Results 11 to 20 of about 26,813 (237)
Karanjin interferes with ABCB1, ABCC1, and ABCG2 [PDF]
Journal of Pharmacy & Pharmaceutical Sciences, 2014 PURPOSE: The prominent ATP-binding cassette (ABC) transporters ABCB1, ABCC1, and ABCG2 are involved in substance transport across physiological barriers and therefore in drug absorption, distribution, and elimination. They also mediate multi-drug resistance in cancer cells.
Martin Michaelis +5 more
core +6 more sources
Journal of Pharmacy & Pharmaceutical Sciences, 2014 PURPOSE: The clinically approved oncogenic BRAF inhibitor PLX4032 (vemurafenib) was shown to be a substrate of the ATP-binding cassette (ABC) transporter ABCB1. Here, we compared PLX4032 and its structurally closely related precursor compound PLX4720 for
Martin Michaelis +7 more
doaj +2 more sources
Frontiers in Pharmacology, 2018 P-Glycoprotein (P-gp, Abcb1) plays a crucial role in drug disposition and functions by hydrolyzing ATP. However, little is known about the regulatory elements governing the transcription of the porcine Abcb1 gene.
Tingting Guo +7 more
doaj +2 more sources
Membrane Assays to Characterize Interaction of Drugs with ABCB1 [PDF]
The Journal of Membrane Biology, 2015 ATP-binding cassette sub-family B member 1 (ABCB1) [P-glycoprotein (P-gp), multidrug resistance protein 1 (MDR1)] can affect the pharmacokinetics, safety, and efficacy of drugs making it important to identify compounds that interact with ABCB1. The ATPase assay and vesicular transport (VT) assay are membrane based assays that can be used to measure the
Zsolt, Fekete +11 more
openaire +4 more sources
ML210 Antagonizes ABCB1- Not ABCG2-Mediated Multidrug Resistance in Colorectal Cancer
BiomedicinesObjectives: ABCB1-mediated multidrug resistance (MDR) compromises chemotherapy efficacy in colorectal cancer (CRC). Despite decades of research, no selective ABCB1 inhibitor has achieved clinical success.
Yan-Chi Li +7 more
doaj +2 more sources
Genetic Polymorphisms in ABCB1 Influence the Pharmacodynamics of Tacrolimus
Therapeutic Drug Monitoring, 2013 Tacrolimus has a large interindividual pharmacokinetic variability, and quantification of its effect is difficult. It is a substrate of ABCB1, an efflux pump expressed more on CD8 T cells than on CD4 T cells. The ABCB1 3435C>T single-nucleotide polymorphism (SNP) has been associated with interindividual differences in ABCB1 activity and may influence ...
Vafadari, Ramin +7 more
openaire +3 more sources
Molecular Cancer, 2022 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
doaj +1 more source
Dynamic induction of drug resistance through a stress-responsive enhancer in acute myeloid leukemia
Molecular & Cellular Oncology, 2020 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
doaj +1 more source
The temporal relationship between ABCB1 promoter hypomethylation, ABCB1 expression and acquisition of drug resistance [PDF]
The Pharmacogenomics Journal, 2010 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
openaire +2 more sources
Pharmaceutics, 2020 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
doaj +1 more source