Results 11 to 20 of about 29,397 (197)
Differential Effects of the Oncogenic BRAF Inhibitor PLX4032 (Vemurafenib) and its Progenitor PLX4720 on ABCB1 Function [PDF]
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 +4 more sources
Low ABCB1 gene expression is an early event in colorectal carcinogenesis. [PDF]
PLoS ONE, 2013 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 +2 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
Molecules, 2016 In recent years, tyrosine kinase inhibitors (TKIs) have been shown capable of inhibiting the ATP-binding cassette (ABC) transporter-mediated multidrug resistance (MDR). In this study, we determine whether osimertinib, a novel selective, irreversible EGFR
Xiao-Yu Zhang +8 more
doaj +2 more sources
ABCB1 Frameshift Deletion in Skye Terriers With Potential Pharmacogenetic Relevance. [PDF]
Anim GenetABSTRACT Ivermectin‐associated neurotoxicity is a potentially life‐threatening condition caused by disruption of the ABCB1 encoded P‐glycoprotein drug transporter in certain dog breeds. Skye terriers are considered at increased risk of ivermectin toxicity despite the absence of an identified molecular cause.
Nielsen M +4 more
europepmc +2 more sources
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
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
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Frontiers in Pharmacology, 2022 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
Purvalanol A, olomoucine II and roscovitine inhibit ABCB1 transporter and synergistically potentiate cytotoxic effects of daunorubicin in vitro. [PDF]
PLoS ONE, 2013 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
Targeted nanopore sequencing for the identification of ABCB1 promoter translocations in cancer
BMC Cancer, 2020 Background Resistance to chemotherapy is the most common cause of treatment failure in acute myeloid leukemia (AML) and the drug efflux pump ABCB1 is a critical mediator.
Mark S. Williams +9 more
doaj +1 more source