization

2001 • 292 citations

Reversal of resistance by GF120918 in cell lines expressing the ABC half-transporter, MXR

1999 • 291 citations

The breast cancer resistance protein transporter ABCG2 is expressed in the human kidney proximal tubule apical membrane

2007 • 278 citations

Frequent expression of the multi‐drug resistance‐associated protein BCRP/MXR/ABCP/ABCG2 in human tumours detected by the BXP‐21 monoclonal antibody in paraffin‐embedded material

2002 • 270 citations

Coexpression of ATP-binding cassette proteins ABCG5 and ABCG8 permits their transport to the apical surface

2002 • 268 citations

P-Glycoprotein and Breast Cancer Resistance Protein: Two Dominant Transporters Working Together in Limiting the Brain Penetration of Topotecan

2007 • 264 citations

Involvement of BCRP (ABCG2) in the Biliary Excretion of Pitavastatin

2005 • 253 citations

Diflomotecan pharmacokinetics in relation to ABCG2 421C>A genotype*1

2004 • 241 citations

Pharmacogenetics of ABCG2 and Adverse Reactions to Gefitinib

2006 • 236 citations

The breast cancer resistance protein (Bcrp1/Abcg2) restricts exposure to the dietary carcinogen 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine.

2003 • 234 citations

Expression of breast cancer resistance protein in blast cells from patients with acute leukemia

2000 • 233 citations

Cyclosporin A Is a Broad-Spectrum Multidrug Resistance Modulator

2005 • 230 citations

Characterisation of the brain multidrug resistance protein (BMDP/ABCG2/BCRP) expressed at the blood–brain barrier

2003 • 229 citations

Promoter characterization and genomic organization of the human breast cancer resistance protein (ATP-binding cassette transporter G2) gene

2001 • 223 citations

Characterization of adriamycin-resistant human breast cancer cells which display overexpression of a novel resistance-related membrane protein.

1990 • 223 citations

The Breast Cancer Resistance Protein (BCRP/ABCG2) Affects Pharmacokinetics, Hepatobiliary Excretion, and Milk Secretion of the Antibiotic Nitrofurantoin

2005 • 220 citations

Single nucleotide polymorphisms modify the transporter activity of ABCG2

2005 • 219 citations

Multidrug Transporter ABCG2/Breast Cancer Resistance Protein Secretes Riboflavin (Vitamin B₂) into Milk

2006 • 219 citations

Pharmacogenomic and Pharmacokinetic Determinants of Erlotinib Toxicity

2008 • 217 citations

Identification of a Novel Estrogen Response Element in the Breast Cancer Resistance Protein ( ABCG2 ) Gene

2004 • 216 citations

Identification of BCRP as transporter of benzo[ a ]pyrene conjugates metabolically formed in Caco-2 cells and its induction by Ah-receptor agonists

2005 • 213 citations

ABCG2: structure, function and role in drug response

2007 • 213 citations

Imatinib mesylate and nilotinib (AMN107) exhibit high-affinity interaction with ABCG2 on primitive hematopoietic stem cells

2007 • 201 citations

Expression and functional characterization of ABCG2 in brain endothelial cells and vessels

2003 • 200 citations

Effect of the ATP-binding cassette drug transporters ABCB1, ABCG2, and ABCC2 on erlotinib hydrochloride (Tarceva) disposition inin vitroandin vivopharmacokinetic studies employing Bcrp1−/−/Mdr1a/1b−/− (triple-knockout) and wild-type mice

2008 • 199 citations

BREAST CANCER RESISTANCE PROTEIN (BCRP/ABCG2) TRANSPORTS FLUOROQUINOLONE ANTIBIOTICS AND AFFECTS THEIR ORAL AVAILABILITY, PHARMACOKINETICS, AND MILK SECRETION

2006 • 196 citations

Functional C3435T polymorphism of MDR1 gene: an impact on genetic susceptibility and clinical outcome of childhood acute lymphoblastic leukemia

2004 • 196 citations

Gene expression profiling of adult acute myeloid leukemia identifies novel biologic clusters for risk classification and outcome prediction

2006 • 194 citations

Localization of the ABCG2 mitoxantrone resistance-associated protein in normal tissues

2005 • 194 citations

Breast Cancer Resistance Protein and P-Glycoprotein in 149 Adult Acute Myeloid Leukemias

2004 • 189 citations

Effect of Breast Cancer Resistance Protein (Bcrp/Abcg2) on the Disposition of Phytoestrogens

2007 • 182 citations

ABCG2 expression, function, and promoter methylation in human multiple myeloma

2006 • 180 citations

Independent Regulation of Apical and Basolateral Drug Transporter Expression and Function in Placental Trophoblasts by Cytokines, Steroids, and Growth Factors

2007 • 179 citations

Expression of breast cancer resistance protein in blast cells from patients with acute leukemia

2000 • 175 citations

Portrait of multifaceted transporter, the multidrug resistance-associated protein 1 (MRP1/ABCC1)

2006 • 172 citations

Peroxisome Proliferator-activated Receptor γ-regulated ABCG2 Expression Confers Cytoprotection to Human Dendritic Cells

2006 • 171 citations

Distribution of breast cancer resistance protein (BCRP/ABCG2) mRNA expression along the human GI tract

2005 • 169 citations

VX-710 (Biricodar) Increases Drug Retention and Enhances Chemosensitivity in Resistant Cells Overexpressing P-Glycoprotein, Multidrug Resistance Protein, and Breast Cancer Resistance Protein

2004 • 165 citations

Functional ABCG2 is overexpressed on primary CML CD34+ cells and is inhibited by imatinib mesylate

2006 • 165 citations

Estrogen-Mediated Post transcriptional Down-regulation of Breast Cancer Resistance Protein/ABCG2

2005 • 164 citations

Evolution of the vertebrate ABC gene family: Analysis of gene birth and death

2006 • 163 citations

Regulation of ABCG2 Expression at the 3′ Untranslated Region of Its mRNA through Modulation of Transcript Stability and Protein Translation by a Putative MicroRNA in the S1 Colon Cancer Cell Line

2008 • 160 citations

Akt Signaling Regulates Side Population Cell Phenotype via Bcrp1 Translocation

2003 • 160 citations

Subcellular distribution of daunorubicin in P-glycoprotein-positive and -negative drug-resistant cell lines using laser-assisted confocal microscopy.

1991 • 160 citations

The distribution of drug-efflux pumps, P-gp, BCRP, MRP1 and MRP2, in the normal blood–testis barrier and in primary testicular tumours

2004 • 159 citations

Breast cancer resistance protein (Bcrp1/Abcg2) reduces systemic exposure of the dietary carcinogens aflatoxin B1, IQ and Trp-P-1 but also mediates their secretion into breast milk

2005 • 154 citations

Effect of ABCG2 genotype on the oral vioavailability of topotecan

2005 • 154 citations

Breast Cancer Resistance Protein (Bcrp/abcg2) Is a Major Determinant of Sulfasalazine Absorption and Elimination in the Mouse

2006 • 153 citations

Membrane vesicle formation due to acquired mitoxantrone resistance in human gastric carcinoma cell line EPG85-257.

1990 • 148 citations

Regulation of BCRP/ABCG2 expression by progesterone and 17β-estradiol in human placental BeWo cells

2005 • 144 citations

Quantitative Investigation of the Role of Breast Cancer Resistance Protein (Bcrp/Abcg2) in Limiting Brain and Testis Penetration of Xenobiotic Compounds

2008 • 140 citations

Genetic Susceptibility Loci for Breast Cancer by Estrogen Receptor Status

2008 • 137 citations

Isolation and characterization of an anthracycline-resistant human leukemic cell line.

1985 • 137 citations

The effect of P-gp (Mdr1a/1b), BCRP (Bcrp1) and P-gp/BCRP inhibitors on the in vivo absorption, distribution, metabolism and excretion of imatinib

2008 • 137 citations

Functional Validation of the Genetic Polymorphisms of Human ATP-Binding Cassette (ABC) Transporter ABCG2: Identification of Alleles That Are Defective in Porphyrin Transport

2006 • 136 citations

Functional expression of rat ABCG2 on the luminal side of brain capillaries and its enhancement by astrocyte‐derived soluble factor(s)

2004 • 134 citations

Reduced intracellular drug accumulation in the absence of P-glycoprotein (mdr1) overexpression in mitoxantrone-resistant human MCF-7 breast cancer cells.

1992 • 134 citations

The Tyrosine Kinase Inhibitor Imatinib Mesylate Enhances the Efficacy of Photodynamic Therapy by Inhibiting ABCG2

2007 • 133 citations

Transport of Glyburide by Placental ABC Transporters: Implications in Fetal Drug Exposure

2006 • 132 citations

Purification and 3D Structural Analysis of Oligomeric Human Multidrug Transporter ABCG2

2006 • 127 citations

Histone Modifications at the ABCG2 Promoter following Treatment with Histone Deacetylase Inhibitor Mirror Those in Multidrug-Resistant Cells

2008 • 124 citations

Polymorphism C3435T of the MDR-1 gene predicts response to preoperative chemotherapy in locally advanced breast cancer

2003 • 123 citations

Breast Cancer Resistance Protein (Bcrp1/Abcg2) Limits Net Intestinal Uptake of Quercetin in Rats by Facilitating Apical Efflux of Glucuronides

2005 • 121 citations

Mechanisms of resistance to anticancer drugs: the role of the polymorphic ABC transporters ABCB1 and ABCG2

2005 • 121 citations

Identification of Intra- and Intermolecular Disulfide Bridges in the Multidrug Resistance Transporter ABCG2

2005 • 119 citations

Progesterone Receptor (PR) Isoforms PRA and PRB Differentially Regulate Expression of the Breast Cancer Resistance Protein in Human Placental Choriocarcinoma BeWo Cells

2007 • 119 citations

Aberrant Promoter Methylation of the ABCG2 Gene in Renal Carcinoma

2006 • 115 citations

The Breast Cancer Resistance Protein (Bcrp1/Abcg2) Limits Fetal Distribution of Glyburide in the Pregnant Mouse: An Obstetric-Fetal Pharmacology Research Unit Network and University of Washington Specialized Center of Research Study

2007 • 113 citations

ABC transporters and inhibitors: new targets, new agents.

2002 • 112 citations

N-Linked Glycosylation of the Human ABC Transporter ABCG2 on Asparagine 596 Is Not Essential for Expression, Transport Activity, or Trafficking to the Plasma Membrane

2005 • 110 citations

Part II: Management of resistance to imatinib in chronic myeloid leukaemia

2007 • 109 citations

The Important Role of Bcrp (Abcg2) in the Biliary Excretion of Sulfate and Glucuronide Metabolites of Acetaminophen, 4-Methylumbelliferone, and Harmol in Mice

2006 • 108 citations

Effect of calcium antagonists on the chemosensitivity of two multidrug-resistant human tumour cell lines which do not overexpress P-glycoprotein

1989 • 107 citations

Genetic support for a quantitative trait nucleotide in the ABCG2 gene affecting milk composition of dairy cattle

2007 • 107 citations

The Role of Placental Breast Cancer Resistance Protein in the Efflux of Glyburide across the Human Placenta

2008 • 103 citations

Reduced drug accumulation and multidrug resistance in human breast cancer cells without associated P-glycoprotein or MRP overexpression

1997 • 102 citations

Interaction of enrofloxacin with breast cancer resistance protein (BCRP/ABCG2): influence of flavonoids and role in milk secretion in sheep

2006 • 101 citations

REGULATION OF THE CELL SURFACE EXPRESSION OF HUMAN BCRP/ABCG2 BY THE PHOSPHORYLATION STATE OF AKT IN POLARIZED CELLS

2005 • 100 citations

Mutational Analysis of ABCG2: Role of the GXXXG Motif

2004 • 99 citations

Influence of breast cancer resistance protein (Abcg2) and p‐glycoprotein (Abcb1a) on the transport of imatinib mesylate (Gleevec^®) across the mouse blood–brain barrier

2007 • 93 citations

Cross-resistance to camptothecin analogues in a mitoxantrone-resistant human breast carcinoma cell line is not due to DNA topoisomerase I alterations.

1995 • 91 citations

Amplification of 4q21-q22 and theMXR gene in independently derived mitoxantrone-resistant cell lines

2000 • 90 citations

Involvement of Breast Cancer Resistance Protein (ABCG2) in the Biliary Excretion Mechanism of Fluoroquinolones

2007 • 87 citations

Overexpression of P-glycoprotein in K562 cells does not confer resistance to the growth inhibitory effects of imatinib (STI571) in vitro

2003 • 86 citations

Expression and Transport Activity of Breast Cancer Resistance Protein (Bcrp/Abcg2) in Dually Perfused Rat Placenta and HRP-1 Cell Line

2006 • 85 citations

Differential Involvement of Mrp2 (Abcc2) and Bcrp (Abcg2) in Biliary Excretion of 4-Methylumbelliferyl Glucuronide and Sulfate in the Rat

2006 • 84 citations

Breast Cancer Resistance Protein: Mediating the Trans-placental Transfer of Glyburide across the Human Placenta

2007 • 84 citations

Impaired renal excretion of 6-hydroxy-5,7-dimethyl-2-methylamino-4-(3-pyridylmethyl) benzothiazole (E3040) sulfate in breast cancer resistance protein (BCRP1/ABCG2) knockout mice.

2004 • 83 citations

Single amino acid substitutions in the transmembrane domains of breast cancer resistance protein (BCRP) alter cross resistance patterns in transfectants

2003 • 81 citations

ABCG2 Expression and Side Population Abundance Regulated by a Transforming Growth Factor β–Directed Epithelial-Mesenchymal Transition

2008 • 80 citations

Breast Cancer Resistance Protein 1 Limits Fetal Distribution of Nitrofurantoin in the Pregnant Mouse

2007 • 79 citations

Reversal of the resistance to STI571 in human chronic myelogenous leukemia K562 cells

2003 • 77 citations

Novel 5′ Untranslated Region Variants of BCRP mRNA Are Differentially Expressed in Drug-Selected Cancer Cells and in Normal Human Tissues: Implications for Drug Resistance, Tissue-Specific Expression, and Alternative Promoter Usage

2006 • 72 citations

The nature of amino acid 482 of human ABCG2 affects substrate transport and ATP hydrolysis but not substrate binding

2006 • 70 citations

Breast Cancer Resistance Protein (BCRP/ABCG2) Is Expressed by Progenitor Cells/Reactive Ductules and Hepatocytes and Its Expression Pattern Is Influenced by Disease Etiology and Species Type: Possible Functional Consequences

2006 • 70 citations

In Vitro Evaluation of Photosensitivity Risk Related to Genetic Polymorphisms of Human ABC Transporter ABCG2 and Inhibition by Drugs

2007 • 70 citations

Oligomerization Domain of the Multidrug Resistance–Associated Transporter ABCG2 and Its Dominant Inhibitory Activity

2007 • 69 citations

ABCG2/BCRP decreases the transfer of a food-born chemical carcinogen, 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) in perfused term human placenta

2008 • 68 citations

Modulation of the Brain Distribution of Imatinib and its Metabolites in Mice by Valspodar, Zosuquidar and Elacridar

2007 • 67 citations

Effect of Walker A mutation (K86M) on oligomerization and surface targeting of the multidrug resistance transporter ABCG2

2005 • 61 citations

Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor

2006 • 57 citations

Evaluation of the Role of Breast Cancer Resistance Protein (BCRP/ABCG2) and Multidrug Resistance-Associated Protein 4 (MRP4/ABCC4) in The Urinary Excretion of Sulfate and Glucuronide Metabolites of Edaravone (MCI-186; 3-Methyl-1-phenyl-2-pyrazolin-5-one)

2007 • 56 citations

Subcellular localization of the ABCG2 transporter in normal and malignant human gallbladder epithelium

2004 • 54 citations

Short Communication: A Polymorphism in ABCG2 in Bos indicus and Bos taurus Cattle Breeds

2006 • 52 citations

MDR1 Single Nucleotide Polymorphisms Predict Response to Vinorelbine-Based Chemotherapy in Patients with Non-Small Cell Lung Cancer

2007 • 46 citations

Involvement of Breast Cancer Resistance Protein (BCRP/ABCG2) in the Biliary Excretion and Intestinal Efflux of Troglitazone Sulfate, the Major Metabolite of Troglitazone with a Cholestatic Effect

2006 • 45 citations

Disposition of 9-nitrocamptothecin and its 9-aminocamptothecin metabolite in relation to ABC transporter genotypes

2006 • 42 citations

An ATP-binding cassette gene (ABCG3) closely related to the multidrug transporter ABCG2 (MXR/ABCP) has an unusual ATP-binding domain

2001 • 36 citations

Mutational Studies of G553 in TM5 of ABCG2: A Residue Potentially Involved in Dimerization

2006 • 36 citations

Lack of Improvement of Oral Absorption of ME3277 by Prodrug Formation Is Ascribed to the Intestinal Efflux Mediated by Breast Cancer Resistant Protein (BCRP/ABCG2)

2005 • 29 citations

Characterization of ABCG2 gene amplification manifesting as extrachromosomal DNA in mitoxantrone-selected SF295 human glioblastoma cells

2005 • 29 citations

Effects of sex hormones on regulation of ABCG2 expression in the placental cell line BeWo.

2006 • 27 citations