Property Summary

NCBI Gene PubMed Count 638
Grant Count 354
R01 Count 144
Funding $47,384,563.17
PubMed Score 2531.48
PubTator Score 1791.58

Knowledge Summary

Patent

No data available

Expression

  Differential Expression (14)

Disease log2 FC p
urothelial carcinoma 1.500 0.003
malignant mesothelioma -6.900 0.000
cutaneous lupus erythematosus 1.500 0.006
osteosarcoma -1.252 0.002
medulloblastoma, large-cell -1.500 0.002
adrenocortical adenoma -1.098 0.016
adrenocortical carcinoma -1.573 0.001
non-small cell lung cancer -1.838 0.000
lung cancer -1.700 0.001
active Crohn's disease -3.180 0.025
lung adenocarcinoma -1.600 0.000
pilocytic astrocytoma 1.100 0.000
Breast cancer -1.500 0.000
ulcerative colitis -5.200 0.000

Synonym

Accession Q9UNQ0 A0A1W3 A8K1T5 O95374 Q4W5I3 Q53ZQ1 Q569L4 Q5YLG4 Q86V64 Q8IX16 Q96LD6 Q96TA8 Q9BY73 Q9NUS0
Symbols MRX
MXR
ABCP
BCRP
BMDP
MXR1
ABC15
BCRP1
CD338
GOUT1
MXR-1
CDw338
UAQTL1
EST157481

Gene

MLP Assay (8)

AID Type Active / Inconclusive / Inactive Description
1325 screening 200 / 0 / 194280 High-throughput multiplex screening for ABC transporter inhibitors: specifically ABCG2 screen, ABCB1 counter-screen
1453 screening 16 / 0 / 257 Single point confirmation screening for ABC transporter inhibitors: specifically ABCG2 screen, ABCB1 counter-screen
1690 confirmatory 16 / 0 / 24 Dose Response for ABC transporter inhibitors: specifically ABCG2 screen, ABCB1 counter-screen
1818 summary 1 / 0 / 0 Summary of High-throughput multiplex screening for ABC transporter inhibitors
2830 other 5 / 0 / 10 Chemo Reversal assay in ABCG2-expressing cells for one set of SAR compounds
488974 other 23 / 0 / 14 SAR hit validation chemo-reversal assay specifically in in ABCG2-expressing cells, ABCB1 counterscreen
489003 confirmatory 75 / 0 / 14 Dose Response for ABC transporter inhibitors: specifically ABCG2 screen, ABCB1 counter-screen. Follow-up assay.
504477 confirmatory 9 / 0 / 1 Chemo Reversal assay in ABCG2-expressing cells for set 2 of SAR compounds

Gene RIF (633)

PMID Text
27192835 The results represented in this work together with previous data proved a link between ABCG2 protein expression, its activity and maintenance of viability and proliferative activity of mesenchymal stem cells cultivated under hypoxia.
27191194 The different 5' UTR variants play an important role in cell type specific regulation and fine tuning of ABCG2 expression.
26943330 hyperactivity of Hh signaling resulted in EGFR-TKI resistance, by EMT introduction and ABCG2 upregulation, and blockade of Hh signaling synergistically increased sensitivity to EGFR-TKIs in primary and secondary resistant NSCLC cells
26914831 association of a functional germline variant on ABCG2 that affects the pharmacokinetics of sunitinib with sunitinib-induced toxicity of renal cell carcinoma patients in the Japanese population
26909964 The data demonstrate potential roles of PDK2 and ABCG2 polymorphisms in the metabolic phenotypes of Tibetan gout patients.
26903388 We conclude from our results that the C421A SNP may lead to reduced ABCG2 protein levels not only by affecting cellular protein stability but also via enhanced microRNA-dependent ABCG2 repression.
26842595 Literature-collated REFs ranged from 0.4 to 5.1 and 1.1 to 90 for intestinal P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), respectively.
26801902 Based on our preclinical results, we suggest analyzing the predictive value of the BCRP in breast cancer patients scheduled for irinotecan treatment.
26714568 ABCG2 was associated with an increased risk of gout during middle age for men (HR = 2.60, 95% CI: 1.89-3.57) and women (HR = 1.78, 95% CI: 1.07-2.96).
26714461 Here, it is our intention to review: 1) recent discoveries that further characterize the role of ABCG2 in oncology, and 2) advances in reversing and circumventing ABC transporter-mediated resistance to anti-cancer therapies.
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AA Sequence

MSSSNVEVFIPVSQGNTNGFPATASNDLKAFTEGAVLSFHNICYRVKLKSGFLPCRKPVEKEILSNINGI      1 - 70
MKPGLNAILGPTGGGKSSLLDVLAARKDPSGLSGDVLINGAPRPANFKCNSGYVVQDDVVMGTLTVRENL     71 - 140
QFSAALRLATTMTNHEKNERINRVIQELGLDKVADSKVGTQFIRGVSGGERKRTSIGMELITDPSILFLD    141 - 210
EPTTGLDSSTANAVLLLLKRMSKQGRTIIFSIHQPRYSIFKLFDSLTLLASGRLMFHGPAQEALGYFESA    211 - 280
GYHCEAYNNPADFFLDIINGDSTAVALNREEDFKATEIIEPSKQDKPLIEKLAEIYVNSSFYKETKAELH    281 - 350
QLSGGEKKKKITVFKEISYTTSFCHQLRWVSKRSFKNLLGNPQASIAQIIVTVVLGLVIGAIYFGLKNDS    351 - 420
TGIQNRAGVLFFLTTNQCFSSVSAVELFVVEKKLFIHEYISGYYRVSSYFLGKLLSDLLPMRMLPSIIFT    421 - 490
CIVYFMLGLKPKADAFFVMMFTLMMVAYSASSMALAIAAGQSVVSVATLLMTICFVFMMIFSGLLVNLTT    491 - 560
IASWLSWLQYFSIPRYGFTALQHNEFLGQNFCPGLNATGNNPCNYATCTGEEYLVKQGIDLSPWGLWKNH    561 - 630
VALACMIVIFLTIAYLKLLFLKKYS                                                 631 - 655
//

Text Mined References (643)

PMID Year Title
27192835 [The Role of ABCG2 Protein in Maintenance of Viability and Proliferative Activity of Bone Marrow Mesenchymal Stem Cells Under Hypoxic Conditions].
27191194 2016 Functional characterization of the ABCG2 5' non-coding exon variants: Stem cell specificity, translation efficiency and the influence of drug selection.
26943330 2016 Blockade of Hedgehog Signaling Synergistically Increases Sensitivity to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non-Small-Cell Lung Cancer Cell Lines.
26914831 2016 Association Study of a Functional Variant on ABCG2 Gene with Sunitinib-Induced Severe Adverse Drug Reaction.
26909964 2016 PDK2 and ABCG2 genes polymorphisms are correlated with blood glucose levels and uric acid in Tibetan gout patients.
26903388 2016 The C421A (Q141K) polymorphism enhances the 3'-untranslated region (3'-UTR)-dependent regulation of ATP-binding cassette transporter ABCG2.
26842595 2016 In Vitro-In Vivo Extrapolation Scaling Factors for Intestinal P-glycoprotein and Breast Cancer Resistance Protein: Part II. The Impact of Cross-Laboratory Variations of Intestinal Transporter Relative Expression Factors on Predicted Drug Disposition.
26801902 2016 Molecular characterization of irinotecan (SN-38) resistant human breast cancer cell lines.
26714568 2016 Gout in Older Adults: The Atherosclerosis Risk in Communities Study.
26714461 2015 New trends for overcoming ABCG2/BCRP-mediated resistance to cancer therapies.
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