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About 530 results

The multidrug transporter ABCG2 (BCRP) is inhibited by plant‐derived cannabinoids
https://bpspubs.onlinelibrary.wiley.com/doi/full/10.1038/sj.bjp.0707467
British Journal of Pharmacology;

Background and purpose: Cannabinoids are used therapeutically for the palliation of the adverse side effects associated with cancer chemotherapy. However, cannabinoids also inhibit both the activity and expression of the multidrug transporter, P‐glycoprotein in vitro. Here we address the interaction of cannabinol (CBN), cannabidiol (CBD) and Δ9‐tetrahydrocannabinol (THC) with the related multi...

Breast cancer resistance protein BCRP (ABCG2)-mediated transepithelial ni...
https://doi.org/10.1016/j.ejphar.2011.10.004
European Journal of Pharmacology; Wright JA, Haslam IS et. al.

Oct 18th, 2011 - In order to determine the capacity and regulation of the breast cancer resistance protein (BCRP)-mediated transport in intact human intestinal epithelial monolayers (Caco-2) in which multiple ABC transporters are expressed, nitrofurantoin has been used as a selective transported substrate. Nitrofurantoin transepithelial secretion was confirmed in both human BCRP and mouse bcrp...

In vivo inhibition of BCRP/ABCG2 mediated transport of nitrofurantoin by ...
https://doi.org/10.1007/s11095-010-0208-5
Pharmaceutical Research; Merino G, Perez M et. al.

Jul 7th, 2010 - The aim of this study was to determine in vivo inhibition by the isoflavones genistein and daidzein of nitrofurantoin (NTF), a well-known substrate of the ABC transporter BCRP/ABCG2. MDCKII cells and their human BCRP- and murine Bcrp1-transduced subclones were used to establish inhibition in transepithelial transport assays. Bcrp1(-/-) and wild-type mice were coadministered...

ABCG2/BCRP: variants, transporter interaction profile of substrates and i...
https://doi.org/10.1080/17425255.2019.1591373
Expert Opinion on Drug Metabolism & Toxicology; Safar Z, Kis E et. al.

Mar 11th, 2019 - ABCG2 has a broad substrate specificity and is one of the most important efflux proteins modulating pharmacokinetics of drugs, nutrients and toxicokinetics of toxicants. ABCG2 is an important player in transporter-mediated drug-drug interactions (tDDI). Areas covered: The aims of the review are i) to cover transporter interaction profile of substrates and inhibitors that can be ut...

Placental BCRP/ABCG2 Transporter Prevents Fetal Exposure to the Estrogeni...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6432861
Toxicological Sciences : an Official Journal of the Society of Toxicology; Szilagyi JT, Gorczyca L et. al.

Dec 23rd, 2018 - In the placenta, the breast cancer resistance protein (BCRP)/ABCG2 efflux transporter limits the maternal-to-fetal transfer of drugs and chemicals. Previous research has pointed to the estrogenic mycotoxin zearalenone as a potential substrate for BCRP. Here, we sought to assess the role of the BCRP transporter in the transplacental disposition of zearalenone during p...

Characterization of the breast cancer resistance protein (BCRP/ABCG2) in ...
https://doi.org/10.1002/ijc.31741
International Journal of Cancer; Reustle A, Fisel P et. al.

Aug 2nd, 2018 - The efflux transporter breast cancer resistance protein BCRP/ABCG2 is well-known for its contribution to multi-drug resistance in cancer. Its relevance in cancer biology independent from drug efflux remains largely elusive. Our study aimed at elucidating the biological relevance and regulatory mechanisms of BCRP/ABCG2 in clear cell renal cell carcinoma (ccRCC) and di...

Neoadjuvant Endocrine Therapy in Breast Cancer Upregulates the Cytotoxic Drug Pump A...
https://doi.org/10.1016/j.clbc.2018.07.002
Clinical Breast Cancer; Baxter DE, Kim B et. al.

Jul 29th, 2018 - Neoadjuvant treatments for primary breast cancer are becoming more common; however, little is known about how these impact on response to subsequent adjuvant therapies. Conveniently, neoadjuvant therapy provides opportunities to consider this question, by studying therapy-induced expression changes using comparisons between pre- and posttreatment samples. These data are relatively lacking in th...

An update on expression and function of P-gp/ABCB1 and BCRP/ABCG2 in the ...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6290921
Expert Opinion on Drug Metabolism & Toxicology; Han LW, Gao C et. al.

Jul 16th, 2018 - P-glycoprotein (P-gp)/ABCB1 and breast cancer resistance protein (BCRP)/ABCG2 are highly expressed in the placenta and fetus throughout gestation and can modulate exposure and toxicity of drugs and xenobiotics to the vulnerable fetus during the sensitive times of growth and development. We aim to provide an update on current knowledge on placental and fetal expressions of the two ...

Buprenorphine, Norbuprenorphine, R-Methadone, and S-Methadone Upregulate BCRP/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5325079
Molecular Pharmacology; Neradugomma NK, Liao MZ et. al.

Dec 15th, 2016 - Opioid dependence during pregnancy is a rising concern. Maintaining addicted pregnant women on long-acting opioid receptor agonist is the most common strategy to manage drug abuse in pregnant women. Methadone (MET) and buprenorphine (BUP) are widely prescribed for opiate maintenance therapy. Norbuprenorphine (NBUP) is the primary active metabolite of BUP. These medications can cross the placent...

Extra-renal elimination of uric acid via intestinal efflux transporter BCRP/A...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3277506
PloS One; Hosomi A, Nakanishi T et. al.

Feb 21st, 2012 - Urinary excretion accounts for two-thirds of total elimination of uric acid and the remainder is excreted in feces. However, the mechanism of extra-renal elimination is poorly understood. In the present study, we aimed to clarify the mechanism and the extent of elimination of uric acid through liver and intestine using oxonate-treated rats and Caco-2 cells as a model of human intestinal epithel...

Evaluation of Alteration in Hepatic and Intestinal BCRP Function In Vivo from
https://doi.org/10.1124/dmd.117.078816
Drug Metabolism and Disposition: the Biological Fate of Chemicals; Futatsugi A, Toshimoto K et. al.

Feb 14th, 2018 - Polymorphism c.421C>A in the ABCG2 gene is thought to reduce the activity of breast cancer resistance protein (BCRP), a xenobiotic transporter, although it is not clear which organ(s) contributes to the polymorphism-associated pharmacokinetic change. The aim of the present study was to estimate quantitatively the influence of c.421C>A on intestinal and hepatic BCRP activity...

Local Drug-Drug Interaction of Donepezil with Cilostazol at Breast Cancer Resistance Pr...
https://doi.org/10.1124/dmd.115.066654
Drug Metabolism and Disposition: the Biological Fate of Chemicals; Takeuchi R, Shinozaki K et. al.

Oct 15th, 2015 - Clinical reports indicate that cardiotoxicity due to donepezil can occur after coadministration with cilostazol. We speculated that the concentration of donepezil in heart tissue might be increased as a result of interaction with cilostazol at efflux transporters such as P-glycoprotein (P-gp, ABCB1) and breast cancer resistance protein (BCRP, ABCG2), which are expressed in many ti...

The phytoestrogens daidzein and equol inhibit the drug transporter BCRP/ABCG2...
https://doi.org/10.1007/s00394-017-1578-9
European Journal of Nutrition; Rigalli JP, Scholz PN et. al.

Nov 4th, 2017 - The soy isoflavone genistein has been described to up-regulate breast cancer resistance protein (BCRP) and, thus, enhance chemoresistance in breast cancer cells. The aim of this work was to assess the effect of long- and short-term incubation with daidzein, the second most abundant soy isoflavone and its metabolite equol on the expression and activity of P-glycoprotein, multidrug resista...

Reverse Translational Research of ABCG2 (BCRP) in Human Disease and Drug ...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5760319
Clinical Pharmacology and Therapeutics; Brackman DJ, Giacomini KM

Oct 12th, 2017 - Reverse translational research takes a bedside-to-bench approach, using sophisticated basic research to explain the biological mechanisms behind observed clinical data. For transporters, which play a role in human disease and drug response, this approach offers a distinct advantage over the typical translational research, which often falters due to inadequate in vitro and preclinical animal mod...

Induction of ABCG2/BCRP restricts the distribution of zidovudine to the f...
https://doi.org/10.1016/j.taap.2017.07.005
Toxicology and Applied Pharmacology; Filia MF, Marchini T et. al.

Jul 14th, 2017 - Safety concerns for fetus development of zidovudine (AZT) administration as prophylaxis of vertical transmission of HIV persist. We evaluated the participation of the ATP-binding cassette efflux transporter ABCG2 in the penetration of AZT into the fetal brain and the relevance for drug safety. Oral daily doses of AZT (60mg/kg body weight) or its vehicle were administered between post ges...

Localization of the placental BCRP/ABCG2 transporter to lipid rafts: Role...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5497756
Placenta Szilagyi JT, Vetrano AM et. al.

Jun 18th, 2017 - The breast cancer resistance protein (BCRP/ABCG2) is an efflux transporter in the placental barrier. By transporting chemicals from the fetal to the maternal circulation, BCRP limits fetal exposure to a range of drugs, toxicants, and endobiotics such as bile acids and hormones. The purpose of the present studies was to 1) determine whether BCRP localizes to highly-or...

Expression and Activity of Breast Cancer Resistance Protein (BCRP/ABCG2) ...
https://doi.org/10.1007/s11095-017-2172-9
Pharmaceutical Research; Nickel S, Selo MA et. al.

May 4th, 2017 - Breast cancer resistance protein (BCRP/ABCG2) has previously been identified with high expression levels in human lung. The subcellular localisation and functional activity of the transporter in lung epithelia, however, remains poorly investigated. The aim of this project was to study BCRP expression and activity in freshly isolated human alveolar epithelial type 2 (AT2) an...

Small-Dosing Clinical Study: Pharmacokinetic, Pharmacogenomic (SLCO2B1 and ABCG2...
https://doi.org/10.1016/j.xphs.2017.03.010
Journal of Pharmaceutical Sciences; Kashihara Y, Ieiri I et. al.

Mar 22nd, 2017 - The aims of this study were (1) to investigate the effects of atorvastatin (10 mg, therapeutic dose) and grapefruit juice (GFJ), inhibitors of OATP2B1, on the pharmacokinetics of substrates for OATP2B1 and BCRP under oral small-dosing conditions (300 μg sulfasalazine, 250 μg rosuvastatin, 300 μg glibenclamide, 1200 μg celiprolol, and 600 μg sumatriptan), and (2) to evaluate the contribut...

Down-regulation of the placental BCRP/ABCG2 transporter in response to hy...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5354084
Placenta Francois LN, Gorczyca L et. al.

Mar 15th, 2017 - The BCRP/ABCG2 efflux transporter protects the developing fetus by limiting the transplacental transfer of drugs and chemicals and prevents the apoptosis of trophoblasts. The purpose of this study was to determine whether hypoxia-related signaling alters placental BCRP expression and function in vitro and in human pregnancies. Human BeWo choriocarcinoma cells were treated w...

ABCG2/BCRP: Specific and Nonspecific Modulators.
https://doi.org/10.1002/med.21428
Medicinal Research Reviews; Peña-Solórzano D, Stark SA et. al.

Dec 22nd, 2016 - Multidrug 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. MDR is associated with increased drug efflux from cells mediated by an energy-dependent mechanism involving the ATP-binding cassette (ABC...