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ABCB1, also known as MDR1, is a gene that encodes P-glycoprotein (P-gp), a membrane-associated ATP-dependent transporter. P-gp is widely expressed in many healthy tissues—in the gastrointestinal tract, liver, kidney, and at the blood–brain barrier. P-gp works to pump xenobiotics such as toxins and drugs out of cells.
Katie T. Skinner +2 more
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Highlights ABCB1 overexpression significantly desensitized both drug-selected and gene-transfected cells, which overexpress ABCB1, to OTS964 and that this drug resistance can be antagonized by verapamil, a known ABCB1 inhibitor.
Yuqi Yang +8 more
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Dynamic induction of drug resistance through a stress-responsive enhancer in acute myeloid leukemia
The drug efflux pump ABCB1 (ATP binding cassette subfamily B member 1) confers chemotherapy resistance in acute myeloid leukemia (AML). We recently identified an ABCB1 enhancer that is activated in response to a range of cellular stressors, including ...
Mark S. Williams, Tim C. P. Somervaille
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Palbociclib was approved by the United States Food and Drug Administration for use, in combination with letrozole, as a first-line treatment for estrogen receptor-positive/human epidermal growth factor receptor 2-negative (ER+/HER2-) postmenopausal ...
Han Fu +9 more
doaj +1 more source
The temporal relationship between ABCB1 promoter hypomethylation, ABCB1 expression and acquisition of drug resistance [PDF]
Induced expression of the Abcb1 drug transporter often occurs in tumors in response to chemotherapy. The role that epigenetic modifications within the ABCB1 promoter play in Abcb1 expression remains unclear. We selected MCF-7 cells for survival in increasing doses of chemotherapy drugs, and assessed the methylation status of 66 CpG sites within the ...
K, Reed +3 more
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International Veterinary Epilepsy Task Force consensus proposal: Medical treatment of canine epilepsy in Europe [PDF]
In Europe, the number of antiepileptic drugs (AEDs) licensed for dogs has grown considerably over the last years. Nevertheless, the same questions remain, which include, 1) when to start treatment, 2) which drug is best used initially, 3) which ...
A Fischer +148 more
core +13 more sources
The rat is one of the most commonly used animal models in pre-clinical studies. Limited information between the sexes and the effect of food consumption on the gastrointestinal (GI) physiology, however, is acknowledged or understood.
Liu Dou +7 more
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Low ABCB1 gene expression is an early event in colorectal carcinogenesis. [PDF]
The ABCB1/MDR1 gene product ABCB1/P-glycoprotein is implicated in the development of colorectal cancer (CRC). NFKB1 encodes transcription factors regulating expression of a number of genes including ABCB1. We have previously found association between the
Vibeke Andersen +7 more
doaj +1 more source
Mechanism of multidrug recognition by MDR1/ABCB1 [PDF]
MDR1/ABCB1, a member of the ABC group of proteins, is clinically important because it is not only involved in multidrug resistance in cancer but also affects the pharmacokinetic properties of various drugs. The most puzzling feature of MDR1 is that it recognizes and transports such a wide variety of substrates.
Yasuhisa, Kimura +3 more
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Purvalanol A, olomoucine II and roscovitine inhibit ABCB1 transporter and synergistically potentiate cytotoxic effects of daunorubicin in vitro. [PDF]
Cyclin-dependent kinase inhibitors (CDKi) have high potential applicability in anticancer therapy, but various aspects of their pharmacokinetics, especially their interactions with drug efflux transporters, have not yet been evaluated in detail. Thus, we
Daniela Cihalova +3 more
doaj +1 more source

