The ABCG2/BCRP transporter and its variants – from structure to pathology

Precision-engineered reporter cell lines reveal ABCG2 regulation in live lung cancer cells

(2020) Daniella Kovacsics et al.   BIOCHEMICAL PHARMACOLOGY

Evidence for Direct Membrane Interaction and Cholesterol Sensing of A-Loop in ABC Transporter ABCG2

(2020) Ali Rasouli et al.   BIOPHYSICAL JOURNAL

ABCG2 requires a single aromatic amino acid to “clamp” substrates and inhibitors into the binding pocket

(2020) Tomoka Gose et al.   FASEB JOURNAL

Germline variant burden in multidrug resistance transporters is a therapy‐specific predictor of survival in breast cancer patients

(2020) Qingyang Xiao et al.   INTERNATIONAL JOURNAL OF CANCER

ABCG2 transports anticancer drugs via a closed-to-open switch

(2020) Benjamin J. Orlando et al.   Nature Communications

The ABCG2 Q141K hyperuricemia and gout associated variant illuminates the physiology of human urate excretion

(2020) Kazi Mirajul Hoque et al.   Nature Communications

Full Rescue of F508del-CFTR Processing and Function by CFTR Modulators Can Be Achieved by Removal of Two Regulatory Regions

(2020) Inna Uliyakina et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Development of precision medicine approaches based on inter-individual variability of BCRP/ABCG2

(2019) Liming Chen et al.   Acta Pharmaceutica Sinica B

Proteomic Quantification of Human Blood–Brain Barrier SLC and ABC Transporters in Healthy Individuals and Dementia Patients

(2019) Zubida M. Al-Majdoub et al.   MOLECULAR PHARMACEUTICS

ABCG2/BCRP: variants, transporter interaction profile of substrates and inhibitors

(2019) Zsolt Safar et al.   Expert Opinion on Drug Metabolism & Toxicology

Genome‐wide Association and Functional Studies Reveal Novel Pharmacological Mechanisms for Allopurinol

(2019) Deanna J. Brackman et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Interindividual and Regional Variability in Drug Transporter Abundance at the Human Blood–Brain Barrier Measured by Quantitative Targeted Proteomics

(2019) Sarah Billington et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Functional Characterization of Clinically-Relevant Rare Variants in ABCG2 Identified in a Gout and Hyperuricemia Cohort

(2019) Toyoda et al.   Cells

Cellular expression and function of naturally occurring variants of the human ABCG2 multidrug transporter

(2019) Boglárka Zámbó et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Age-Related Functional and Expressional Changes in Efflux Pathways at the Blood-Brain Barrier

(2019) Franciska Erdő et al.   Frontiers in Aging Neuroscience

Impact of Q141K on the Transport of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors by ABCG2

(2019) Yutaka Inoue et al.   Cells

Mechanics and pharmacology of substrate selection and transport by eukaryotic ABC exporters

(2019) Sriram Srikant et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Target genes, variants, tissues and transcriptional pathways influencing human serum urate levels

(2019) Adrienne Tin et al.   NATURE GENETICS

The ABCG2 multidrug transporter is a pump gated by a valve and an extracellular lid

(2019) Narakorn Khunweeraphong et al.   Nature Communications

Cellular Processing of the ABCG2 Transporter—Potential Effects on Gout and Drug Metabolism

(2019) Orsolya Mózner et al.   Cells

Systematic genetic analysis of early-onset gout: ABCG2 is the only associated locus

(2019) Faseeh Zaidi et al.   RHEUMATOLOGY

Hyperuricemia enhances intracellular urate accumulation via down-regulation of cell-surface BCRP/ABCG2 expression in vascular endothelial cells

(2018) Hisakazu Komori et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Architecture of a channel-forming O-antigen polysaccharide ABC transporter

(2018) Yunchen Bi et al.   NATURE

Genetic analysis of quantitative traits in the Japanese population links cell types to complex human diseases

(2018) Masahiro Kanai et al.   NATURE GENETICS

Structural basis of small-molecule inhibition of human multidrug transporter ABCG2

(2018) Scott M. Jackson et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

IUPred2A: context-dependent prediction of protein disorder as a function of redox state and protein binding

(2018) Bálint Mészáros et al.   NUCLEIC ACIDS RESEARCH

Structural basis of small-molecule inhibition of human multidrug transporter ABCG2

(2018) Scott M. Jackson et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Clinically relevant mutations in the ABCG2 transporter uncovered by genetic analysis linked to erythrocyte membrane protein expression

(2018) Boglárka Zámbó et al.   Scientific Reports

Polymorphisms of the multidrug pump ABCG2: a systematic review of their effect on protein expression, function and drug pharmacokinetics

(2018) Niall Heyes et al.   DRUG METABOLISM AND DISPOSITION

ABCG2: does resolving its structure elucidate the mechanism?

(2018) Parth Kapoor et al.   BIOCHEMICAL SOCIETY TRANSACTIONS

EMC Is Required to Initiate Accurate Membrane Protein Topogenesis

(2018) Patrick J. Chitwood et al.   CELL

Cryo-EM structures of a human ABCG2 mutant trapped in ATP-bound and substrate-bound states

(2018) Ioannis Manolaridis et al.   NATURE

Functional Rescue of ABCC6 Deficiency by 4-Phenylbutyrate Therapy Reduces Dystrophic Calcification in Abcc6 –/– Mice

(2017) Viola Pomozi et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Structure of the human multidrug transporter ABCG2

(2017) Nicholas M. I. Taylor et al.   NATURE

The eukaryotic linear motif resource – 2018 update

(2017) Marc Gouw et al.   NUCLEIC ACIDS RESEARCH

Functional non-synonymous variants of ABCG2 and gout risk

(2017) Blanka Stiburkova et al.   RHEUMATOLOGY

Structure-function relationships in ABCG2: insights from molecular dynamics simulations and molecular docking studies

(2017) Ricardo J. Ferreira et al.   Scientific Reports

The structure of the human ABC transporter ABCG2 reveals a novel mechanism for drug extrusion

(2017) Narakorn Khunweeraphong et al.   Scientific Reports

A comprehensive analysis of the association of common variants of ABCG2 with gout

(2017) Kuang-Hui Yu et al.   Scientific Reports

Functional characterization of the ABCG2 5′ non-coding exon variants: Stem cell specificity, translation efficiency and the influence of drug selection

(2016) Sára Sándor et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

Hypoxia regulates ABCG2activity through the activivation of ERK1/2/HIF-1α and contributes to chemoresistance in pancreatic cancer cells

(2016) Xiaodan He et al.   CANCER BIOLOGY & THERAPY

Pilot PET Study to Assess the Functional Interplay Between ABCB1 and ABCG2 at the Human Blood-Brain Barrier

(2016) M Bauer et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Gout

(2016) Nicola Dalbeth et al.   LANCET

Crystal structure of the human sterol transporter ABCG5/ABCG8

(2016) Jyh-Yeuan Lee et al.   NATURE

Mechanistic diversity in ATP-binding cassette (ABC) transporters

(2016) Kaspar P Locher   NATURE STRUCTURAL & MOLECULAR BIOLOGY

ABCG2 loss-of-function polymorphism predicts poor response to allopurinol in patients with gout

(2016) R L Roberts et al.   PHARMACOGENOMICS JOURNAL

Jump into a New Fold—A Homology Based Model for the ABCG2/BCRP Multidrug Transporter

(2016) Laura László et al.   PLoS One

Mechanistic diversity in ATP-binding cassette (ABC) transporters

(2016) Kaspar P Locher   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Functional Rescue of Trafficking-Impaired ABCB4 Mutants by Chemical Chaperones

(2016) Raquel Gordo-Gilart et al.   PLoS One

Association Study of a Functional Variant on ABCG2 Gene with Sunitinib-Induced Severe Adverse Drug Reaction

(2016) Siew-Kee Low et al.   PLoS One

Genome-wide association study of clinically defined gout identifies multiple risk loci and its association with clinical subtypes

(2015) Hirotaka Matsuo et al.   ANNALS OF THE RHEUMATIC DISEASES

Endocytosis of ABCG2 drug transporter caused by binding of 5D3 antibody: trafficking mechanisms and intracellular fate

(2015) Maciej Studzian et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Identification of residues in ABCG2 affecting protein trafficking and drug transport, using co-evolutionary analysis of ABCG sequences

(2015) A. J. Haider et al.   BIOSCIENCE REPORTS

The linker region of breast cancer resistance protein ABCG2 is critical for coupling of ATP-dependent drug transport

(2015) S. Macalou et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Genome-wide association study identifies ABCG2 (BCRP) as an allopurinol transporter and a determinant of drug response

(2015) CC Wen et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Rescuing Trafficking Mutants of the ATP-binding Cassette Protein, ABCA4, with Small Molecule Correctors as a Treatment for Stargardt Eye Disease

(2015) Inna Sabirzhanova et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

New trends for overcoming ABCG2/BCRP-mediated resistance to cancer therapies

(2015) David Westover et al.   JOURNAL OF EXPERIMENTAL & CLINICAL CANCER RESEARCH

Correlation between the promoter methylation status of ATP-binding cassette sub-family G member 2 and drug sensitivity in colorectal cancer cell lines

(2015) HYUN-HYE MOON et al.   ONCOLOGY REPORTS

An update on the genetic architecture of hyperuricemia and gout

(2015) Tony R Merriman   ARTHRITIS RESEARCH & THERAPY

Genetic analysis of <i>ABCG2</i> and <i>SLC2A9</i> gene polymorphisms in gouty arthritis in a Korean population

(2015) Yun Sung Kim et al.   KOREAN JOURNAL OF INTERNAL MEDICINE

Sunitinib-induced severe toxicities in a Japanese patient with the ABCG2 421 AA genotype

(2015) Yuji Miura et al.   BMC CANCER

Role of the Breast Cancer Resistance Protein (BCRP/ABCG2) in Drug Transport—an Update

(2014) Qingcheng Mao et al.   AAPS Journal

Tumor heterogeneity and cancer stem cell paradigm: Updates in concept, controversies and clinical relevance

(2014) Anup Kumar Singh et al.   INTERNATIONAL JOURNAL OF CANCER

Functional Polymorphisms of the ABCG2 Gene Are Associated with Gout Disease in the Chinese Han Male Population

(2014) Danqiu Zhou et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Association between ABCG2 Q141K polymorphism and gout risk affected by ethnicity and gender: a systematic review and meta-analysis

(2014) Zheng Dong et al.   International Journal of Rheumatic Diseases

PTEN Regulates BCRP/ABCG2 and the Side Population through the PI3K/Akt Pathway in Chronic Myeloid Leukemia

(2014) Fang-Fang Huang et al.   PLoS One

LKB1/AMPK and PKA Control ABCB11 Trafficking and Polarization in Hepatocytes

(2014) László Homolya et al.   PLoS One

A CFTR corrector (lumacaftor) and a CFTR potentiator (ivacaftor) for treatment of patients with cystic fibrosis who have a phe508del CFTR mutation: a phase 2 randomised controlled trial

(2014) Michael P Boyle et al.   Lancet Respiratory Medicine

Drug–Drug Interaction Studies: Regulatory Guidance and An Industry Perspective

(2013) Thomayant Prueksaritanont et al.   AAPS Journal

Effects of the gout-causing Q141K polymorphism and a CFTR ΔF508 mimicking mutation on the processing and stability of the ABCG2 protein

(2013) Hajnalka Sarankó et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

International Transporter Consortium Commentary on Clinically Important Transporter Polymorphisms

(2013) K M Giacomini et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Gout-causing Q141K mutation in ABCG2 leads to instability of the nucleotide-binding domain and can be corrected with small molecules

(2013) O. M. Woodward et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Stimulus-induced expression of the ABCG2 multidrug transporter in HepG2 hepatocarcinoma model cells involves the ERK1/2 cascade and alternative promoters

(2012) Hugues de Boussac et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Interaction of the EGFR inhibitors gefitinib, vandetanib, pelitinib and neratinib with the ABCG2 multidrug transporter: Implications for the emergence and reversal of cancer drug resistance

(2012) Csilla Hegedüs et al.   BIOCHEMICAL PHARMACOLOGY

Role of breast cancer resistance protein (BCRP/ABCG2) in cancer drug resistance

(2012) Karthika Natarajan et al.   BIOCHEMICAL PHARMACOLOGY

Histone Deacetylase Inhibitors Influence Chemotherapy Transport by Modulating Expression and Trafficking of a Common Polymorphic Variant of the ABCG2 Efflux Transporter

(2012) A. Basseville et al.   CANCER RESEARCH

Dynamic ABCG2 expression in human embryonic stem cells provides the basis for stress response

(2012) Zsuzsa Erdei et al.   EUROPEAN BIOPHYSICS JOURNAL WITH BIOPHYSICS LETTERS

Rab5 is necessary for the biogenesis of the endolysosomal system in vivo

(2012) Anja Zeigerer et al.   NATURE

Structure of AMP-PNP-bound vitamin B12 transporter BtuCD–F

(2012) Vladimir M. Korkhov et al.   NATURE

ABCG2 null alleles define the Jr(a−) blood group phenotype

(2012) Teresa Zelinski et al.   NATURE GENETICS

Null alleles of ABCG2 encoding the breast cancer resistance protein define the new blood group system Junior

(2012) Carole Saison et al.   NATURE GENETICS

Genome-wide association analyses identify 18 new loci associated with serum urate concentrations

(2012) Anna Köttgen et al.   NATURE GENETICS

Individualized risk for statin-induced myopathy: current knowledge, emerging challenges and potential solutions

(2012) QiPing Feng et al.   PHARMACOGENOMICS

Expression Levels of the ABCG2 Multidrug Transporter in Human Erythrocytes Correspond to Pharmacologically Relevant Genetic Variations

(2012) Ildikó Kasza et al.   PLoS One

Cancer drug pan-resistance: pumps, cancer stem cells, quiescence, epithelial to mesenchymal transition, blocked cell death pathways, persisters or what?

(2012) P. Borst   Open Biology

Mechanisms of CFTR Folding at the Endoplasmic Reticulum

(2012) Soo Jung Kim et al.   Frontiers in Pharmacology

Breast cancer resistance protein BCRP/ABCG2 regulatory microRNAs (hsa-miR-328, -519c and -520h) and their differential expression in stem-like ABCG2+ cancer cells

(2011) Xin Li et al.   BIOCHEMICAL PHARMACOLOGY

Identification of Proline Residues in or near the Transmembrane Helices of the Human Breast Cancer Resistance Protein (BCRP/ABCG2) That Are Important for Transport Activity and Substrate Specificity

(2011) Zhanglin Ni et al.   BIOCHEMISTRY

Rescue of ΔF508-CFTR Trafficking via a GRASP-Dependent Unconventional Secretion Pathway

(2011) Heon Yung Gee et al.   CELL

Multidrug Efflux Pumps and Cancer Stem Cells: Insights Into Multidrug Resistance and Therapeutic Development

(2011) K Moitra et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Antibody binding shift assay for rapid screening of drug interactions with the human ABCG2 multidrug transporter

(2011) Ágnes Telbisz et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Tyrosine kinase inhibitors as modulators of ATP binding cassette multidrug transporters: substrates, chemosensitizers or inducers of acquired multidrug resistance?

(2011) Anna Brózik et al.   Expert Opinion on Drug Metabolism & Toxicology

Effects of Cellular, Chemical, and Pharmacological Chaperones on the Rescue of a Trafficking-defective Mutant of the ATP-binding Cassette Transporter Proteins ABCB1/ABCB4

(2011) Julien Gautherot et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Quantitative Membrane Protein Expression at the Blood–Brain Barrier of Adult and Younger Cynomolgus Monkeys

(2011) Katsuaki Ito et al.   JOURNAL OF PHARMACEUTICAL SCIENCES

Identification of a novel, tissue-specific ABCG2 promoter expressed in pediatric acute megakaryoblastic leukemia

(2011) Patrick K. Campbell et al.   LEUKEMIA RESEARCH

Upregulation of ABCG2 by Romidepsin via the Aryl Hydrocarbon Receptor Pathway

(2011) K. K. W. To et al.   MOLECULAR CANCER RESEARCH

Bile acid stimulates hepatocyte polarization through a cAMP-Epac-MEK-LKB1-AMPK pathway

(2011) D. Fu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Correction of the F508del-CFTR protein processing defect in vitro by the investigational drug VX-809

(2011) F. Van Goor et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Posttranslational negative regulation of glycosylated and non-glycosylated BCRP expression by Derlin-1

(2010) Takashi Sugiyama et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

A novel xenobiotic responsive element regulated by aryl hydrocarbon receptor is involved in the induction of BCRP/ABCG2 in LS174T cells

(2010) Leslie M. Tompkins et al.   BIOCHEMICAL PHARMACOLOGY

hsa-miR-520h downregulates ABCG2 in pancreatic cancer cells to inhibit migration, invasion and side populations

(2010) F Wang et al.   BRITISH JOURNAL OF CANCER

Influence of CYP3A5 and drug transporter polymorphisms on imatinib trough concentration and clinical response among patients with chronic phase chronic myeloid leukemia

(2010) Naoto Takahashi et al.   JOURNAL OF HUMAN GENETICS

Regulatory Insertion Removal Restores Maturation, Stability and Function of ΔF508 CFTR

(2010) Andrei A. Aleksandrov et al.   JOURNAL OF MOLECULAR BIOLOGY

ABCG2: A potential marker of stem cells and novel target in stem cell and cancer therapy

(2010) Xi-wei Ding et al.   LIFE SCIENCES

Expression of ABCG2 (BCRP) Is Regulated by Nrf2 in Cancer Cells That Confers Side Population and Chemoresistance Phenotype

(2010) Anju Singh et al.   MOLECULAR CANCER THERAPEUTICS

Membrane transporters in drug development

(2010)   NATURE REVIEWS DRUG DISCOVERY

Dynamic vs Static ABCG2 Inhibitors to Sensitize Drug Resistant Cancer Cells

(2010) Hui Peng et al.   PLoS One

Arginine 383 is a crucial residue in ABCG2 biogenesis

(2009) Orsolya Polgar et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

PTEN/PI3K/Akt Pathway Regulates the Side Population Phenotype and ABCG2 Activity in Glioma Tumor Stem-like Cells

(2009) Anne-Marie Bleau et al.   Cell Stem Cell

Interaction of ABC Multidrug Transporters with Anticancer Protein Kinase Inhibitors: Substrates and/or Inhibitors?

(2009) Csilla Ozvegy-Laczka et al.   CURRENT CANCER DRUG TARGETS

Disruption of N-linked glycosylation enhances ubiquitin-mediated proteasomal degradation of the human ATP-binding cassette transporter ABCG2

(2009) Hiroshi Nakagawa et al.   FEBS Journal

Rab11b Regulates the Apical Recycling of the Cystic Fibrosis Transmembrane Conductance Regulator in Polarized Intestinal Epithelial Cells

(2009) Mark R. Silvis et al.   MOLECULAR BIOLOGY OF THE CELL

Escape from hsa-miR-519c enables drug-resistant cells to maintain high expression of ABCG2

(2009) K. K.W. To et al.   MOLECULAR CANCER THERAPEUTICS

MicroRNA-328 Negatively Regulates the Expression of Breast Cancer Resistance Protein (BCRP/ABCG2) in Human Cancer Cells

(2009) Y.-Z. Pan et al.   MOLECULAR PHARMACOLOGY

Identification of a urate transporter, ABCG2, with a common functional polymorphism causing gout

(2009) O. M. Woodward et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Common Defects of ABCG2, a High-Capacity Urate Exporter, Cause Gout: A Function-Based Genetic Analysis in a Japanese Population

(2009) H. Matsuo et al.   Science Translational Medicine

Quality control of human ABCG2 protein in the endoplasmic reticulum: Ubiquitination and proteasomal degradation

(2008) Kanako Wakabayashi-Nakao et al.   ADVANCED DRUG DELIVERY REVIEWS

ABCG2: A perspective

(2008) Robert W. Robey et al.   ADVANCED DRUG DELIVERY REVIEWS

Purification and structural analyses of ABCG2

(2008) Christopher A. McDevitt et al.   ADVANCED DRUG DELIVERY REVIEWS

The ABCA1 Q597R mutant undergoes trafficking from the ER upon ER stress

(2008) Arowu R. Tanaka et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

High level functional expression of the ABCG2 multidrug transporter in undifferentiated human embryonic stem cells

(2008) Ágota Apáti et al.   BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES

Pharmacogenomic and Pharmacokinetic Determinants of Erlotinib Toxicity

(2008) Charles M. Rudin et al.   JOURNAL OF CLINICAL ONCOLOGY

Association of three genetic loci with uric acid concentration and risk of gout: a genome-wide association study

(2008) Abbas Dehghan et al.   LANCET

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) K. K. W. To et al.   MOLECULAR AND CELLULAR BIOLOGY

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

(2008) K. K.W. To et al.   MOLECULAR CANCER RESEARCH

Major SNP (Q141K) Variant of Human ABC Transporter ABCG2 Undergoes Lysosomal and Proteasomal Degradations

(2008) Tomoka Furukawa et al.   PHARMACEUTICAL RESEARCH