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The Bioflavonoid Kaempferol Is an Abcg2 Substrate and Inhibits Abcg2-Mediated Quercetin Efflux
Drug Metabolism and Disposition, 2011The flavonoids quercetin and kaempferol are major constituents of Ginkgo biloba extract. The ATP-binding cassette efflux transporter, breast cancer resistance protein (Bcrp, Abcg2), is involved in the transport of quercetin and represents a possible mechanism for the low bioavailability of quercetin.
Guohua, An +2 more
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Pharmacogenomic Importance of ABCG2
Pharmacogenomics, 2008The ATP-binding cassette transporter ABCG2 (BCRP, MXR and ABCP) is highly expressed in the gastrointestinal tract and liver, and governs absorption, distribution and excretion of a wide variety of clinically important drugs. Common germline polymorphisms in the ABCG2 gene have been described that can affect expression, cellular localization and/or ...
George, Cusatis, Alex, Sparreboom
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Assessing the ABCG2 Protein Interactome: a Potential Strategy to Disrupt ABCG2 Function
The FASEB Journal, 2020The ATP‐binding cassette sub‐family G member 2, ABCG2, is an important plasma membrane transporter that removes potentially harmful endogenous toxins and xenobiotics from cells. ABCG2 was identified as an important contributor to the multidrug resistance phenotype in cancer cells because it exported a wide ...
Ailsa Gavan McHarg +2 more
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Metabolism of KO143, an ABCG2 inhibitor
Drug Metabolism and Pharmacokinetics, 2017The ATP-binding cassette sub-family G member 2 (ABCG2) plays an important role in modulating drug disposition and endobiotic homeostasis. KO143 is a potent and relatively selective ABCG2 inhibitor. We found that the metabolic stability of KO143 was very poor in human liver microsomes (HLM).
Ke, Liu +7 more
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Physiological and pharmacological roles of ABCG2 (BCRP): Recent findings in Abcg2 knockout mice
Advanced Drug Delivery Reviews, 2009The multidrug transporter ABCG2 (BCRP/MXR/ABCP) can actively extrude a broad range of endogenous and exogenous substrates across biological membranes. ABCG2 limits oral availability and mediates hepatobiliary and renal excretion of its substrates, and thus influences the pharmacokinetics of many drugs. Recent work, relying mainly on the use of Abcg2(-/-
Maria L H, Vlaming +2 more
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Comparative analysis of ABCG2+ and ABCG2-retinoblastoma cells in three-dimensional culture
Oncocytology Journal, 2014Aims: Retinoblastoma (Rb) is the most common intraocular malignancy of early childhood. Subpopulations of Rb cells express the stem cell marker ABCG2; yet little is known regarding the differences between ABCG2+ and ABCG2- subpopulations, particularly in threedimensional culture.
Gail M Seigel +3 more
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2021
The multidrug transporter ABCG2 is best known for its ability to efflux a wide variety of compounds, but its aberrant overexpression in cancer can lead to multidrug resistance. ABCG2 plays a role in tumor cell survival by enhancing the rate of autophagy, a conserved, catabolic recycling process that breaks down damaged proteins and cellular organelles ...
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The multidrug transporter ABCG2 is best known for its ability to efflux a wide variety of compounds, but its aberrant overexpression in cancer can lead to multidrug resistance. ABCG2 plays a role in tumor cell survival by enhancing the rate of autophagy, a conserved, catabolic recycling process that breaks down damaged proteins and cellular organelles ...
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The ABCG2 Multidrug Transporter
2015ABCG2 is an ATP-binding cassette (ABC) half-transporter localized to the cell membrane and important in normal physiology, in normal tissue protection including in the maternal-fetal barrier and the blood brain barrier, and potentially in multidrug resistance. Dimerization is required for function.
Agnes Basseville +6 more
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ROLE OF ABCG2/BCRP IN BIOLOGY AND MEDICINE
Annual Review of Pharmacology and Toxicology, 2006▪ Abstract The protein variously named ABCG2/BCRP/MXR/ABCP is a recently described ATP-binding cassette (ABC) transporter originally identified by its ability to confer drug resistance that is independent of Mrp1 (multidrug-resistance protein 1) and Pgp (P-glycoprotein).
P, Krishnamurthy, J D, Schuetz
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Differential inhibition of murine Bcrp1/Abcg2 and human BCRP/ABCG2 by the mycotoxin fumitremorgin C
European Journal of Pharmacology, 2010Breast Cancer Resistance Protein (ABCG2/BCRP) is an ATP-binding cassette transporter expressed in absorptive and excretory organs whose main physiological role is protection of cells against xenobiotics. In addition, ABCG2/BCRP expression has been linked to cellular resistance to anticancer drugs due to the acquisition of a multidrug resistance ...
Lucía, González-Lobato +4 more
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