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Recent Advances in the Development of P-gp Inhibitors
Anti-Cancer Agents in Medicinal Chemistry, 2009During the last decades multidrug resistance (MDR) emerged as main problem in the anti-cancer therapy with cytostatically active agents. Classical as well as recently developed cytostatics develop the phenomenon of loosing activity in former drug-sensitive cells.
Christiane, Baumert, Andreas, Hilgeroth
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A porcine lymphocyte model for P‐gp inhibition studies
Journal of Veterinary Pharmacology and Therapeutics, 2011Short ...
Schrickx, J.A., Fink-Gremmels, J.
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Journal of Molecular Modeling, 2012
P-glycoprotein (P-gp) has a major role to play in drug pharmacokinetics and pharmacodynamics, since it effluxes many cytotoxic hydrophobic anticancer drugs from gastrointestinal tract, brain, liver and kidney. Piperine is known to enhance the bioavailability of curcumin, as a substrate of P-gp by at least 2000%.
Durg Vijay, Singh +2 more
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P-glycoprotein (P-gp) has a major role to play in drug pharmacokinetics and pharmacodynamics, since it effluxes many cytotoxic hydrophobic anticancer drugs from gastrointestinal tract, brain, liver and kidney. Piperine is known to enhance the bioavailability of curcumin, as a substrate of P-gp by at least 2000%.
Durg Vijay, Singh +2 more
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Pharmaceutical Research, 2004
To determine whether female sex-steroid hormones and their metabolites can modulate P-glycoprotein (P-gp) expression and catalytic activity and to investigate P-gp mediated transport of these sex-steroids across MDR1-transfected Madine-Darby canine kidney (MDCK) cells.Changes in P-gp protein and MDR1 mRNA expression levels were examined in the presence
Winnie Y, Kim, Leslie Z, Benet
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To determine whether female sex-steroid hormones and their metabolites can modulate P-glycoprotein (P-gp) expression and catalytic activity and to investigate P-gp mediated transport of these sex-steroids across MDR1-transfected Madine-Darby canine kidney (MDCK) cells.Changes in P-gp protein and MDR1 mRNA expression levels were examined in the presence
Winnie Y, Kim, Leslie Z, Benet
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Pharmaceutical Research, 2023
The differences between intestinal and systemic (hepatic and renal) P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) roles in drug disposition are difficult to define. Accordingly, we characterized Encequidar (ECD) as an intestinal P-gp and BCRP specific inhibitor to evaluate their role in drug disposition.We assessed the in vitro and ...
Jessica Chu +12 more
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The differences between intestinal and systemic (hepatic and renal) P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) roles in drug disposition are difficult to define. Accordingly, we characterized Encequidar (ECD) as an intestinal P-gp and BCRP specific inhibitor to evaluate their role in drug disposition.We assessed the in vitro and ...
Jessica Chu +12 more
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Importance of P-gp PET Imaging in Pharmacology
Current Pharmaceutical Design, 2016Capillary endothelial cells in the brain express P-glycoprotein (P-gp), which works as a functional blood-brain barrier (BBB). P-gp pumps out multiple types of molecules from the brain parenchyma into the blood. Therefore, altered P-gp function at the BBB will change the concentrations of therapeutic drugs in the central nervous system (CNS) and hence ...
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P-gp Transporter and its Role in Neurodegenerative Diseases
Current Topics in Medicinal Chemistry, 2009This paper describes an overview of recent insights concerning some socially relevant neurodegenerative diseases such as Alzheimer's (AD), Parkinson's (PD), Huntington's (HD) and Creutzfeldt-Jakob's (CJD) diseases, amyotrophic lateral sclerosis (ALS) and epilepsy.
RAPPOSELLI, SIMONA +2 more
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Drug Efflux Transporters: P-gp and BCRP
2021The efflux transporters P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) play important roles in protecting tissues from potentially harmful xenobiotic substances, mainly by virtue of their location in the intestinal epithelium and in the blood–brain barrier.
Peter Bungay, Sharan Bagal
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Flavonoids as P-gp Inhibitors: A Systematic Review of SARs
Current Medicinal Chemistry, 2019P-glycoprotein, also known as ABCB1 in the ABC transporter family, confers the simultaneous resistance of metastatic cancer cells towards various anticancer drugs with different targets and diverse chemical structures.
Jiahua, Cui +2 more
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Effect of berberine on the pharmacokinetics of substrates of CYP3A and P‐gp
Phytotherapy Research, 2009AbstractThein vivoeffects of berberine (BBR), the widely used bioactive herbal ingredient from many traditional Chinese medicinal herbs, on the pharmacokinetics of carbamazepine (CBZ, a substrate of CYP3A) and its metabolite carbamazepine 10,11‐epoxide (ECBZ), digoxin (DIG, a substrate of P‐gp) and cyclosporine A (CsA, a dual substrate of CYP3A and P ...
W, Qiu +4 more
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