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About 1,553 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 multid...

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 16th, 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...

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

Dec 23rd, 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...

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 22nd, 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...

Expression of BCRP/ABCG2 Protein in Invasive Breast Cancer and Response t...
https://doi.org/10.1159/000520871
Oncology Research and Treatment; Zhang YS, Yang C et. al.

Nov 15th, 2021 - Breast cancer resistance protein (BCRP), or ATP-binding cassette subfamily G member 2 (ABCG2), is an ATP-binding cassette (ABC) transporter that mediates energy-dependent transport of substrate drugs out of the cell. Its overexpression may contribute to intrinsic drug resistance in vitro. However, the current literature has not yet clarified the clinical significance of BCRP...

Interactions between riluzole and ABCG2/BCRP transporter.
https://doi.org/10.1016/j.neulet.2008.12.061
Neuroscience Letters; Milane A, Vautier S et. al.

Jan 17th, 2009 - Amyotrophic lateral sclerosis (ALS) is a neurodegenerative fatal disease. Drugs used in this disease need to cross the blood-brain barrier (BBB). Only riluzole is approved for ALS treatment. We have investigated riluzole as a breast cancer resistance protein (BCRP) substrate by studying its brain transport in CF1 mdr1a (-/-) mice and its intracellular uptake on BeWo cells (human placental chori...

Regional expression of the BCRP/ABCG2 transporter in term human placentas.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3946646
Reproductive Toxicology (Elmsford, N.Y.); Memon N, Bircsak KM et. al.

Nov 26th, 2013 - The breast cancer resistance protein (BCRP, ABCG2) is an efflux transporter that removes xenobiotics that cross the placenta back to the maternal circulation, thereby limiting exposure of the fetus to drugs and chemicals. Currently, variability of BCRP expression within the placenta is not known. Ten placentas were collected from healthy women undergoing elective Cesarean s...

Differential inhibition of murine Bcrp1/Abcg2 and human BCRP/ABCG2...
https://doi.org/10.1016/j.ejphar.2010.07.016
European Journal of Pharmacology; González-Lobato L, Real R et. al.

Jul 27th, 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 phenotype. Fumitremorg...

Physiological and pharmacological roles of ABCG2 (BCRP): recent findings ...
https://doi.org/10.1016/j.addr.2008.08.007
Advanced Drug Delivery Reviews; Vlaming ML, Lagas JS et. al.

Jan 3rd, 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(-/-) mice, has re...

ABCG2/BCRP interaction with the sea grass Thalassia testudinum.
https://doi.org/10.1515/dmpt-2015-0013
Drug Metabolism and Personalized Therapy; Miguel V, Otero JA et. al.

Oct 8th, 2015 - The aqueous ethanolic extract from leaves of the marine plant Thalassia testudinum has shown antioxidant, cytoprotective, and neuroprotective properties. The chemical composition of this extract, rich in polyphenols, could interfere with active transport of drugs out of the cell and circumvent the phenomenon of multidrug resistance (MDR). The extract can act as an MDR modulator through its inte...

Interaction of Isoflavones with the BCRP/ABCG2 Drug Transporter.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4713194
Current Drug Metabolism; Bircsak KM, Aleksunes LM

Jul 17th, 2015 - This review will provide a comprehensive overview of the interactions between dietary isoflavones and the ATP-binding cassette (ABC) G2 efflux transporter, which is also named the breast cancer resistance protein (BCRP). Expressed in a variety of organs including the liver, kidneys, intestine, and placenta, BCRP mediates the disposition and excretion of numerous endogenous chemicals and xenobio...

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 12th, 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 utilized to test...

BCRP/ABCG2 inhibition sensitizes hepatocellular carcinoma cells to sorafe...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3877048
PloS One; Huang WC, Hsieh YL et. al.

Jan 7th, 2014 - The multikinase inhibitor, sorafenib (Nexavar®, BAY43-9006), which inhibits both the Raf/MEK/ERK pathway and several receptor tyrosine kinases (RTKs), has shown significantly therapeutic benefits in advanced hepatocellular carcinoma (HCC). However, not all HCC patients respond to sorafenib well and new therapeutic strategies to optimize the efficacy of sorafenib are urgently required. Overexpre...

Structure and function of the human breast cancer resistance protein (BCRP/AB...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2950214
Current Drug Metabolism; Ni Z, Bikadi Z et. al.

Sep 4th, 2010 - The human breast cancer resistance protein (BCRP/ABCG2) is the second member of the G subfamily of the large ATP-binding cassette (ABC) transporter superfamily. BCRP was initially discovered in multidrug resistant breast cancer cell lines where it confers resistance to chemotherapeutic agents such as mitoxantrone, topotecan and methotrexate by extruding these compounds out ...

BCRP/ABCG2 confers anticancer drug resistance without covalent dimerization.
https://doi.org/10.1111/j.1349-7006.2010.01605.x
Cancer Science; Shigeta J, Katayama K et. al.

Jun 4th, 2010 - In previous studies, we demonstrated that the breast cancer resistance protein (BCRP, ABCG2) forms an S-S homodimer. The BCRP-C603S mutant substituting Ser for Cys-603 in the third extracellular domain formed both a 70-75-kDa monomer and 140-150-kDa dimer, suggesting that Cys-603 is an important residue in the covalent bridge. These results also suggested the involvement of...

Pharmacogenomics of MRP transporters (ABCC1-5) and BCRP (ABCG2).
https://doi.org/10.1080/03602530801952617
Drug Metabolism Reviews; Gradhand U, Kim RB

May 9th, 2008 - Elucidation of the key mechanisms that confer interindividual differences in drug response remains an important focus of drug disposition and clinical pharmacology research. We now know both environmental and host genetic factors contribute to the apparent variability in drug efficacy or in some cases, toxicity. In addition to the widely studied and recognized genes involved in the metabolism o...

BCRP/ABCG2 in the placenta: expression, function and regulation.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2346511
Pharmaceutical Research; Mao Q

Jan 19th, 2008 - Knowledge concerning transport of maternally administered drugs across the placental barrier is essential for determining potential toxicity of drugs to the fetus and the value of drug therapy during pregnancy. An important determinant for fetal drug exposure is the expression of efflux transporters in the placenta. Among human tissues, the ATP-binding cassette efflux transporter BCRP (g...

BCRP/ABCG2 Transporter Regulates Accumulation of Cadmium in Kidney Cells:...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8382159
Drug Metabolism and Disposition: the Biological Fate of C... Wen X, Kozlosky D et. al.

Jun 3rd, 2021 - Exposure to the environmental pollutant cadmium is ubiquitous, as it is present in cigarette smoke and the food supply. Over time, cadmium enters and accumulates in the kidneys, where it causes tubular injury. The breast cancer resistance protein (BCRP, ATP-Binding Cassette G2 ABCG2) is an efflux transporter that mediates the urinary secretion of pharmaceuticals and toxins. The

The role of human ABC transporter ABCG2 (BCRP) in pharmacotherapy.
https://doi.org/10.1016/j.addr.2008.12.001
Advanced Drug Delivery Reviews; Ishikawa T

Jan 7th, 2009 - The role of human ABC transporter ABCG2 (BCRP) in pharmacotherapy.|2009|Ishikawa T,|genetics,metabolism,physiology,genetics,metabolism,physiology,metabolism,

New trends for overcoming ABCG2/BCRP-mediated resistance to cancer therap...
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4696234
Journal of Experimental & Clinical Cancer Research : CR; Westover D, Li F

Dec 31st, 2015 - ATP-binding cassette (ABC) transporters make up a superfamily of transmembrane proteins that play a critical role in the development of drug resistance. This phenomenon is especially important in oncology, where superfamily member ABCG2 (also called BCRP - breast cancer resistance protein) is known to interact with dozens of anti-cancer agents that are ABCG2 substrates. In ...