Results 121 to 130 of about 19,287 (163)

Sensitization of ABCG2-overexpressing cells to conventional chemotherapeutic agent by sunitinib was associated with inhibiting the function of ABCG2

Cancer Letters, 2009
Sunitinib is an ATP-competitive multi-targeted tyrosine kinase inhibitor. In this study, we evaluated the possible interaction of sunitinib with P-glycoprotein (P-gp, ABCB1), multidrug resistance protein 1 (MRP1, ABCC1), breast cancer resistance protein (BCRP, ABCG2) and lung-resistance protein (LRP) in vitro.
Liwu Fu, Amit Tiwari, Zhe-Sheng Chen
exaly   +3 more sources

The Bioflavonoid Kaempferol Is an Abcg2 Substrate and Inhibits Abcg2-Mediated Quercetin Efflux

Drug Metabolism and Disposition, 2011
The 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, Jorge, Gallegos, Marilyn E, Morris   +2 more
openaire   +2 more sources

Pharmacogenomic Importance of ABCG2

Pharmacogenomics, 2008
The 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
openaire   +2 more sources

Design of Inhibitors of BCRP/ABCG2

Future Medicinal Chemistry, 2015
BCRP/ABCG2, a second member of ABC transporter subclass G, has been shown to be overexpressed in several solid tumors, acute myelogenous leukemia and chronic myeloid leukemia. A variety of chemically unrelated anticancer drugs have been found to be transported by ABCG2 leading to their lower intracellular accumulation and hence causing chemoresistance.
Kapil, Juvale, Michael, Wiese
openaire   +2 more sources

Metabolism of KO143, an ABCG2 inhibitor

Drug Metabolism and Pharmacokinetics, 2017
The 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, Junjie, Zhu, Yixian, Huang, Chaoyue, Li, Jie, Lu, Madhav, Sachar, Song, Li, Xiaochao, Ma   +7 more
openaire   +2 more sources

Assessing the ABCG2 Protein Interactome: a Potential Strategy to Disrupt ABCG2 Function

The FASEB Journal, 2020
The 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, Tomoka Gose, John D. Schuetz   +2 more
openaire   +1 more source

Physiological and pharmacological roles of ABCG2 (BCRP): Recent findings in Abcg2 knockout mice

Advanced Drug Delivery Reviews, 2009
The 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, Jurjen S, Lagas, Alfred H, Schinkel   +2 more
openaire   +2 more sources

Comparative analysis of ABCG2+ and ABCG2-retinoblastoma cells in three-dimensional culture

Oncocytology Journal, 2014
Aims: 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, Ruby Yanru Chen-Tsai, Robert Diaz, Linda Cassidy   +3 more
openaire   +1 more source

Differential inhibition of murine Bcrp1/Abcg2 and human BCRP/ABCG2 by the mycotoxin fumitremorgin C

European Journal of Pharmacology, 2010
Breast 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, Rebeca, Real, Julio G, Prieto, Ana I, Alvarez, Gracia, Merino   +4 more
openaire   +2 more sources