Results 191 to 200 of about 26,096 (220)
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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 K Tiwari, Zhe-Sheng Chen
exaly   +3 more sources

Superior Pyrimidine Derivatives as Selective ABCG2 Inhibitors and Broad-Spectrum ABCB1, ABCC1, and ABCG2 Antagonists

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
openaire   +2 more sources

ABCG2/BCRP: Specific and Nonspecific Modulators

Medicinal Research Reviews, 2016
AbstractMultidrug 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
openaire   +2 more sources

Comparison of chemotherapeutic drug resistance in cells transfected with canineABCG2or felineABCG2

Veterinary and Comparative Oncology, 2015
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
openaire   +2 more sources

Role of ABCG2 in Transport of the Mammalian Lignan Enterolactone and its Secretion into Milk in Abcg2 Knockout Mice

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
openaire   +2 more sources

ABCG2 as a therapeutic target candidate for gout

Expert Opinion on Therapeutic Targets, 2017
Hyperuricemia (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
openaire   +2 more sources

Trials and Tribulations in the Expression and Purification of ABCG2

2016
ABC (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 ...
openaire   +2 more sources

Cryo-EM Structures of a Human ABCG2 Mutant Trapped in ATP-Bound and Substrate-Bound States

Nature, 2018
Henning Stahlberg   +2 more
exaly  

Single Nucleotide Polymorphisms Modify the Transporter Activity of ABCG2

Cancer Chemotherapy and Pharmacology, 2005
Rob Robey   +2 more
exaly  

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