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Gene Review

Abcg2  -  ATP-binding cassette, sub-family G (WHITE)...

Mus musculus

Synonyms: ABC15, ABCP, AI428558, ATP-binding cassette sub-family G member 2, Abcp, ...
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Disease relevance of Abcg2


High impact information on Abcg2


Chemical compound and disease context of Abcg2


Biological context of Abcg2


Anatomical context of Abcg2


Associations of Abcg2 with chemical compounds


Regulatory relationships of Abcg2

  • Akt signaling regulates side population cell phenotype via Bcrp1 translocation [6].
  • We have found that Abcg2 mRNA expression was up-regulated in differentiating erythroid cells, coinciding with increased expression of other erythroid-specific genes [13].

Other interactions of Abcg2

  • It is noteworthy that the most profound decrease in the biliary clearance of the glucuronide conjugates was observed in Bcrp-deficient mouse livers, although the biliary clearance of 4MUG was also approximately 35% lower in Mrp2-deficient mouse livers [11].
  • Persistent expression of the ATP-binding cassette transporter, Abcg2, identifies cardiac SP cells in the developing and adult heart [4].
  • Therefore, we examined Abcg2 expression during murine embryogenesis and observed robust expression in the blood islands of the E8.5 yolk sac and in developing tissues including the heart [4].
  • Increased expression of the Abcg2 transporter during erythroid maturation plays a role in decreasing cellular protoporphyrin IX levels [13].

Analytical, diagnostic and therapeutic context of Abcg2

  • After oral administration of 20 mg/kg sulfasalazine, the area under the plasma concentration (AUC) time profile in Bcrp1 (abcg2)-/- knockout (KO) mice was approximately 111-fold higher than that in FVB wild-type (WT) mice [3].
  • After single-pass liver perfusion with 1 muM CDF diacetate for 30 min and an additional 30-min perfusion with CDF-free buffer, cumulative biliary excretion of CDF in Abcg2-/- mice was significantly higher than in wild-type mice (65 +/- 6 and 47 +/- 15% of dose, respectively, p < 0.05), whereas CDF recovery in bile of Abcc2-/- mice was negligible [14].
  • Furthermore, gonadectomy and hypophysectomy experiments were conducted to determine whether sex steroids and/or growth hormone are responsible for Bcrp gender-divergent expression patterns [1].
  • METHODS: The transport activity of ME3277 in the presence and absence of ATP was determined using a rapid filtration method with the membrane vesicles prepared from LLC-PK1 cells expressing BCRP [15].
  • Interaction with BCRP was examined with a mitoxantrone-efflux assay in BCRP-overexpressing MCF7/mx cells, with flow cytometry [16].


  1. Tissue distribution and hormonal regulation of the breast cancer resistance protein (Bcrp/Abcg2) in rats and mice. Tanaka, Y., Slitt, A.L., Leazer, T.M., Maher, J.M., Klaassen, C.D. Biochem. Biophys. Res. Commun. (2005) [Pubmed]
  2. 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. Zhou, S., Morris, J.J., Barnes, Y., Lan, L., Schuetz, J.D., Sorrentino, B.P. Proc. Natl. Acad. Sci. U.S.A. (2002) [Pubmed]
  3. Breast cancer resistance protein (Bcrp/abcg2) is a major determinant of sulfasalazine absorption and elimination in the mouse. Zaher, H., Khan, A.A., Palandra, J., Brayman, T.G., Yu, L., Ware, J.A. Mol. Pharm. (2006) [Pubmed]
  4. Persistent expression of the ATP-binding cassette transporter, Abcg2, identifies cardiac SP cells in the developing and adult heart. Martin, C.M., Meeson, A.P., Robertson, S.M., Hawke, T.J., Richardson, J.A., Bates, S., Goetsch, S.C., Gallardo, T.D., Garry, D.J. Dev. Biol. (2004) [Pubmed]
  5. Cellular and molecular regulation of skeletal muscle side population cells. Meeson, A.P., Hawke, T.J., Graham, S., Jiang, N., Elterman, J., Hutcheson, K., Dimaio, J.M., Gallardo, T.D., Garry, D.J. Stem Cells (2004) [Pubmed]
  6. Akt signaling regulates side population cell phenotype via Bcrp1 translocation. Mogi, M., Yang, J., Lambert, J.F., Colvin, G.A., Shiojima, I., Skurk, C., Summer, R., Fine, A., Quesenberry, P.J., Walsh, K. J. Biol. Chem. (2003) [Pubmed]
  7. Contribution of the ABC transporters Bcrp1 and Mdr1a/1b to the side population phenotype in mammary gland and bone marrow of mice. Jonker, J.W., Freeman, J., Bolscher, E., Musters, S., Alvi, A.J., Titley, I., Schinkel, A.H., Dale, T.C. Stem Cells (2005) [Pubmed]
  8. A mutation hot spot in the Bcrp1 (Abcg2) multidrug transporter in mouse cell lines selected for Doxorubicin resistance. Allen, J.D., Jackson, S.C., Schinkel, A.H. Cancer Res. (2002) [Pubmed]
  9. Prospective isolation of murine hematopoietic stem cells by expression of an Abcg2/GFP allele. Tadjali, M., Zhou, S., Rehg, J., Sorrentino, B.P. Stem Cells (2006) [Pubmed]
  10. Hematopoietic cells from mice that are deficient in both Bcrp1/Abcg2 and Mdr1a/1b develop normally but are sensitized to mitoxantrone. Zhou, S., Zong, Y., Lu, T., Sorrentino, B.P. BioTechniques (2003) [Pubmed]
  11. The important role of bcrp (abcg2) in the biliary excretion of sulfate and glucuronide metabolites of acetaminophen, 4-methylumbelliferone, and harmol in mice. Zamek-Gliszczynski, M.J., Nezasa, K., Tian, X., Kalvass, J.C., Patel, N.J., Raub, T.J., Brouwer, K.L. Mol. Pharmacol. (2006) [Pubmed]
  12. Substrate overlap between Mrp4 and Abcg2/Bcrp affects purine analogue drug cytotoxicity and tissue distribution. Takenaka, K., Morgan, J.A., Scheffer, G.L., Adachi, M., Stewart, C.F., Sun, D., Leggas, M., Ejendal, K.F., Hrycyna, C.A., Schuetz, J.D. Cancer Res. (2007) [Pubmed]
  13. Increased expression of the Abcg2 transporter during erythroid maturation plays a role in decreasing cellular protoporphyrin IX levels. Zhou, S., Zong, Y., Ney, P.A., Nair, G., Stewart, C.F., Sorrentino, B.P. Blood (2005) [Pubmed]
  14. Altered hepatobiliary disposition of 5 (and 6)-carboxy-2',7'-dichlorofluorescein in Abcg2 (Bcrp1) and Abcc2 (Mrp2) knockout mice. Nezasa, K., Tian, X., Zamek-Gliszczynski, M.J., Patel, N.J., Raub, T.J., Brouwer, K.L. Drug Metab. Dispos. (2006) [Pubmed]
  15. 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). Kondo, C., Onuki, R., Kusuhara, H., Suzuki, H., Suzuki, M., Okudaira, N., Kojima, M., Ishiwata, K., Jonker, J.W., Sugiyama, Y. Pharm. Res. (2005) [Pubmed]
  16. In vitro and in vivo evaluation of WK-X-34, a novel inhibitor of P-glycoprotein and BCRP, using radio imaging techniques. Jekerle, V., Klinkhammer, W., Scollard, D.A., Breitbach, K., Reilly, R.M., Piquette-Miller, M., Wiese, M. Int. J. Cancer (2006) [Pubmed]
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