Abcg2

Summary

Gene Symbol: Abcg2
Description: ATP binding cassette subfamily G member 2 (Junior blood group)
Alias: ABC15, ABCP, AI428558, BCRP, Bcrp1, MXR, MXR1, ATP-binding cassette sub-family G member 2, ATP-binding cassette, sub-family G (WHITE), member 2, breast cancer resistance protein 1 homolog, mitoxantrone resistance protein 1, urate exporter
Species: mouse
Products:     Abcg2

Top Publications

  1. Krohn M, Lange C, Hofrichter J, Scheffler K, Stenzel J, Steffen J, et al. Cerebral amyloid-? proteostasis is regulated by the membrane transport protein ABCC1 in mice. J Clin Invest. 2011;121:3924-31 pubmed publisher
    ..Thus, by altering the temporal aggregation profile of A?, pharmacological activation of ABC transporters could impede the neurodegenerative cascade that culminates in the dementia of AD. ..
  2. Zhou S, Zong Y, Ney P, Nair G, Stewart C, Sorrentino B. Increased expression of the Abcg2 transporter during erythroid maturation plays a role in decreasing cellular protoporphyrin IX levels. Blood. 2005;105:2571-6 pubmed
    b>ABCG2/BCRP is a member of the adenosine triphosphate-binding cassette (ABC) transporter family and is expressed in intestine, kidney, and liver, where it modulates the absorption and excretion of xenobiotic compounds...
  3. Martin C, Meeson A, Robertson S, Hawke T, Richardson J, Bates S, et al. Persistent expression of the ATP-binding cassette transporter, Abcg2, identifies cardiac SP cells in the developing and adult heart. Dev Biol. 2004;265:262-75 pubmed
    ..In this study, we confirm that Abcg2 is a determinant of the SP cell phenotype...
  4. Krishnamurthy P, Ross D, Nakanishi T, Bailey Dell K, Zhou S, Mercer K, et al. The stem cell marker Bcrp/ABCG2 enhances hypoxic cell survival through interactions with heme. J Biol Chem. 2004;279:24218-25 pubmed
    ..the ABC transporter and marker of stem and progenitor cells known as the breast cancer resistance protein (BCRP or ABCG2) confers a strong survival advantage under hypoxic conditions...
  5. Jonker J, Musters S, Vlaming M, Plosch T, Gooijert K, Hillebrand M, et al. Breast cancer resistance protein (Bcrp1/Abcg2) is expressed in the harderian gland and mediates transport of conjugated protoporphyrin IX. Am J Physiol Cell Physiol. 2007;292:C2204-12 pubmed
    ..We have previously shown that mice with a deficiency in the ABC transporter Bcrp1/Abcg2 display a novel type of protoporphyria...
  6. Tanaka K, Hall J, Troy A, Cornelison D, Majka S, Olwin B. Syndecan-4-expressing muscle progenitor cells in the SP engraft as satellite cells during muscle regeneration. Cell Stem Cell. 2009;4:217-25 pubmed publisher
    ..We propose that this subset of SP cells (satellite-SP cells), characterized by ABCG2, Syndecan-4, and Pax7 expression, constitutes a self-renewing muscle stem cell capable of generating both ..
  7. Yang J, Milton M, Yu S, Liao M, Liu N, Wu J, et al. P-glycoprotein and breast cancer resistance protein affect disposition of tandutinib, a tyrosine kinase inhibitor. Drug Metab Lett. 2010;4:201-12 pubmed
    ..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...
  8. Higashikuni Y, Sainz J, Nakamura K, Takaoka M, Enomoto S, Iwata H, et al. The ATP-binding cassette transporter BCRP1/ABCG2 plays a pivotal role in cardiac repair after myocardial infarction via modulation of microvascular endothelial cell survival and function. Arterioscler Thromb Vasc Biol. 2010;30:2128-35 pubmed publisher
    To clarify the impact of breast cancer resistance protein 1 (BCRP1)/ATP-binding cassette transporter subfamily G member 2 (ABCG2) expression on cardiac repair after myocardial infarction (MI).
  9. Jonker J, Buitelaar M, Wagenaar E, van der Valk M, Scheffer G, Scheper R, et al. The breast cancer resistance protein protects against a major chlorophyll-derived dietary phototoxin and protoporphyria. Proc Natl Acad Sci U S A. 2002;99:15649-54 pubmed
    ..Pheophorbide a occurs in various plant-derived foods and food supplements. Bcrp1 transports pheophorbide a and is highly efficient in limiting its uptake from ingested food...

More Information

Publications89

  1. de Vries N, Zhao J, Kroon E, Buckle T, Beijnen J, van Tellingen O. P-glycoprotein and breast cancer resistance protein: two dominant transporters working together in limiting the brain penetration of topotecan. Clin Cancer Res. 2007;13:6440-9 pubmed
    ..Whereas the effect of P-glycoprotein (P-gp) at the BBB is well established, the role of breast cancer resistance protein (BCRP) that is also expressed at the BBB is not.
  2. Tanaka Y, Slitt A, Leazer T, Maher J, Klaassen C. Tissue distribution and hormonal regulation of the breast cancer resistance protein (Bcrp/Abcg2) in rats and mice. Biochem Biophys Res Commun. 2005;326:181-7 pubmed
    Breast cancer resistance protein (Bcrp/Abcg2) is a member of the ABC transporter family...
  3. Zhou S, Morris J, Barnes Y, Lan L, Schuetz J, Sorrentino B. Bcrp1 gene expression is required for normal numbers of side population stem cells in mice, and confers relative protection to mitoxantrone in hematopoietic cells in vivo. Proc Natl Acad Sci U S A. 2002;99:12339-44 pubmed
    ..Previous studies have implicated the ATP binding cassette transporter genes Mdr1a/1b and/or Bcrp1 in the SP phenotype...
  4. Jonker J, Freeman J, Bolscher E, Musters S, Alvi A, Titley I, et al. Contribution of the ABC transporters Bcrp1 and Mdr1a/1b to the side population phenotype in mammary gland and bone marrow of mice. Stem Cells. 2005;23:1059-65 pubmed
    ..The ATP-binding cassette transporters Bcrp1 (Abcg2) and Mdr1a/1b (Abcb1a/1b) have been implicated as being responsible for this phenotype...
  5. Tadjali M, Zhou S, Rehg J, Sorrentino B. Prospective isolation of murine hematopoietic stem cells by expression of an Abcg2/GFP allele. Stem Cells. 2006;24:1556-63 pubmed
    ..The Abcg2 transporter is expressed in hematopoietic stem cells (HSCs) and confers this dye efflux activity...
  6. Hartz A, Madole E, Miller D, Bauer B. Estrogen receptor beta signaling through phosphatase and tensin homolog/phosphoinositide 3-kinase/Akt/glycogen synthase kinase 3 down-regulates blood-brain barrier breast cancer resistance protein. J Pharmacol Exp Ther. 2010;334:467-76 pubmed publisher
    Breast cancer resistance protein (BCRP) is an ATP-driven efflux pump at the blood-brain barrier that limits central nervous system pharmacotherapy...
  7. Martin C, Ferdous A, Gallardo T, Humphries C, Sadek H, Caprioli A, et al. Hypoxia-inducible factor-2alpha transactivates Abcg2 and promotes cytoprotection in cardiac side population cells. Circ Res. 2008;102:1075-81 pubmed publisher
    ..We have previously established that the multidrug resistance protein Abcg2 is the molecular determinant of the side population (SP) progenitor cell population...
  8. Merino G, van Herwaarden A, Wagenaar E, Jonker J, Schinkel A. Sex-dependent expression and activity of the ATP-binding cassette transporter breast cancer resistance protein (BCRP/ABCG2) in liver. Mol Pharmacol. 2005;67:1765-71 pubmed
    The breast cancer resistance protein (BCRP/ABCG2) is an ATP-binding cassette drug efflux transporter present in the liver and other tissues that affects the pharmacological behavior of many compounds...
  9. Shimizu T, Sugiura T, Wakayama T, Kijima A, Nakamichi N, Iseki S, et al. PDZK1 regulates breast cancer resistance protein in small intestine. Drug Metab Dispos. 2011;39:2148-54 pubmed publisher
    ..blot analysis of intestinal brush-border membranes revealed that expression of breast cancer resistance protein (BCRP) but not of P-glycoprotein is reduced in pdzk1(-/-) mice...
  10. Zhou S, Schuetz J, Bunting K, Colapietro A, Sampath J, Morris J, et al. The ABC transporter Bcrp1/ABCG2 is expressed in a wide variety of stem cells and is a molecular determinant of the side-population phenotype. Nat Med. 2001;7:1028-34 pubmed
    ..Here we show that expression of the Bcrp1 (also known as Abcg2 murine/ABCG2 human) gene is a conserved feature of stem cells from a wide variety of sources...
  11. Fatima S, Zhou S, Sorrentino B. Abcg2 expression marks tissue-specific stem cells in multiple organs in a mouse progeny tracking model. Stem Cells. 2012;30:210-21 pubmed publisher
    The side population phenotype is associated with the Hoechst dye efflux activity of the Abcg2 transporter and identifies hematopoietic stem cells (HSCs) in the bone marrow...
  12. de Waart D, Vlaming M, Kunne C, Schinkel A, Oude Elferink R. Complex pharmacokinetic behavior of ezetimibe depends on abcc2, abcc3, and abcg2. Drug Metab Dispos. 2009;37:1698-702 pubmed publisher
    ..Abcc2, Abcc3, and Abcg2 are ATP-binding cassette (ABC) transporters that are expressed in both liver and intestine and are capable of ..
  13. Bihorel S, Camenisch G, Lemaire M, Scherrmann J. Influence of breast cancer resistance protein (Abcg2) and p-glycoprotein (Abcb1a) on the transport of imatinib mesylate (Gleevec) across the mouse blood-brain barrier. J Neurochem. 2007;102:1749-57 pubmed
    ..by p-glycoprotein (p-gp or multidrug resistance protein Mdr1a), and probably by breast cancer resistance protein (Bcrp1), two efflux pumps expressed at the blood-brain barrier (BBB)...
  14. Yang Z, Zhu W, Gao S, Yin T, Jiang W, Hu M. Breast cancer resistance protein (ABCG2) determines distribution of genistein phase II metabolites: reevaluation of the roles of ABCG2 in the disposition of genistein. Drug Metab Dispos. 2012;40:1883-93 pubmed publisher
    It was recently proposed that the improved oral bioavailability of genistein aglycone and conjugates in Bcrp1(-/-) mice is mainly due to increased intestinal absorption of aglycone and subsequent elevated exposure to conjugation enzymes...
  15. Zander S, Kersbergen A, van der Burg E, de Water N, van Tellingen O, Gunnarsdottir S, et al. Sensitivity and acquired resistance of BRCA1;p53-deficient mouse mammary tumors to the topoisomerase I inhibitor topotecan. Cancer Res. 2010;70:1700-10 pubmed publisher
    ..As mechanisms of in vivo resistance, we identified overexpression of Abcg2/Bcrp and markedly reduced protein levels of the drug target Top1 (without altered mRNA levels)...
  16. Shen S, Callaghan D, Juzwik C, Xiong H, Huang P, Zhang W. ABCG2 reduces ROS-mediated toxicity and inflammation: a potential role in Alzheimer's disease. J Neurochem. 2010;114:1590-604 pubmed publisher
    ..We have previously observed that, in Alzheimer's disease brain, ABCG2 is up-regulated and AP-1 is activated, but NF-?B is not activated...
  17. Gnana Prakasam J, Reddy S, Veeranan Karmegam R, Smith S, Martin P, Ganapathy V. Polarized distribution of heme transporters in retinal pigment epithelium and their regulation in the iron-overload disease hemochromatosis. Invest Ophthalmol Vis Sci. 2011;52:9279-86 pubmed publisher
    FLVCR, BCRP, and PCFT/HCP-1 represent the three heme transporters identified thus far in mammalian cells, but there is very little known about their expression and regulation in the retina...
  18. Brayboy L, Oulhen N, Long S, Voigt N, Raker C, Wessel G. Multidrug resistance transporter-1 and breast cancer resistance protein protect against ovarian toxicity, and are essential in ovarian physiology. Reprod Toxicol. 2017;69:121-131 pubmed publisher
    ..Here we use genetic deletions in MDR1a/b/BCRP of mice to test MDR function in ovarian somatic cells and find that mdr1a/b/bcrp-/- mice had significantly ..
  19. Takenaka K, Morgan J, Scheffer G, Adachi M, Stewart C, Sun D, et al. Substrate overlap between Mrp4 and Abcg2/Bcrp affects purine analogue drug cytotoxicity and tissue distribution. Cancer Res. 2007;67:6965-72 pubmed
    ..of the purine nucleotide analogue, 9-(2-(phosphonomethoxy)ethyl)-adenine (PMEA), and up-regulation of Abcg2 in some tissues of the Mrp4 KO mouse prompted us to evaluate the possibility that Abcg2 might transport purine-..
  20. Schriml L, Dean M. Identification of 18 mouse ABC genes and characterization of the ABC superfamily in Mus musculus. Genomics. 2000;64:24-31 pubmed
    ..The mouse ABC genes could be grouped into the seven previously described human ABC subfamilies. Three mouse ABC genes mapped to regions implicated in cholesterol gallstone susceptibility...
  21. Brendel C, Scharenberg C, Dohse M, Robey R, Bates S, Shukla S, et al. Imatinib mesylate and nilotinib (AMN107) exhibit high-affinity interaction with ABCG2 on primitive hematopoietic stem cells. Leukemia. 2007;21:1267-75 pubmed
    ..The ATP binding-cassette transporters ABCB1 (MDR-1; P-glycoprotein) and ABCG2 are highly expressed on primitive hematopoietic stem cells (HSCs) and have been shown to interact with TKIs...
  22. Kim Y, Kwon H, Shinozaki N, Hashimoto S, Shimono M, Cho S, et al. Comparative analysis of ABCG2-expressing and label-retaining cells in mouse submandibular gland. Cell Tissue Res. 2008;334:47-53 pubmed publisher
    ..We found that LRCs were distributed in the acinus, duct, myoepithelium, and connective tissue. Moreover, ABCG2 (a known stem cell marker) was used for the characterization of LRCs and the localization of cells as putative ..
  23. Fukuda Y, Cheong P, Lynch J, Brighton C, Frase S, Kargas V, et al. The severity of hereditary porphyria is modulated by the porphyrin exporter and Lan antigen ABCB6. Nat Commun. 2016;7:12353 pubmed publisher
    ..Collectively, these studies support ABCB6 role as a genetic modifier of porphyria and suggest that porphyrin-inducing drugs may produce excessive toxicities in individuals with the rare Lan(-) blood type. ..
  24. Kort A, Sparidans R, Wagenaar E, Beijnen J, Schinkel A. Brain accumulation of the EML4-ALK inhibitor ceritinib is restricted by P-glycoprotein (P-GP/ABCB1) and breast cancer resistance protein (BCRP/ABCG2). Pharmacol Res. 2015;102:200-7 pubmed publisher
    We aimed to clarify the roles of the multidrug transporters ABCB1 and ABCG2 in oral availability and brain accumulation of ceritinib, an oral anaplastic lymphoma kinase (ALK) inhibitor used to treat metastatic non-small cell lung cancer (..
  25. Lin F, de Gooijer M, Roig E, Buil L, Christner S, Beumer J, et al. ABCB1, ABCG2, and PTEN determine the response of glioblastoma to temozolomide and ABT-888 therapy. Clin Cancer Res. 2014;20:2703-13 pubmed publisher
    ..We have elucidated important factors controlling ABT-888 efficacy in glioblastoma...
  26. Higashikuni Y, Sainz J, Nakamura K, Takaoka M, Enomoto S, Iwata H, et al. The ATP-binding cassette transporter ABCG2 protects against pressure overload-induced cardiac hypertrophy and heart failure by promoting angiogenesis and antioxidant response. Arterioscler Thromb Vasc Biol. 2012;32:654-61 pubmed publisher
    ATP-binding cassette transporter subfamily G member 2 (ABCG2), expressed in microvascular endothelial cells in the heart, has been suggested to regulate several tissue defense mechanisms...
  27. Alvarez A, Vallejo F, Barrera B, Merino G, Prieto J, Tomás Barberán F, et al. Bioavailability of the glucuronide and sulfate conjugates of genistein and daidzein in breast cancer resistance protein 1 knockout mice. Drug Metab Dispos. 2011;39:2008-12 pubmed publisher
    ..Breast cancer resistance protein (ABCG2/BCRP) interacts with genistein and daidzein, which are among the natural substrates of the transporter and ..
  28. Allen J, Brinkhuis R, Wijnholds J, Schinkel A. The mouse Bcrp1/Mxr/Abcp gene: amplification and overexpression in cell lines selected for resistance to topotecan, mitoxantrone, or doxorubicin. Cancer Res. 1999;59:4237-41 pubmed
    ..Each of the resulting drug-resistant lines showed marked gene amplification of Bcrp1, the mouse homologue of the human ATP-binding cassette transporter gene BCRP/MXR/ABCP, and greatly elevated ..
  29. Chow K, Fessel J, Kaoriihida Stansbury -, Schmidt E, Gaskill C, Alvarez D, et al. Dysfunctional resident lung mesenchymal stem cells contribute to pulmonary microvascular remodeling. Pulm Circ. 2013;3:31-49 pubmed publisher
    ..We crossed (floxp)sod3 and mT/mG reporter mice to a strain expressing Cre recombinase under the control of the ABCG2 promoter...
  30. Lin F, Buil L, Sherris D, Beijnen J, van Tellingen O. Dual mTORC1 and mTORC2 inhibitor Palomid 529 penetrates the blood-brain barrier without restriction by ABCB1 and ABCG2. Int J Cancer. 2013;133:1222-33 pubmed publisher
    ..of Palomid 529 with ATP-binding cassette (ABC) drug efflux transporters ABCB1 (P-gp/P-glycoprotein) and ABCG2 (BCRP/Breast Cancer Resistant Protein) by in vitro transwell assays, and their effects on the brain penetration ..
  31. Yasuda K, Cline C, Vogel P, Onciu M, Fatima S, Sorrentino B, et al. Drug transporters on arachnoid barrier cells contribute to the blood-cerebrospinal fluid barrier. Drug Metab Dispos. 2013;41:923-31 pubmed publisher
    ..Immunohistochemical analysis showed P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) in mouse AB cells but not other meningeal tissue...
  32. Scharenberg C, Mannowetz N, Robey R, Brendel C, Repges P, Sahrhage T, et al. ABCG2 is expressed in late spermatogenesis and is associated with the acrosome. Biochem Biophys Res Commun. 2009;378:302-7 pubmed publisher
    ..for the isolation of stem cells is based on the increased efflux of Hoechst 33342 lipophilic dye mediated by ABCG2, an ATP-binding cassette transporter which is highly expressed in various stem cells...
  33. Yamagata T, Kusuhara H, Morishita M, Takayama K, Benameur H, Sugiyama Y. Improvement of the oral drug absorption of topotecan through the inhibition of intestinal xenobiotic efflux transporter, breast cancer resistance protein, by excipients. Drug Metab Dispos. 2007;35:1142-8 pubmed
    Recently, breast cancer resistance protein (BCRP/ABCG2) has been shown to limit the oral absorption of its substrates in the intestine...
  34. Bakhsheshian J, Hall M, Robey R, Herrmann M, Chen J, Bates S, et al. Overlapping substrate and inhibitor specificity of human and murine ABCG2. Drug Metab Dispos. 2013;41:1805-12 pubmed publisher
    b>ABCG2 (also known as breast cancer resistance protein) is an ATP-binding cassette (ABC) transporter localized to the plasma membrane where it mediates the efflux of xenobiotics, including potential therapeutics...
  35. Nakanishi H, Yonezawa A, Matsubara K, Yano I. Impact of P-glycoprotein and breast cancer resistance protein on the brain distribution of antiepileptic drugs in knockout mouse models. Eur J Pharmacol. 2013;710:20-8 pubmed publisher
    ..of ATP-binding cassette transporters such as P-glycoprotein (Pgp) and breast cancer resistance protein (Bcrp)...
  36. van de Wetering K, Sapthu S. ABCG2 functions as a general phytoestrogen sulfate transporter in vivo. FASEB J. 2012;26:4014-24 pubmed publisher
    b>ABCG2 is an ATP-dependent efflux transporter that limits the systemic exposure of its substrates. The preferred substrates of ABCG2 in vivo are largely unknown...
  37. Jonker J, Merino G, Musters S, van Herwaarden A, Bolscher E, Wagenaar E, et al. The breast cancer resistance protein BCRP (ABCG2) concentrates drugs and carcinogenic xenotoxins into milk. Nat Med. 2005;11:127-9 pubmed
    ..Here we show that the multidrug transporter BCRP (encoded by ABCG2) is strongly induced in the mammary gland of mice, cows and humans during lactation and that it is responsible for ..
  38. Choi J, Song J, Lee M, Cho W, Chung J, Lyoo C, et al. P-Glycoprotein, not BCRP, Limits the Brain Uptake of [(18)F]Mefway in Rodent Brain. Mol Imaging Biol. 2016;18:267-73 pubmed publisher
    ..2 SUV in the triple knockout mice (tKO, Mdr1a/b((-/-))Bcrp1((-/-))) was comparable to that of the double knockout mice (dKO, Mdr1a/b((-/-))) and 2-fold those of the wild-type ..
  39. Hasegawa M, Kusuhara H, Adachi M, Schuetz J, Takeuchi K, Sugiyama Y. Multidrug resistance-associated protein 4 is involved in the urinary excretion of hydrochlorothiazide and furosemide. J Am Soc Nephrol. 2007;18:37-45 pubmed
    ..vesicles that expressed multidrug resistance-associated protein 4 (MRP4) and breast cancer resistance protein (BCRP)...
  40. Gavrilova O, Geyer J, Petzinger E. In vivo relevance of Mrp2-mediated biliary excretion of the Amanita mushroom toxin demethylphalloin. Biochim Biophys Acta. 2007;1768:2070-7 pubmed
    ..and in Mrp2 deficient TR(-) Wistar rats as well as in normal wild-type FVB mice, Mdr1a,b(-/-) knockout mice, and Bcrp1(-/-) knockout mice by in situ bile duct/gallbladder cannulation. A subtoxic dose of 0.03 mg DMP/kg b.w...
  41. Susanto J, Lin Y, Chen Y, Shen C, Yan Y, Tsai S, et al. Porphyrin homeostasis maintained by ABCG2 regulates self-renewal of embryonic stem cells. PLoS ONE. 2008;3:e4023 pubmed publisher
    ..The ATP binding cassette transporter ABCG2 is expressed in a wide variety of somatic and embryonic stem cells...
  42. Rong Z, Xu Y, Zhang C, Xiang D, Li X, Liu D. Evaluation of intestinal absorption of amtolmetin guacyl in rats: breast cancer resistant protein as a primary barrier of oral bioavailability. Life Sci. 2013;92:245-51 pubmed publisher
    ..The purpose of the present study was to investigate the role of efflux transporters on the intestinal absorption of amtolmetin guacyl (MED-15)...
  43. Pan G, Giri N, Elmquist W. Abcg2/Bcrp1 mediates the polarized transport of antiretroviral nucleosides abacavir and zidovudine. Drug Metab Dispos. 2007;35:1165-73 pubmed
    ..this study was to characterize the interaction of these nucleoside reverse transcriptase inhibitors with the Abcg2/Bcrp1 transporter, the murine homolog of human breast cancer resistance protein (BCRP), using a Bcrp1-transfected Madin-..
  44. Cisternino S, Mercier C, Bourasset F, Roux F, Scherrmann J. Expression, up-regulation, and transport activity of the multidrug-resistance protein Abcg2 at the mouse blood-brain barrier. Cancer Res. 2004;64:3296-301 pubmed
    The breast cancer resistance protein (BCRP/ABCG2) is, like P-glycoprotein (P-gp), a member of the ABC family of drug transporters. These proteins actively transport various anticancer drugs from cells, causing multidrug resistance...
  45. de Vries N, Buckle T, Zhao J, Beijnen J, Schellens J, van Tellingen O. Restricted brain penetration of the tyrosine kinase inhibitor erlotinib due to the drug transporters P-gp and BCRP. Invest New Drugs. 2012;30:443-9 pubmed publisher
    ..As erlotinib is a known substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) we have investigated the effect of these ABC-transporters on the brain penetration of erlotinib.
  46. Tam J, Vemuri V, Liu J, Batkai S, Mukhopadhyay B, Godlewski G, et al. Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity. J Clin Invest. 2010;120:2953-66 pubmed publisher
    ..These results suggest that targeting peripheral CB1R has therapeutic potential for alleviating cardiometabolic risk in obese patients. ..
  47. Ueno H, Ferrari G, Hattori T, Saban D, Katikireddy K, Chauhan S, et al. Dependence of corneal stem/progenitor cells on ocular surface innervation. Invest Ophthalmol Vis Sci. 2012;53:867-72 pubmed publisher
    ..The purpose of this study was to identify the relationship between corneolimbal epithelial progenitor/stem cells and sensory nerves using a denervated mouse model of NK...
  48. Hamdan A, Koyanagi S, Wada E, Kusunose N, Murakami Y, Matsunaga N, et al. Intestinal expression of mouse Abcg2/breast cancer resistance protein (BCRP) gene is under control of circadian clock-activating transcription factor-4 pathway. J Biol Chem. 2012;287:17224-31 pubmed publisher
    b>ABCG2, encoding breast cancer resistance protein (BCRP), is a member of the ATP-binding cassette transporter family and is often associated with cancer chemotherapeutic resistance...
  49. An G, Gallegos J, Morris M. The bioflavonoid kaempferol is an Abcg2 substrate and inhibits Abcg2-mediated quercetin efflux. Drug Metab Dispos. 2011;39:426-32 pubmed publisher
    ..6-fold (from 97.5 to 8.37) in the presence of kaempferol in MDCK/Bcrp1 cells, indicating that kaempferol is a Bcrp inhibitor...
  50. Karthikeyan C, Malla R, Ashby C, Amawi H, Abbott K, Moore J, et al. Pyrimido[1″,2″:1,5]pyrazolo[3,4-b]quinolines: Novel compounds that reverse ABCG2-mediated resistance in cancer cells. Cancer Lett. 2016;376:118-26 pubmed publisher
    ..the effect of eight novel pyrimido[1″,2″:1,5]pyrazolo[3,4-b]quinoline (IND) derivatives that inhibit ABCG2 transporter restoring cancer cell chemosensitivity...
  51. Tang S, Nguyen L, Sparidans R, Wagenaar E, Beijnen J, Schinkel A. Increased oral availability and brain accumulation of the ALK inhibitor crizotinib by coadministration of the P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar. Int J Cancer. 2014;134:1484-94 pubmed publisher
    ..We used knockout mice to study the roles of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) in plasma pharmacokinetics and brain accumulation of oral crizotinib, and the feasibility of improving crizotinib ..
  52. Leggas M, Panetta J, Zhuang Y, Schuetz J, Johnston B, Bai F, et al. Gefitinib modulates the function of multiple ATP-binding cassette transporters in vivo. Cancer Res. 2006;66:4802-7 pubmed
    ..these effects have primarily been attributed to the inhibition of breast cancer resistance protein (BCRP; ABCG2)...
  53. Wright J, Haslam I, Coleman T, Simmons N. Breast cancer resistance protein BCRP (ABCG2)-mediated transepithelial nitrofurantoin secretion and its regulation in human intestinal epithelial (Caco-2) layers. Eur J Pharmacol. 2011;672:70-6 pubmed publisher
    In order to determine the capacity and regulation of the breast cancer resistance protein (BCRP)-mediated transport in intact human intestinal epithelial monolayers (Caco-2) in which multiple ABC transporters are expressed, nitrofurantoin ..
  54. Hoque M, Shah A, More V, Miller D, Bendayan R. In vivo and ex vivo regulation of breast cancer resistant protein (Bcrp) by peroxisome proliferator-activated receptor alpha (Pparα) at the blood-brain barrier. J Neurochem. 2015;135:1113-22 pubmed publisher
    Breast cancer resistance protein (Bcrp/Abcg2) localized at the blood-brain barrier (BBB) limits permeability into the brain of many xenobiotics, including pharmacological agents...
  55. Zong Y, Zhou S, Fatima S, Sorrentino B. Expression of mouse Abcg2 mRNA during hematopoiesis is regulated by alternative use of multiple leader exons and promoters. J Biol Chem. 2006;281:29625-32 pubmed
    b>ABCG2 encodes a transmembrane transporter associated with multidrug resistance in various cancer cells...
  56. Doyle M, Zhou S, Tanaka K, Pisconti A, Farina N, Sorrentino B, et al. Abcg2 labels multiple cell types in skeletal muscle and participates in muscle regeneration. J Cell Biol. 2011;195:147-63 pubmed publisher
    ..It also contains muscle side population (SP) cells, which express Abcg2 and may participate in muscle regeneration or may represent a source of satellite cell replenishment...
  57. Geschwind D, Ou J, Easterday M, Dougherty J, Jackson R, Chen Z, et al. A genetic analysis of neural progenitor differentiation. Neuron. 2001;29:325-39 pubmed
    ..This combination of methods demonstrates the power of using custom microarrays derived from RDA-subtracted libraries for both gene discovery and gene expression analysis in the central nervous system. ..
  58. Sawicki W, Kujawa M, Jankowska Steifer E, Mystkowska E, Hyc A, Kowalewski C. Temporal/spatial expression and efflux activity of ABC transporter, P-glycoprotein/Abcb1 isoforms and Bcrp/Abcg2 during early murine development. Gene Expr Patterns. 2006;6:738-46 pubmed
    ..Here, we present the study of temporal/spatial patterns of Abcb1 isoforms and Abcg2 transporter expression and efflux activity in pre- and early postimplantation murine embryos...
  59. Cattelotte J, Tournier N, Rizzo Padoin N, Schinkel A, Scherrmann J, Cisternino S. Changes in dipole membrane potential at the mouse blood-brain barrier enhance the transport of 99mTechnetium Sestamibi more than inhibiting Abcb1, Abcc1, or Abcg2. J Neurochem. 2009;108:767-75 pubmed publisher
    ..influence of BBB features like the ATP-binding cassette transporters (Abcb1/P-glycoprotein (P-gp), Abcc1/Mrp1, and Abcg2/Bcrp), organic cation transporters (Slc22a1-3/Oct1-3), the transmembrane potential and the dipole membrane ..
  60. Chapy H, Saubaméa B, Tournier N, Bourasset F, Behar Cohen F, Declèves X, et al. Blood-brain and retinal barriers show dissimilar ABC transporter impacts and concealed effect of P-glycoprotein on a novel verapamil influx carrier. Br J Pharmacol. 2016;173:497-510 pubmed publisher
    The respective impact and interplay between ABC (P-glycoprotein/P-gp/Abcb1a, BCRP/ABCG2, MRP/ABCC) and SLC transporter functions at the blood-brain barrier (BBB) and blood-retinal barriers (BRB) are incompletely understood...
  61. Vlaming M, van Esch A, Pala Z, Wagenaar E, van de Wetering K, van Tellingen O, et al. Abcc2 (Mrp2), Abcc3 (Mrp3), and Abcg2 (Bcrp1) are the main determinants for rapid elimination of methotrexate and its toxic metabolite 7-hydroxymethotrexate in vivo. Mol Cancer Ther. 2009;8:3350-9 pubmed publisher
    The multidrug transporters ABCC2, ABCC3, and ABCG2 can eliminate potentially toxic compounds from the body and have overlapping substrate specificities...
  62. Signer R, Magee J, Salic A, Morrison S. Haematopoietic stem cells require a highly regulated protein synthesis rate. Nature. 2014;509:49-54 pubmed publisher
    ..Pten deficiency thus depletes HSCs and promotes leukaemia partly by increasing protein synthesis. Either increased or decreased protein synthesis impairs HSC function. ..
  63. Zander S, Kersbergen A, Sol W, Gonggrijp M, van de Wetering K, Jonkers J, et al. Lack of ABCG2 shortens latency of BRCA1-deficient mammary tumors and this is not affected by genistein or resveratrol. Cancer Prev Res (Phila). 2012;5:1053-60 pubmed publisher
    In addition to their role in drug resistance, the ATP-binding cassette (ABC) transporters ABCG2 and ABCB1 have been suggested to protect cells from a broad range of substances that may foster tumorigenesis...
  64. Durmus S, Xu N, Sparidans R, Wagenaar E, Beijnen J, Schinkel A. P-glycoprotein (MDR1/ABCB1) and breast cancer resistance protein (BCRP/ABCG2) restrict brain accumulation of the JAK1/2 inhibitor, CYT387. Pharmacol Res. 2013;76:9-16 pubmed publisher
    ..In vitro, CYT387 was efficiently transported by both human MDR1 and BCRP, and very efficiently by mouse Bcrp1 and its transport could be inhibited by specific MDR1 inhibitor, zosuquidar and/or specific BCRP inhibitor, Ko143...
  65. Takada T, Ichida K, Matsuo H, Nakayama A, Murakami K, Yamanashi Y, et al. ABCG2 dysfunction increases serum uric acid by decreased intestinal urate excretion. Nucleosides Nucleotides Nucleic Acids. 2014;33:275-81 pubmed publisher
    ..G2 (ABCG2), also known as breast cancer resistance protein (BCRP), is identified as a high-capacity urate exporter and its dysfunction has an association with serum uric acid (SUA) levels and gout/hyperuricemia risk...
  66. Marriott S, Baskir R, Gaskill C, Menon S, Carrier E, Williams J, et al. ABCG2pos lung mesenchymal stem cells are a novel pericyte subpopulation that contributes to fibrotic remodeling. Am J Physiol Cell Physiol. 2014;307:C684-98 pubmed publisher
    ..Adult lung tissue contains a population of perivascular ABCG2(pos) mesenchymal stem cells (MSC) that are precursors of myofibroblasts and distinct from NG2 pericytes...
  67. Hartz A, Mahringer A, Miller D, Bauer B. 17-?-Estradiol: a powerful modulator of blood-brain barrier BCRP activity. J Cereb Blood Flow Metab. 2010;30:1742-55 pubmed publisher
    The ATP-driven efflux transporter, breast cancer resistance protein (BCRP), handles many therapeutic drugs, including chemotherapeutics, limiting their ability to cross the blood-brain barrier...
  68. Pfister O, Oikonomopoulos A, Sereti K, Sohn R, Cullen D, Fine G, et al. Role of the ATP-binding cassette transporter Abcg2 in the phenotype and function of cardiac side population cells. Circ Res. 2008;103:825-35 pubmed publisher
    ..SP cells are identified and characterized by a unique efflux of Hoechst 33342 dye. Abcg2 belongs to the ATP-binding cassette (ABC) transporter superfamily and constitutes the molecular basis for the dye ..
  69. De Wolf C, Yamaguchi H, van der Heijden I, Wielinga P, Hundscheid S, Ono N, et al. cGMP transport by vesicles from human and mouse erythrocytes. FEBS J. 2007;274:439-50 pubmed
    ..by the ABCC4-specific substrate prostaglandin E1, cGMP transport into mouse vesicles was inhibited equally by Abcg2 and Abcc4 inhibitors/substrates...
  70. van Herwaarden A, Wagenaar E, Karnekamp B, Merino G, Jonker J, Schinkel A. 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. Carcinogenesis. 2006;27:123-30 pubmed
    The breast cancer resistance protein (BCRP/ABCG2) usually protects the body from a wide variety of environmental and dietary xenotoxins by reducing their net uptake from intestine and by increasing their hepatobiliary, intestinal and ..
  71. Chang H, Huang W, Lin S, Huang W, Shen C, Mao W, et al. ABCG2 deficiency in skin impairs re-epithelialization in cutaneous wound healing. Exp Dermatol. 2016;25:355-61 pubmed publisher
    The ATP-binding cassette transporter ABCG2 is expressed in the interfollicular epidermis and mediates the side-population phenotype in skin cells. However, the role of ABCG2 in skin is unclear...
  72. Real R, Egido E, Perez M, Gonzalez Lobato L, Barrera B, Prieto J, et al. Involvement of breast cancer resistance protein (BCRP/ABCG2) in the secretion of danofloxacin into milk: interaction with ivermectin. J Vet Pharmacol Ther. 2011;34:313-21 pubmed publisher
    ..The main purpose was to determine whether danofloxacin is an in vitro substrate for Bcrp1/BCRP and to assess its involvement in danofloxacin secretion into milk...
  73. Tomioka N, Tamura Y, Takada T, Shibata S, Suzuki H, Uchida S, et al. Immunohistochemical and in situ hybridization study of urate transporters GLUT9/URATv1, ABCG2, and URAT1 in the murine brain. Fluids Barriers CNS. 2016;13:22 pubmed
    ..and highly-sensitive in situ hybridization was used to assess the distribution of UA transporters: GLUT9/URATv1, ABCG2, and URAT1. Immunostaining for GLUT9 was observed in ependymal cells, neurons, and brain capillaries...
  74. Tang S, Lagas J, Lankheet N, Poller B, Hillebrand M, Rosing H, et al. Brain accumulation of sunitinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by oral elacridar and sunitinib coadministration. Int J Cancer. 2012;130:223-33 pubmed publisher
    ..We aimed to investigate the in vivo roles of the ATP-binding cassette drug efflux transporters ABCB1 and ABCG2 in plasma pharmacokinetics and brain accumulation of oral sunitinib, and the feasibility of improving sunitinib ..
  75. Shukla S, Zaher H, Hartz A, Bauer B, Ware J, Ambudkar S. Curcumin inhibits the activity of ABCG2/BCRP1, a multidrug resistance-linked ABC drug transporter in mice. Pharm Res. 2009;26:480-7 pubmed publisher
    ..of curcumin as an inhibitor of the multidrug-resistance-linked ATP Binding Cassette (ABC) drug transporter, ABCG2. Photoaffinity labeling with [125I]-iodoarylazidoprazosin was used to characterize the interaction of ..
  76. Schumacher T, Krohn M, Hofrichter J, Lange C, Stenzel J, Steffen J, et al. ABC transporters B1, C1 and G2 differentially regulate neuroregeneration in mice. PLoS ONE. 2012;7:e35613 pubmed publisher
    ..Therefore, we sought to determine brain-related phenotypic changes in animals lacking the expression of distinct ABC transporters (ABCB1, ABCG2 or ABCC1).
  77. Dankers A, Sweep F, Pertijs J, Verweij V, van den Heuvel J, Koenderink J, et al. Localization of breast cancer resistance protein (Bcrp) in endocrine organs and inhibition of its transport activity by steroid hormones. Cell Tissue Res. 2012;349:551-63 pubmed publisher
    Breast cancer resistance protein (BCRP) is known for its protective function against the toxic effects of exogenous compounds. In addition to this, a role in the transport of endogenous compounds has been described...
  78. Morfouace M, Cheepala S, Jackson S, Fukuda Y, Patel Y, Fatima S, et al. ABCG2 Transporter Expression Impacts Group 3 Medulloblastoma Response to Chemotherapy. Cancer Res. 2015;75:3879-89 pubmed publisher
    ..Herein we show that among this class of drug transporters, only ABCG2 was expressed at highly increased levels in human G3 medulloblastoma and a mouse model of this disease...
  79. Vlaming M, Teunissen S, van de Steeg E, van Esch A, Wagenaar E, Brunsveld L, et al. Bcrp1;Mdr1a/b;Mrp2 combination knockout mice: altered disposition of the dietary carcinogen PhIP (2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine) and its genotoxic metabolites. Mol Pharmacol. 2014;85:520-30 pubmed publisher
    ..To investigate the overlapping functions of Bcrp1, Mdr1a/b, and Mrp2 in vivo, we generated Bcrp1;Mdr1a/b;Mrp2(-/-) mice, which are viable and fertile...
  80. Ge G, Zhang H, Li R, Liu H. The Function of SDF-1-CXCR4 Axis in SP Cells-Mediated Protective Role for Renal Ischemia/Reperfusion Injury by SHH/GLI1-ABCG2 Pathway. Shock. 2017;47:251-259 pubmed publisher
    ..analysis corroborated that SDF-1/CXCR4 further induced the expression of ATP-binding cassette transporter ABCG2, an essential element for SP-mediated kidney regeneration after renal I/R injury...