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Validated All-in-One™ qPCR Primer for ABCG2(NM_004827.2) Search again
By default, qPCR primer pairs are designed to measure the expression level of the splice variant (accession number) you selected for this gene WITHOUT consideration of other possible variants of this gene. If this gene has multiple variants, and you would like to measure the expression levels of one particular variant, multiple variants, or all variants, please contact us for a custom service project at inquiry@genecopoeia.com.
Validated result:
Summary
The membrane-associated protein encoded by this gene is included in the superfamily of ATP-binding cassette (ABC) transporters. ABC proteins transport various molecules across extra- and intra-cellular membranes. ABC genes are divided into seven distinct subfamilies (ABC1, MDR/TAP, MRP, ALD, OABP, GCN20, White). This protein is a member of the White subfamily.
Gene References into function
- role in transport of 7-ethyl-10-hydroxycamptothecin (SN-38) in human lung cancer cells
- ABCG2 protein effluxes hoechst 33342 in hematopoietic stem cells
- homodimer formation is essential for BCRP drug resistance
- There is no indication that elevated BCRP expression in breast carcinomas confers resistance to anthracyclines.
- Increased expression in relapsed or refractory acute myeloid leukemia compared to level at diagnosis.
- Expression of the BCRP gene reduces the response to chemotherapy in AML and that BCRP expression is higher at the time of relapse.
- Overexpression of wild-type breast cancer resistance protein mediates methotrexate resistance.
- involvement of ABCG2 in multidrug resistance in cancer, especially with regard to acute myeloid leukemia
- characterization of different isoforms without possible endogenous dimerization partners
- ABCG2 expression conferred resistance to mitoxantrone & topotecan, but not to idarubicin. High levels of ABCG2 mRNA expression in adult AML blast specimens are relatively uncommon. ABCG2 expression may be limited to a small cell subpopulation.
- The breast cancer resistance protein protects against pheophorbide a, a major chlorophyll-derived dietary phototoxin, and protoporphyria.
- In both normal and tumour brain tissue, BCRP is located at the blood-brain barrier, mainly at the luminal surface of microvessel endothelium. It may pose an additional barrier to drug access to the brain.
- results showed that ABCG2 confers resistance to indolocarbazoles by transporting them in an energy-dependent manner
- polymorphisms in BCRP1 result in low amounts of BCRP, which results in hypersensitivity of normal cells to such anticancer drugs as irinotecan and mitoxantrone
- RNA expression of this protein in breast cancer correlates with response to chemotherapy.
- Function of the ABC transporters, P-gp, multidrug resistance protein and BCRP, in minimal residual disease in acute myeloid leukemia
- BCRP may play a role in the transport of sterols in human, in addition to its ability to transport multiple drugs and toxins.
- transports sulfated conjugates of steroids and xenobiotics
- functional study on polymorphism and determination of critical role of arginine-482 in methotrexate transport
- Wld-type as well as R482T BCRP mediates cellular efflux of 9-AC but not 9-NC. Zplar groups at the 9 or 10 position of the CPT A ring facilitate interaction with BCRP.
- ABCG2 is a component of the energy-dependent efflux system for certain folates and antifolates.
- ABCG2 is expressed and functions as a transporter in the brain.
- Single amino acid substitutions in the transmembrane domains of breast cancer resistance protein (BCRP) alter cross resistance patterns in transfectants
- REVIEW: multidrug resistance in breast cancer
- Higher ABCG2 expression is associated with T-lineage acute lymphoblastic leukemia
- human ABCG2 likely exists and functions as a homotetramer
- BCRP may serve as a molecular target for reducing drug resistance to chemotherapy in advanced lung cancer patients.
- VX-710 modulates Pgp, MRP-1, and BCRP(R482), and has potential as a clinical broad-spectrum multidrug resistance modulator in malignancies.
- ABCG2 overexpression is associated with drug resistance to SN38 in colon cancer cells and in irinotecan-treated metastases
- Bcrp/ABCG2 enhances hypoxic cell survival through interactions with heme
- subcellular localization of ABCG2 in gallbladder adenocarcinoma
- As a method of circumventing ABCG2-associated drug resistance, low-polarity camptothecin analogues are considered to be potent lead compounds.
- BCRP mRNA levels, antibody staining and function correlated strongly in cell lines but not in acute myeloid leukemia samples, suggesting complex biology of BCRP in AML and incomplete modeling by cell lines
- imatinib is a substrate for BCRP; it competes with mitoxantrone for drug export
- GXXXG motif promotes proper packing of the transmembrane segments in the functional ABCG2 homodimer, although it does not solely arbitrate dimerization
- Results suggest that 1) the predominant allelic expression pattern of BCRP in placental samples is biallelic, and 2) the mutation C421A is not a genetic variant acting in cis, but is considered to influence translation efficiency.
- conformational changes of the ABCG2 multidrug transporter modify its interaction with a monoclonal antibody on the cell surface
- Cyclosporin A is neither a substrate nor an inhibitor of the human ABCG2 transporter.
- The breast cancer resistance protein (BCRP) can be expressed in AML and BCRP mRNA expression was determined in samples from 40 AML patients by real-time RT-PCR.
- The ABCG2, a member of the ATP binding cassette (ABC) transporters, has been identified as a molecular determinant for bone marrow stem cells and proposed as a universal marker for stem cells.
- substrate specificity of the Arg (wild-type) form is unique and that amino acid replacements at position 482 induce major alterations in both the transport activity and substrate specificity of this protein
- The ABCG2 (MXR/BCRP/ABCP) is associated with mitoxantrone resistance accompanied by cross-resistance to a broad spectrum of cytotoxic drugs.
- glycosylation of ABCG2 on asparagine 596 is not essential for expression, transport activity, or trafficking to the plasma membrane
- ABCG2 might play a significant role in maintaining human neural stem cells in an undifferentiated state
- Side populations amounting to <1% of total cells, which were sensitive to the ABCG2-inhibitor fumitremorgin C, were found in the conjunctival and limbal epithelia, but were absent from the stem cell-free corneal epithelium.
- 19 SNPs were found in the ABCG2 gene, of which 7 were previously unknown, and results will be used in future studies to explore the influence of the different SNPs on ABCG2 protein expression, activity, and substrate specificity.
- data presented argue against a role for BCRP in primary drug resistance in multiple myeloma
- BCRP is a candidate renal cell cancer susceptibility gene.
- The induction of BCRP expression was inhibited in Caco-2 cells by co-incubation with the AhR antagonist PD98059.
- Expression of P-gp, but not BCRP, decreases dramatically with gestational age in human placentae.
- Chemoresistance of melanomas and neuroendocrine carcinomas of the skin cannot be explained by expression of the ABCG2-chemoresistance gene.
- Side population is enriched with tumorigenic stem-like cancer cells, ABCG2 expression identifies mainly fast-cycling tumor progenitors, and the ABCG2- population contains primitive stem-like cancer cells.
- ABCB1, ABCC1, ABCC2, and ABCG2 haplotypes influence response to nelfinavir
- data suggest that ABCG2 functions as a dimer, but do not exclude functional higher order oligomers
- Single nucleotide polymorphisms within the BCRP gene affect the transporter function of the protein and thus can modulate drug sensitivity and substrate pharmacokinetics and pharmacodynamics in affected cells and individuals. (review)
- Review. Current knowledge of BCRP and its relevance to multidrug resistance and drug disposition.
- genetic polymorphisms of human ABC transporter ABCG2 and new camptothecin analogues that can circumvent AGCG2-associated multidrug resistance of cancer
- ABCB1, ABCC1, and ABCG1 are expressed differently in gastric and nongastric gastrointestinal stromal tumors and do not impair the initial response of the tumor to imatinib
- MRP3, BCRP, and P-glycoprotein have roles in progression of adult acute myeloid leukemia
- BCRP may mediate the drug resistance of ovarian cancer cells to topotecan by reducing intracellular drug concentrations.
- Cys-603 is an important residue in the covalent bridge between BCRP monomers but that a functioning unit of BCRP may not necessarily require covalent linkages in breast cancers
- these studies have revealed how ABCG2 influences the absorption, distribution, and excretion of drugs and cytotoxins {review}
- Results suggest that placental BCRP can play an important role in preventing the accumulation of potentially toxic xenobiotics in the trophoblast cells.
- evidence that clearly indicates that glyburide is preferentially transported by BCRP and MRP3
- cysteine residues in the extra-cellular loop are considered to play pivotal roles in homodimer formation and plasma membrane localization of ABCG2
- BCRP causes measurable imatinib resistance, but this effect is attenuated by imatinib-mediated inhibition of BCR-ABL, which in turn downregulates overall BCRP levels posttranscriptionally via the PI3K-Akt pathway.
- These data show that cancer-associated down-regulation of BCRP is likely to be a common phenomenon in several tissues.
- glycine 553 is important for protein trafficking and are consistent with, but do not yet prove, its involvement in ABCG2 homodimerization
- BCRP was over-expressed in 24 patients and was significantly co-expressed with P-glycoprotein in acute myeloid leukemia.
- BCRP overexpression in the drug-selected cancer cells is accompanied by multiple transcriptional start sites and predominance of the more efficiently translated E1c isoform. The exon 1 variation suggests that alternative promoters of the BCRP gene exist.
- Taurine amidate does not affect ABCG2-mediated Estrone 3-sulfate transport and is not an ABCG2 substrate.
- residue 482 plays an important role in substrate transport and ATP turnover, but that the nature of this amino acid may not be important for substrate recognition and binding
- Inhibitors GF120918 and 6-prenylchrysin, which alter mitoxantrone efflux much better for wild-type than mutant ABCG2.
- These data suggest that DNA methylation-dependent formation of a repressor complex in the CpG island contributes to inactivation of ABCG2.
- Data show that tetrahydrocurcumin inhibits the efflux function of ABCB1, ABCC1, and ABCG2 and it is able to extend the multidrug resistance reversing activity of curcuminoids in vivo.
- BCRP transports anticancer drugs more efficiently at low pH, independent of the dissociation status of the substrate.
- 3D structural analysis of oligomeric human multidrug transporter ABCG2
- analysis of genetic polymorphisms of human ABC transporter ABCG2 using the flp recombinase system
- ABCC4/Abcc4 and ABCG2/Abcg2 have roles in cGMP transport
- results suggest that the P269S variant could be a functionally altered variant; genetic polymorphisms of BCRP were found to be very common in Koreans, as well as in other ethnic groups
- RALBP1 and ABCG2 transport doxorubicin differently in lung and breast cancer cell lines
- ABCG2 protects cells during the period of transient membrane instability associated with cell differentiation and fusion, highlighting a novel, previously unrecognised role of ABCG2 as a survival factor during the formation of the placental syncytium.
- Based on our functional validation, the above-mentioned non-synonymous polymorphisms as well as acquired mutants (R482G and R482T) of ABCG2 were classified into four groups
- This review focuses on our current knowledge about normal tissue distribution, tumor expression profiles, and substrates and inhibitors of ABCG2.
- CD34-related MDR1/BCRP coexpression remained significantly associated with a lower CR rate, thereby identifying a clinically resistant subgroup of elderly AML patients
- The study indicates an essential role of membrane cholesterol for the function of ABCG2.
- study showed that T623C BCRP encodes a non-functional BCRP and that T1291C BCRP encodes a low-functional BCRP
- Show low endogenous ABCG2 protein expression, localization and activity in cultures of rat brain microvessel endothelial and glial cells.
- By increasing intracellular photosensitizer levels in ABCG2+ tumors, imatinib mesylate or other ABCG2 transport inhibitors may enhance efficacy and selectivity of clinical photosensitizing agents.
- ABCG2 was significantly hypersensitive against KP772.
- Although the SLCO1B1 polymorphism was found to have a significant effect on the pharmacokinetics of pitavastatin, a nonsynonymous ABCG2 variant, 421C>A, did not appear to be associated with the altered pharmacokinetics of pitavastatin.
- During the exposure to anticancer drugs, an allele-specific Q141 ABCG2 gene amplification occurs that confers a drug resistance advantage when compared to the K141 ABCG2.
- BCRP Guanine34Adenosine and Cytosine421Adenosine polymorphisms are associated with the risk and survival of diffuse large B-cell lymphoma.
- Suggest that BCRP could play a significant role in the pharmacokinetic interactions of ketoconazole or itraconazole with BCRP substrate drugs.
- dose-dependent, reversible inhibition of ABCG2-mediated efflux in primary human and murine HSC by both imatinib and nilotinib; ABCG2-transduced K562 cells were protected from imatinib and nilotinib-mediated cell death and from downregulation of P-CRKL
- BCRP may play a hitherto unrecognized survival role in the placenta, protecting the trophoblast against cytokine-induced apoptosis and possibly other extrinsic activators via modulation of ceramide signaling
- Membrane cholesterol selectively modulates the activity of the human ABCG2 multidrug transporter.
- The absolute presence of ABCG2-positive cells in the tumor is a single independent prognostic factor, suggesting the underlying roles in malignant characteristics of esophageal squamous cell carcinoma other than drug resistance.
- Results suggest that Bcrp and Mrp4 are partly involved in the luminal efflux of edaravone sulfate and edaravone glucuronide, respectively.
- wild type ABCG2 is degraded in lysosomes, and the misfolded ABCG2 lacking intramolecular disulfide bond undergoes ubiquitin-mediated protein degradation in proteasomes
- imatinib does not interact at the ATP-binding sites of either Pgp or ABCG2 despite their strong affinity for the ATP-binding pocket of the tyrosine kinases; it behaves like a transport substrate as it stimulates ATP hydrolysis by these transporters
- ABCG2 higher expression is associated with minimal residual disease in mantle cell lymphoma
- statistically significant correlations between MRP1 and LRP expression and between MRP1 or LRP expression and MDR1 expression
- Human adult dental pulp tissue contains side population cells...that express ABCG2
- This is the first evidence to clearly indicate that glyburide is preferentially transported by BCRP, in the brush border of the human placenta.
- P-gp, rather than BCRP or OCT1, is partially responsible for the development of imatinib-resistance due to constitutive and functional overexpression, leading to reduced intracellular accumulation of imatinib in resistant K562 cells.
- The expression of ABCG2 may explain in part the ineffectiveness of doxorubicin as a single modality treatment for anaplastic thyroid cancer or for treatment of metastatic follicular thyroid cancer.
- We describe a novel nonsense mutation in exon 10 of the ABCG5 gene in a 10-year-old girl showing clinical and biochemical features of sitosterolaemia
- Progesterone receptor isoforms differentially regulate expression of ABCG2 in placental choriocarcinoma cells.
- ABCG2 is a regulatory protein of early human hematopoietic development.
- Pim-1 kinase phosphorylates BCRP/ABCG2 and thereby promotes its multimerization and drug-resistant activity in human prostate cancer cells
- identify a steroid-binding element in the membrane domain of ABCG2 with a similarity to steroid hormone/nuclear receptors
- Certain genetic polymorphisms and/or inhibition of ABCG2 by drugs can enhance the potential risk of photosensitivity.
- BCRP expression in lymphoblasts, liver and intestine is associated with novel promoter and intron 1 single nucleotide polymorphisms.
- Determination of P-glycoprotein, MDR-related protein 1, breast cancer resistance protein, and lung-resistance protein expression in leukemic stem cells of acute myeloid leukemia.
- certain genetic polymorphisms can affect the protein stability of ABCG2
- ABCG2 expression in MCF7 cells is regulated during an EMT, and that the EMT effect reflects posttranslational regulation of ABCG2 function by E-cadherin as well as transcriptional repression of the ABCG2 gene.
- Results of molecular dockings of known BCRP substrates to the BCRP model indicate multiple binding sites in BCRP.
- Breast cancer resistance protein is variably expressed and localized in human fetal membranes and decidua.
- these aspects of the transporter warrant further research aimed at understanding ABCG2's structure, function and regulation of expression--REVIEW
- Multidrug resistance (MDR) phenotype arises following low-dose, single-step exposure to doxorubicin, and further suggest that ABCG2 may mediate early stages of MDR development.
- ABCG2, an efflux pump for xenobiotics/drugs, was expressed at much higher levels in failing hearts compared to nonfailing control hearts. ABCG2 was found in cardiac capillary endothelial cells and cardiomyocytes
- Commonly occurring SNPs in BCRP linked with significantly increased oral sulfasalazine plasma exposure in humans.
- Three cysteine residues (Cys284, Cys374, Cys438) are required concurrently for the function of ABCG2 and potentially for intramolecular disulfide bond formation.
- BCRP actively transports glyburide.
- Dasatinib is a substrate of both efflux proteins, ABCB1 and ABCG2.
- The binding of a putative miRNA at the 3'UTR of ABCG2 suppresses the expression of ABCG2.
- These results indicate that Pgp down-regulates BCRP expression in a drug-free state in which JNK/c-Jun is involved.
- biochemical analysis of a model of the large extracellular loop of the ABCG2 protein
- Human ABC transporters ABCG2 (BCRP) and ABCG4
- Review highlights the influence of ATP-binding cassette transporter ABCG2 (ABCP, BCRP and MXR) polymorphisms on the absorption and disposition of a wide variety of drugs.
- in prostate cancer cells at least two mechanisms of drug resistance are interconnected. PTEN and mTOR signaling were shown: to be involved into regulation of MRP1 and BCRP
- Increased exposure to amine 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP)may decrease survival, but the ABCG2 C421A polymorphism does not appear to increase the risk of prostate cancer.
- Co-expression of cytokeratin 8 and breast cancer resistant protein indicates a multifactorial drug-resistant phenotype in human breast cancer cell line.
- heterozygous carriers of the minor alleles of SNPs rs2622621 and rs1481012 had a decreased risk of colorectal cancer
- High level functional expression of the ABCG2 multidrug transporter in undifferentiated embryonic stem cells is reported.
- Lower expression of BCRP is associated with minimal residual disease.
- results indicate the protective role of intrinsic ABCG2 expression in hepatocellular carcinoma cells
- Lapatinib reverses ABCB1- and ABCG2-mediated MDR by directly inhibiting their transport function.
- Cellular phototoxicity evoked through the inhibition of human ABC transporter ABCG2 by cyclin-dependent kinase inhibitors in vitro.
- Curcumin may be used to enhance drug exposure when the rate-limiting step of drug absorption and/or tissue distribution is impacted by ABCG2.
- The growth inhibitory effects of berberine treatment on MCF-7 cells may be partly via effects on side population (SP) cells and ABCG2 expression.
- Major SNP (Q141K) variant of human ABC transporter ABCG2 undergoes lysosomal and proteasomal degradations.
- ABCG2 polymorphism is associated with chemotherapy-induced diarrhea in patients with diffuse large B-cell lymphoma who received frontline rituximab plus cyclophosphamide/doxorubicin/vincristine/pred-nisone chemotherapy.
- evidence support a 6-transmembrane segment model for BCRP with the amino and carboxyl termini of the membrane-spanning domain located intracellularly
- ABCG2 expression is correlated neither to side population nor to hematopoietic progenitor function in human umbilical cord blood.
- ABCC3 C-211T and ABCG2 C421A as candidate transporter SNPs to be further investigated as possible predictors of the clinical outcome of chemotherapy in lung cancer patients.
- study found a small population of plasma cells expresses a high level of ABCG2; high expression of ABCG2 appeared to be induced by the synergistic action of IL-6 & endoplasmic reticulum stress, and could protect the plasma cells from apoptotic stimuli
- ABCG2 expression was limited to microvessel endothelial cells in infants born at 22 (0/7)-42 (0/7) weeks of gestation.
- We have demonstrated the expression of BCRP in human corneal epithelial cells and, for the first time, demonstrated its functional activity leading to drug efflux.
