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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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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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ABCG2/BCRP: Specific and Nonspecific Modulators
Medicinal Research Reviews, 2016AbstractMultidrug resistance (MDR) in cancer cells is the development of resistance to a variety of structurally and functionally nonrelated anticancer drugs. This phenomenon has become a major obstacle to cancer chemotherapy seriously affecting the clinical outcome.
Diana, Peña-Solórzano +4 more
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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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Journal of Medicinal Chemistry, 2020
In the search for highly effective modulators addressing ABCG2-mediated MDR, 23 pyrimidines were synthesized and biologically assessed. Seven derivatives with (a) nitrogen- and/or halogen-containing residue(s) had extraordinary potencies against ABCG2 (IC50 < 150 nM). The compounds competitively inhibited ABCG2-mediated Hoechst 33342 transport but were
Katja Silbermann +6 more
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In the search for highly effective modulators addressing ABCG2-mediated MDR, 23 pyrimidines were synthesized and biologically assessed. Seven derivatives with (a) nitrogen- and/or halogen-containing residue(s) had extraordinary potencies against ABCG2 (IC50 < 150 nM). The compounds competitively inhibited ABCG2-mediated Hoechst 33342 transport but were
Katja Silbermann +6 more
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ABCG2 as a therapeutic target candidate for gout
Expert Opinion on Therapeutic Targets, 2017Hyperuricemia (chronically elevated serum uric acid) is the main pathology underlying the development of gout, the most common inflammatory arthropathy. Management of these conditions therefore relies on controlling serum uric acid levels. ATP-binding cassette transporter, sub-family G, member 2 (ABCG2/BCRP) is a well-studied urate transporter ...
Kyoko Fujita, Kimiyoshi Ichida
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Comparison of chemotherapeutic drug resistance in cells transfected with canine
AbstractABCG2(ATP binding cassette subfamily G, member 2) mediates resistance to a variety of cytotoxic agents. Although humanABCG2is well characterized, the function of canineABCG2has not been studied previously. FelineABCG2has an amino acid substitution in the adenosine triphosphate‐binding domain that decreases its transport capacity relative to ...
R S, Lewis +5 more
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Drug Metabolism and Disposition, 2014
Lignans are phytoestrogens that are metabolized by the gut microbiota to enterodiol and enterolactone, the main biologically active enterolignans. Substantial interindividual variation in plasma concentration and urinary excretion of enterolignans has been reported, this being determined, at least in part, by the intake of lignan precursors, the gut ...
Verónica, Miguel +6 more
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Lignans are phytoestrogens that are metabolized by the gut microbiota to enterodiol and enterolactone, the main biologically active enterolignans. Substantial interindividual variation in plasma concentration and urinary excretion of enterolignans has been reported, this being determined, at least in part, by the intake of lignan precursors, the gut ...
Verónica, Miguel +6 more
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Trials and Tribulations in the Expression and Purification of ABCG2
2016ABC (ATP binding cassette) transporters are a diverse superfamily of membrane proteins, which couple the transport of substrate with the hydrolysis of ATP. ABCG2 (ATP binding cassette G2, also known as Breast Cancer Resistance Protein (BCRP), is a well-known multidrug efflux pump that transports a wide range of structurally unrelated chemotherapeutic ...
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